L-Canavanine sulfate

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L-Canavanine sulfate  纯度: ≥98.0%

L-Canavanine sulfate 是诱导型 NO 合酶 (NO synthase) 的选择性抑制剂。

L-Canavanine sulfate

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 ¥550 In-stock
50 mg ¥500 In-stock
100 mg ¥700 In-stock
200 mg   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.

储存方式

4°C, sealed storage, away from moisture

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

溶解性数据
In Vitro: 

H2O : 100 mg/mL (364.63 mM; Need ultrasonic and warming)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.6463 mL 18.2315 mL 36.4631 mL
5 mM 0.7293 mL 3.6463 mL 7.2926 mL
10 mM 0.3646 mL 1.8232 mL 3.6463 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)。-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。

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.

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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