Disitertide TFA(Synonyms: P144 TFA)

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Disitertide TFA (Synonyms: P144 TFA) 纯度: 95.87%

Disitertide (P144) TFA 是转化生长因子 TGFβ1 的多肽抑制剂,特异性的阻断其与受体间的相互作用。Disitertide (P144) TFA 也是PI3K 的抑制剂和凋亡 (apoptosis) 诱导剂。

Disitertide TFA(Synonyms: P144 TFA)

Disitertide TFA Chemical Structure

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10 mg ¥5600 In-stock
25 mg ¥11500 In-stock
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Disitertide TFA 相关产品

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生物活性

Disitertide (P144) TFA is a peptidic transforming growth factor-beta 1 (TGF-β1) inhibitor specifically designed to block the interaction with its receptor. Disitertide (P144) TFA is also a PI3K inhibitor and an apoptosis inducer[1][2][3][4][5].

IC50 & Target

TGF-β1, P13K[1][2].

体外研究
(In Vitro)

Disitertide (100 μg/mL) suppresses the protein expression levels of PI3K and p-Akt, and induce the protein expression of Bax in MC3T3-E1 cells[2].
Disitertide (TGF-β1 inhibitor) abrogates the MACC1- AS1 expression in GC cells, suggesting that targeting TGFβ signaling pathway may be a potential strategy to inhibit MSC-induced stemness and chemoresistance[3].
Disitertide (P144, 10 μg/mL to 200 μg/mL) affects proliferation, induces apoptosis as well as anoikis in A172 and U-87 MG GBM cell lines[5].

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.

Western Blot Analysis[2]

Cell Line: Mouse embryo osteoblast precursor MC3T3-E1 cells.
Concentration: 100 μg/mL.
Incubation Time: 4 h.
Result: Significantly suppressed the protein expression levels of PI3K and p-Akt, and induce the protein expression of Bax in MC3T3-E1 cells compared with the miR-590 group.

体内研究
(In Vivo)

Disitertide (Topical application, 300 μg/mL) may promote scar maturation and clinical improvement of hypertrophic scar morphology features in an “in vivo” model in nude mice after two weeks of treatment[4].

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: Human hypertrophic scars were implanted in 60 nude mice[4].
Dosage: 300 μg/mL was added the Lipogel.
Administration: Topical application daily administered.
Result: Successful shedding was achieved in 83,3% of the xenografts.

Clinical Trial

分子量

1694.84

Formula

C70H110N17O24S2F3

Sequence Shortening

TSLDASIIWAMMQN

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Sealed storage, away from moisture and light

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶解性数据
In Vitro: 

DMSO : 50 mg/mL (29.50 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.5900 mL 2.9501 mL 5.9003 mL
5 mM 0.1180 mL 0.5900 mL 1.1801 mL
10 mM 0.0590 mL 0.2950 mL 0.5900 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 2.5 mg/mL (1.48 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (1.48 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (1.48 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (1.48 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (1.48 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (1.48 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Cindy Neuzillet, et al. Targeting the TGFβ pathway for cancer therapy. Pharmacol Ther. 2015 Mar;147:22-31.

    [2]. Jun Yang, et al. Upregulation of microRNA‑590 in rheumatoid arthritis promotes apoptosis of bone cells through transforming growth factor‑β1/phosphoinositide 3‑kinase/Akt signaling. Int J Mol Med. 2019 May;43(5):2212-2220.

    [3]. Wanming He, et al. MSC-regulated lncRNA MACC1-AS1 promotes stemness and chemoresistance through fatty acid oxidation in gastric cancer. Oncogene. 2019 Jun;38(23):4637-4654.

    [4]. Shan Shan Qiu, et al. Effect of P144® (Anti-TGF-β) in an “In Vivo” Human Hypertrophic Scar Model in Nude Mice. PLoS One. 2015 Dec 31;10(12):e0144489.

    [5]. Gabriel Gallo-Oller, et al. P144, a Transforming Growth Factor beta inhibitor peptide, generates antitumoral effects and modifies SMAD7 and SKI levels in human glioblastoma cell lines. Cancer Lett. 2016 Oct 10;381(1):67-75.

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