This fluorogenic (FRET) substrate containing an anthraniloyl group and a 3-nitrotyrosine as the resonance energy transfer donor/quencher pair, was developed for the assay of 2A protease from human rhinovirus (kcat/Km = 154 M-1s-1), which has been viewed as an important enzyme target for antiviral intervention.
溶解度
分子量
1200.32
化学式
C57H77N13O16
存储条件
Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
Documents
Figures
Reference
M.G.Cordingley et al., J. Biol. Chem., 265, 9062 (1990)
L-Canavanine sulfate 是诱导型 NO 合酶 (NO synthase) 的选择性抑制剂。
L-Canavanine sulfate Chemical Structure
CAS No. : 2219-31-0
规格
价格
是否有货
数量
10 mM * 1 mL in Water
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In-stock
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询价
500 mg
询价
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生物活性
L-Canavanine sulfate is a selective inhibitor of inducible NO synthase.
IC50 & Target
NO synthase[1]
体外研究 (In Vitro)
L-Canavanine sulfate (L-CAV) causes only a limited degree of cytotoxicity in HeLa, Hep G2, and SK-HEP-1 cells when given alone in arginine-rich media with IC50 values ranging from 5 to 10 mM. In HaCaT keratinocyte cell line, IC50 of L-Canavanine sulfate exceeds the concentration of 10 mM, indicating low cytotoxicity in normal cells in vitro. In arginine-free media, IC50 of L-Canavanine sulfate in HeLa, Hep G2, and SK-HEP-1 cells are 0.21±0.04; 0.64±0.16; and 1.18±0.14 mM, respectively. L-Canavanine sulfate, which is hardly toxic alone, potentiates the cytotoxicity of vinblastine (VIN) and paclitaxel (PTX) in HeLa and hepatocellular carcinoma 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)
Administration of L-Canavanine sulfate (100 mg/kg) produces a moderate increase in mean arterial pressure of 20 mm Hg, returns blood pressure to near basal levels and completely attenuates the lipopolysaccharide-induced hypotension. All, but one, endotoxaemic rats dosed with L-Canavanine sulfate (100 mg/kg) survive for 6 h post lipopolysaccharide, after which time the experiment is terminated (n=7)[1]. L-canavanine inhibits DNA synthesis by Li 210 cells in vivo and significantly increases the lifespan of animals bearing the Li 210 leukemia. An optimal dose of 18 g/kg produces a peak increase in lifespan of 44%. The therapeutic dose range is narrow, and a dose of 24 g/kg causes death due to drug toxicity[3].
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
274.25
Formula
C5H14N4O7S
CAS 号
2219-31-0
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Teale DM, et al. L-canavanine restores blood pressure in a rat model of endotoxic shock. Eur J Pharmacol. 1994 Dec 12;271(1):87-92.
[2]. Nurcahyanti AD, et al. Cytotoxic potentiation of vinblastine and paclitaxel by L-canavanine in human cervical cancer and hepatocellular carcinoma cells. Phytomedicine. 2015 Dec 15;22(14):1232-7.
[3]. Green MH, et al. Antitumor activity of L-canavanine against L1210 murine leukemia. Cancer Res. 1980 Mar;40(3):535-7.
Cell Assay [2]
A dose-dependent cytotoxicity is examined using the MTT assay. Into each well of 96-well plates, 2×104 of cells are seeded, and after 24 h incubation, cells are incubated with test compounds (including L-Canavanine sulfate). After 24 h, 0.5 mg/mL of MTT is added to each well of HeLa, Caco-2, MIA PaCa-2, BxPC-3 and SK-HEP-1 cells, while MTT is added to Hep G2 after 48 h incubation with test compounds (including L-Canavanine sulfate). The cells are then incubated for 3 h so that the viable cells could produce formazan crystals; they are then dissolved in 100 μL DMSO. After incubation for 10 min in a shaker, the absorption of the formazan is measured at 570 nm using a reader[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.
Animal Administration [1]
Male rats weighing 295 to 305 g are used. After a period of stabilization, 6 mg lipopolysaccharide/kg is administered intravenously in 0.3 mL over 2 min, and cardiovascular parameters are monitored over 5 to 6 h. L-Canavanine sulfate is administered intravenously in a 0.2 mL volume bolus injection at 100 mg/kg[1].
Mice: L-Canavanine is dissolved in phosphate-buffered saline[1]. L-Canavanine (100 mg/mb) is infused at a rate of 0.1 mL/hr through a catheter implanted S.C. over the back. Groups of 5 mice are treated at each dose beveltogether with 6 to 8 control animals and are inspected twice per day for median time of death[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.
参考文献
[1]. Teale DM, et al. L-canavanine restores blood pressure in a rat model of endotoxic shock. Eur J Pharmacol. 1994 Dec 12;271(1):87-92.
[2]. Nurcahyanti AD, et al. Cytotoxic potentiation of vinblastine and paclitaxel by L-canavanine in human cervical cancer and hepatocellular carcinoma cells. Phytomedicine. 2015 Dec 15;22(14):1232-7.
[3]. Green MH, et al. Antitumor activity of L-canavanine against L1210 murine leukemia. Cancer Res. 1980 Mar;40(3):535-7.
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