Urethane-d5 (Ethyl carbamate-d5) is the deuterium labeled Urethane. Urethane (Ethyl carbamate), the ethyl ester of carbamic acid, is a byproduct of fermentation found in various food products. Urethane has the ability to suppress bacterial, protozoal, sea urchin egg, and plant tissue growth in vitro[1].
体外研究 (In Vitro)
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
94.12
Formula
C3H2D5NO2
CAS 号
73962-07-9
中文名称
氨基甲酸乙酯 d5
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
6 months
-20°C
1 month
参考文献
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.
[2]. K J Field, et al. Hazards of urethane (ethyl carbamate): a review of the literature. Lab Anim. 1988 Jul;22(3):255-62.;R E Sotomayor, et al. Mutagenicity, metabolism, and DNA interactions of urethane. Toxicol Ind Health. 1990 Jan;6(1):71-108.
Vinpocetine (Ethyl apovincaminate) is a derivative of the alkaloid Vincamine that blocks voltage-gated Na+ channels. The IC50 value of Vinpocetine on direct IKK inhibition in the cell-free system is 17.17 μM. Vinpocetine is a phosphodiesterase (PDE) inhibitor and inhibits NF-κB-dependent inflammatory responses by directly targeting IκB kinase complex (IKK), and has been widely used for the treatment of cerebrovascular disorders[1][2][3].
IC50 & Target
IKK
17.17 μM (IC50)
体外研究 (In Vitro)
Vinpocetine (5-50 μM; 7 hours; VSMCs, HUVECs, A549 cells and RAW264.7 cells) potently inhibits TNF-α-induced NF-κB-dependent transcriptional activity in a dose-dependent manner with an approximate IC50 value of 25 μM. Vinpocetine do not have a significant effect on cell viability[1]. Vinpocetine (50 μM; 7 hours; VSMCs, HUVECs, A549 cells and RAW264.7 cells) potently inhibits TNF-α-induced up-regulation of TNF-α, IL-1β, IL-8, MCP-1, VCAM-1, ICAM-1and MIP-2 transcripts in several cell types[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
RT-PCR[1]
Cell Line:
VSMCs, HUVECs, A549 cells and RAW264.7 cells
Concentration:
50 μM
Incubation Time:
7 hours
Result:
Inhibited TNF-α-induced up-regulation of TNF-α, IL-1β, IL-8, MCP-1, VCAM-1, ICAM-1and MIP-2 transcripts in several cell types.
体内研究 (In Vivo)
Vinpocetine (2.5-10 mg/kg; intraperitoneal injection; C57BL/6 mice) potently inhibits TNF-α- or LPS-induced up-regulation of proinflammatory mediators, including TNF-α, IL-1β, and MIP-2, and decreases interstitial infiltration of polymorphonuclear leukocytes in a mouse model of TNF-α- or LPS-induced lung inflammation[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
C57BL/6 mice (8 weeks of age)[1]
Dosage:
2.5 mg/kg, 5 mg/kg, and 10 mg/kg
Administration:
Intraperitoneal injection
Result:
Inhibited TNF-α- or LPS-induced up-regulation of proinflammatory mediators, including TNF-α, IL-1β, and MIP-2, and decreased interstitial infiltration of polymorphonuclear leukocytes in a mouse model of TNF-α- or LPS-induced lung inflammation.
Clinical Trial
分子量
350.45
Formula
C22H26N2O2
CAS 号
42971-09-5
中文名称
长春西汀；长春西丁；长春乙酯；卡兰；阿扑长春胺酸乙酯；长春酸乙酯
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Kye-Im Jeon et al. Vinpocetine inhibits NF-κB-dependent inflammation via an IKK-dependent but PDE-independent mechanism PNAS May 25, 2010 vol. 107 no. 21 9795-9800
[2]. Patyar S, et al. Role of vinpocetine in cerebrovascular diseases. Pharmacol Rep. 2011;63(3):618-28.
[3]. Alexandre E. Medina Vinpocetine as a potent antiinflammatory agent PNAS June 1, 2010, Vol. 107, No. 22 9921-9922.
Telotristat ethyl (LX1032) is a novel, orally-delivered inhibitor of tryptophan hydroxylase that reduces serotonin production.
体内研究 (In Vivo)
Telotristat ethyl (15, 50, 150, 300 mg/kg, po, qd) reduces serotonin content in the periphery, but not in the brain of the mice. Telotristat ethyl (200 mg/kg po, qd) prevents the increase in blood neutrophil counts that is observed after TNBS challenge, provides significant protection in a mouse model of inflammatory bowel disease. Telotristat ethyl (200 mg/kg po, qd) protects the mouse IBD model confirmed by histopathology evaluation[1]. Telotristat ethyl (15, 50, 150, 300 mg/kg) depletes 5-HT from the jejunum but not the brain. But Telotristat ethyl (200 mg/kg, p.o.) does not deplete enteric neuronal serotonin (5-HT), or alter constitutive gastrointestinal motility in mice. Telotristat ethyl (200 mg/kg) alleviates the severity of trinitrobenzene sulfonic acid (TNBS)-induced colitis[2].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
分子量
574.98
Formula
C27H26ClF3N6O3
CAS 号
1033805-22-9
中文名称
特罗司他乙酯
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Tamas Oravecz, et al. LX1606 (aka LX1032), a Novel Inhibitor of Serotonin Synthesis, Alleviates Development of Inflammatory Bowel Disease in a Preclinical Model.
[2]. Margolis, K.G., et al., Pharmacological reduction of mucosal but not neuronal serotonin opposes inflammation in mouse intestine. Gut, 2013.
Animal Administration [2]
For studies of the effects of peripheral TPH inhibitors on gut and brain 5-HT concentrations, LP-920540 is formulated in 0.1% Tween 80 in 0.25% methylcellulose and administered to mice once daily via oral gavage at 10 mL/kg for 4 consecutive days. Telotristat ethyl is formulated in 15% cyclodextrin (CaptisolTM, pH 3-4) or 0.25% methylcellulose and given to mice once daily via oral gavage at 10 mL/kg for 4 consecutive days. Whole brain, jejunum and colon (mesentery fat removed, gut lumen opened and blotted dry) are collected, snap frozen, and stored at -80ºC for future. LP-920540, Telotristat ethyl, LP-778914, LP-778920 and vehicle control are also formulated with 0.5% methycellulose at appropriate doses in coded vials. The contents of the coded vials are given by oral gavage in amounts determined by the weights of the recipient mice. After the experiments, results are analyzed.
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献
[1]. Tamas Oravecz, et al. LX1606 (aka LX1032), a Novel Inhibitor of Serotonin Synthesis, Alleviates Development of Inflammatory Bowel Disease in a Preclinical Model.
[2]. Margolis, K.G., et al., Pharmacological reduction of mucosal but not neuronal serotonin opposes inflammation in mouse intestine. Gut, 2013.
Urethane (Ethyl carbamate), the ethyl ester of carbamic acid, is a byproduct of fermentation found in various food products. Urethane has the ability to suppress bacterial, protozoal, sea urchin egg, and plant tissue growth in vitro[1].
体外研究 (In Vitro)
Urethane is a good clastogen in mammalian somatic cells in vivo, but it shows variable results with cells in vitro. Urethane efficiently induces sister chromatid exchanges in a variety of cells[2].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
Urethane has been used for many years to produce hypnosis and narcosis in mammals, fish, and amphibians. At anaesthetic dosages (1-1.2 g/kg body weight for rats) Urethane has a wide margin of safety and causes minimal changes in blood pressure, aortic blood flow, and blood-gas values[1]. At a dosage of 1g/kg IP (administered intraperitoneally), Urethane will arrest cell division in the crypt of liberkuhn cells in mice[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
分子量
89.09
Formula
C3H7NO2
CAS 号
51-79-6
中文名称
氨基甲酸乙酯；尿烷；乌来糖
运输条件
Room temperature in continental US; may vary elsewhere.
Ethyl Caffeate is a natural phenolic compound isolated from Bidens pilosa. Ethyl caffeate suppresses NF-κB activation and its downstream inflammatory mediators, inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2), and prostaglandin E2 (PGE2) in vitro or in mouse skin[1].
IC50 & Target[1]
NF-κB
COX-2
体外研究 (In Vitro)
Ethyl Caffeate markedly suppresses the lipopolysaccharide (LPS)-induced nitric oxide (NO) production with IC50 of 5.5 μg/ml[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
208.21
Formula
C11H12O4
CAS 号
102-37-4
中文名称
咖啡酸乙酯
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Chiang YM, et al. Ethyl caffeate suppresses NF-kappaB activation and its downstream inflammatory mediators, iNOS, COX-2, and PGE2 in vitro or in mouse skin. Br J Pharmacol. 2005 Oct;146(3):352-63.
Ethyl orsellinate is a lichen metabolite and a derivative of lecanoric acid with antiproliferative and antitumour activities[1]. Ethyl Orsellinate is against A. salina for the cytotoxic activity with an LC50 of 495 μM[2].
体外研究 (In Vitro)
Ethyl Orsellinate (0-50 μg/ml; 48 hours) inhibits Hep-2 cells, MCF-7 breast cancer cells, and 786-0 kidney carcinoma cells, as well as B16-F10 murine melanoma and non-cancerous Vero cells (IC50s=31.2, 70.3, 47.5, 64.8, and 28.1 µg/ml, respectively)[2].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
196.20
Formula
C10H12O4
CAS 号
2524-37-0
中文名称
山梨酸乙酯
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
6 months
-20°C
1 month
参考文献
[1]. Bogo D, et al. In vitro antitumour activity of orsellinates. Z Naturforsch C. 2010 Jan-Feb;65(1-2):43-8.
[2]. Gomes AT, et al. Cytotoxic activity of orsellinates. Z Naturforsch C. 2006 Sep-Oct;61(9-10):653-7.
Atorvastatin ethyl ester is a derivative of Atorvastatin and displays strong inhibition of the 9-cis-RA-induced Gal4 reporter activity[1].
分子量
586.69
Formula
C35H39FN2O5
CAS 号
1146977-93-6
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Wang X , et al. Discovery of atorvastatin as a tetramer stabilizer of nuclear receptor RXRα through structure-based virtual screening. Bioorg Chem. 2019 Apr;85:413-419.
2′-Ethyl Simvastatin (compound 6) is a Mevinolin analog, with HMG-CoA reductase inhibition[1].
IC50 & Target
HMG-CoA reductase[1]
分子量
390.51
Formula
C23H34O5
CAS 号
79902-42-4
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. AGGARWAL, D., et al. A quantitative structure-activity relationship study of 3-hydroxy-3methylglutaryl-coenzyme A reductase inhibitors. Journal of Pharmacobio-Dynamics, 1988;11(9), 591–599.
[1]. Biswadip Banerji, et al. The inhibition of factor inhibiting hypoxia-inducible factor (FIH) by beta-oxocarboxylic acids. Chem Commun (Camb). 2005 Nov 21;(43):5438-40.
Ethyl gallate is a nonflavonoid phenolic compound and also a scavenger of hydrogen peroxide.
体外研究 (In Vitro)
Ethyl gallate is a nonflavonoid phenolic compound and also a scavenger of hydrogen peroxide. After treatment for 24 h or 48 h with Ethyl gallate, HL-60 cells show changes in morphology, including shrinkage of the cell membrane and the development of apoptotic bodies. Consistent with these effects, the viability of Ethyl gallate-treated cells decreases in a time- and dose-dependent manner, demonstrating that Ethyl gallate has a cytotoxic effect on HL-60 cells. Ethyl gallate treatment increases the proportion of cells in subG1 phase in a concentration- and time-dependent manner. Treatment of cells for 24 h or 48 h with 50 μM or 75 μM Ethyl gallate increases the percentage of cells in the subG1 phase from a baseline of 2.9% to 26.5% or 52.6%, respectively. It is found that Ethyl gallate treatment of HL-60 cells decreases the expression of Bcl-2 at 75 μM Ethyl gallate, and increases Bax and truncated Bid (tBid) expression at 24 h[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
No significant difference in the serum total protein, albumin, globulin and glucose is found between the rats fed with A. nilotica (L.) leaf extract on ethyl gallate equivalent basis and those fed with Ethyl gallate alone. Significant differences in total bilirubin level, however, exist between the rats that receive A. nilotica (L.) leaf extract, 500 mg/kg body weight (ethyl gallate equivalent of 10 mg/kg, 0.34±0.01 mg/dL) and those receiving 10 mg/kg body weight of Ethyl gallate (0.26±0.01 mg/dL). Significant difference is found for ALT between groups fed with 500 and 1000 mg/kg body weight of A. nilotica (L.) leaf extract (26.52±1.23 and 30.05±1.38 U/L) and 10 and 20 mg/kg of Ethyl gallate (20.50±0.94 and 24.67±1.13 U/L)[2].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
198.17
Formula
C9H10O5
CAS 号
831-61-8
中文名称
没食子酸乙酯
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Kim WH, et al. Ethyl gallate induces apoptosis of HL-60 cells by promoting the expression of caspases-8, -9, -3, apoptosis-inducing factor and endonuclease G. Int J Mol Sci. 2012;13(9):11912-22.
[2]. Mohan S, et al. In vitro protection of biological macromolecules against oxidative stress and in vivo toxicity evaluation of Acacia nilotica (L.) and ethyl gallate in rats. BMC Complement Altern Med. 2014 Jul 21;14:257.
Kinase Assay [1]
The expression of apoptosis-related proteins (caspases-8, -9, -3; AIF; Endo G; Bid; Bax; and Bcl-2) in HL-60 cells is determined by sodium dodecyl sulfate-polyacrylamide gel electrophoresis (SDS-PAGE) of lysates followed by western blotting. For this, HL-60 cells (1.5×106) are treated with 50 μM or 75 μM Ethyl gallate for 6 h, 12 h, or 24 h. Total cell lysates are obtained by resuspending cells in ice-cold radioimmunoprecipitation assay (RIPA) buffer for 30 min followed by centrifugation. Protein concentration is determined using a NanoDrop spectrophotometer. Aliquots of lysates (100 μg protein equivalents) are resolved by 12% SDS-PAGE and transferred onto nitrocellulose membranes[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay [1]
HL-60 cells (1×106) are treated with 50 μM or 75 μM Ethyl gallate for 24 h or 48 h at 37°C. Cells are then harvested by centrifugation and fixed in 70% ethanol at 4°C for 24 h. Fixed cells are resuspended in PBS containing 40 μg/mL Propidium iodide (PI), 100 μg/mL RNase A, and 0.1% Triton X-100 and incubated in the dark for 30 min at room temperature. Cell cycle distribution is analyzed by flow cytometry on a FACSCalibur. To investigate apoptotic cells, HL-60 cells (1×106) incubated with different concentration of 50 μM, 75 μM and 100 μM Ethyl gallate for 24 h or 48 h at 37°C, and then DAPI staining is conducted. The cells are photographed using a fluorescence microscopy[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration [2]
Forty eight female albino Wistar rats of six to eight weeks old are used and divided into eight groups based on their body weights. Group 1 rats serve as control receiving 1.0 mL of the vehicle (0.1% ethanol); Group 2 rats receive A. nilotica (L.) leaf extract (250 mg/kg body weight); Group 3 rats receive A. nilotica (L.) leaf extract (500 mg/kg body weight); Group 4 rats receive A. nilotica (L.) leaf extract (1000 mg/kg body weight); Group 5 rats receive A. nilotica (L.) leaf extract (2000 mg/kg body weight); Group 6 rats receive Ethyl gallate (5 mg/kg body weight); Group 7 rats receive Ethyl gallate (10 mg/kg body weight); Group 8 rats receive Ethyl gallate (20 mg/kg body weight). Body weights are recorded on 0th and 14th day for each group and all rats are decapitated after an overnight fast[2].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献
[1]. Kim WH, et al. Ethyl gallate induces apoptosis of HL-60 cells by promoting the expression of caspases-8, -9, -3, apoptosis-inducing factor and endonuclease G. Int J Mol Sci. 2012;13(9):11912-22.
[2]. Mohan S, et al. In vitro protection of biological macromolecules against oxidative stress and in vivo toxicity evaluation of Acacia nilotica (L.) and ethyl gallate in rats. BMC Complement Altern Med. 2014 Jul 21;14:257.
PEG3-bis-(ethyl phosphonate) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
IC50 & Target
PEGs
体外研究 (In Vitro)
PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
434.40
Formula
C16H36O9P2
CAS 号
160625-24-1
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. An S, et al. Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs. EBioMedicine. 2018 Oct;36:553-562
(E)-Ethyl p-methoxycinnamate is a natural product found in Kaempferia galangal with anti-inflammatory, anti-neoplastic and anti-microbial effects. (E)-Ethyl p-methoxycinnamate inhibits COX-1 and COX-2 in vitro with IC50s of 1.12 and 0.83 μM, respectively[1].
IC50 & Target[1]
COX-1
1.12 μM (IC50)
COX-2
0.83 μM (IC50)
分子量
206.24
Formula
C12H14O3
CAS 号
24393-56-4
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Umar MI, et al. Bioactivity-guided isolation of ethyl-p-methoxycinnamate, an anti-inflammatory constituent, from Kaempferia galangal L. extracts. Molecules. 2012 Jul 23;17(7):8720-34.
PEG5-bis-(Ethyl phosphonate) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
IC50 & Target
PEGs
体外研究 (In Vitro)
PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
522.50
Formula
C20H44O11P2
CAS 号
1446282-28-5
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. An S, et al. Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs. EBioMedicine. 2018 Oct;36:553-562
Alkyne-ethyl-PEG1-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
IC50 & Target
PEGs
体外研究 (In Vitro)
PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
198.26
Formula
C11H18O3
CAS 号
2100306-55-4
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. An S, et al. Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs. EBioMedicine. 2018 Oct;36:553-562
Ethyl 3,4-dihydroxybenzoate (Ethyl protocatechuate), an antioxidant, is a prolyl-hydroxylase inhibitor found in the testa of peanut seeds. Ethyl 3,4-dihydroxybenzoate protects myocardium by activating NO synthase and generating mitochondrial ROS. Ethyl 3,4-dihydroxybenzoate induces cell autophagy and apoptosis in ESCC cells. Ethyl 3,4-dihydroxybenzoate is a collagen synthesis inhibitor and has a bone protecting-effect[1][2][3][4].
分子量
182.18
Formula
C9H10O4
CAS 号
3943-89-3
中文名称
原儿茶酸乙酯
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Bo Han, et al. A prolyl-hydroxylase inhibitor, ethyl-3,4-dihydroxybenzoate, induces cell autophagy and apoptosis in esophageal squamous cell carcinoma cells via up-regulation of BNIP3 and N-myc downstream-regulated gene-1. PLoS One. 2014 Sep 18;9(9):e107204.
[2]. Sebastian Philipp, et al. Desferoxamine and ethyl-3,4-dihydroxybenzoate protect myocardium by activating NOS and generating mitochondrial ROS. Am J Physiol Heart Circ Physiol. 2006 Jan;290(1):H450-7.
[3]. Byeong-Ju Kwon, et al. Ethyl-3,4-dihydroxybenzoate with a dual function of induction of osteogenic differentiation and inhibition of osteoclast differentiation for bone tissue engineering. Tissue Eng Part A. 2014 Nov;20(21-22):2975-84.
[4]. D Nandan, et al. Ethyl-3,4-dihydroxybenzoate inhibits myoblast differentiation: evidence for an essential role of collagen. J Cell Biol. 1990 May;110(5):1673-9.
