CAS NO: | 138470-70-9 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | Mozavaptan hydrochloride (OPC-31260 hydrochloride) is a benzazepine derivative and a potent, selective, competitive and orally activevasopressin V2receptorantagonist with anIC50of 14 nM. Mozavaptan hydrochloride shows ~85-fold selectivity forV2receptorover V1receptor (IC50of 1.2 μM), and can antagonize the antidiuretic action of arginine vasopressin (AVP) in vivo. Mozavaptan hydrochloride has the potential for hyponatremia, syndrome of inappropriate antidiuretic hormone (SIADH), and congestive heart failure treatment[1][2]. | ||||||||||||||||
IC50& Target | IC50: 14 nM (Vasopressin V2receptor); 1.2 μM (Vasopressin V1receptor)[1] | ||||||||||||||||
体外研究 (In Vitro) | Mozavaptan (OPC-31260) inhibits AVP binding to binding to rat liver (V1 receptor) and kidney (V2 receptor) plasma membranes in a competitive manner and that it is about 100 times more selective for V2 receptors. Kdvalue for [3H]-AVP in rat liver is 1.1 nM; in rat kidney is 1.38 nM. The Kdof [3H]-AVP is reduced significantly in both rat liver and kidney in the presence of Mozavaptan (Kdof 2.47 nM and 5.51 nM for V1 receptor at the doses of 0.3 μM and 1 μM.respectively; Kdof 2.4 nM and 4.03 nM for V2 receptor at the doses of 0.3 μM and 1 μM.respectively)[1]. | ||||||||||||||||
体内研究 (In Vivo) | Mozavaptan (OPC-31260; 1-30 mg/kg; oral administration; hydrated conscious rats) treatment dose-dependently increases urine flow and decreased urine osmolality[1].
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分子量 | 464.00 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C27H30ClN3O2 | ||||||||||||||||
CAS 号 | 138470-70-9 | ||||||||||||||||
中文名称 | 盐酸莫扎伐普坦 | ||||||||||||||||
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: DMSO : 20.83 mg/mL(44.89 mM;Need ultrasonic) H2O : 10 mg/mL(21.55 mM;Need ultrasonic) 配制储备液
* 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。 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
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