Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Lixivaptan (VPA-985) 是一种具有口服活性的选择性加压素受体 V2 拮抗剂,对人和大鼠的IC50值分别为 1.2 和 2.3 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 269 | 现货 | ||
2 mg | ¥ 379 | 现货 | ||
5 mg | ¥ 598 | 现货 | ||
10 mg | ¥ 995 | 现货 | ||
25 mg | ¥ 2,290 | 现货 | ||
50 mg | ¥ 3,990 | 现货 | ||
100 mg | ¥ 5,680 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 666 | 现货 |
产品描述 | Lixivaptan (VPA-985) is an orally active and selective vasopressin receptor V2 antagonist(Ki = 2.3 nM) |
靶点活性 | rat V2:2.3 nM (IC50), human V2:1.2 nM (IC50) |
体内活性 | Consistent with the development of a polycystic kidney phenotype, control PCK rats showed enlarged kidneys, extensive cyst formation, and early signs of serum creatinine elevation at 12 weeks of age.?Compared to controls, PCK rats treated with low-dose lixivaptan showed a 26% reduction in % kidney weight/body weight (p < 0.01);?a 54% reduction in kidney cystic score (p < 0.001), a histomorphometric measure of cystic burden;?a 23% reduction in kidney cAMP levels (p < 0.05), a biochemical marker of disease;?and a 13% reduction in plasma creatinine (p < 0.001), indicating preserved renal function.?These reductions were associated with 3-fold increases in 24-h urine output, demonstrating the potent aquaretic effect of lixivaptan[1]. |
动物实验 | Four-week old PCK rats were fed rodent chow with 0.5% lixivaptan (low dose) or 1% lixivaptan (high dose), or chow only (control) for 8 weeks.?Urine output was measured at weeks 7 and 10 of age.?Animals were killed at 12 weeks of age;?kidneys and livers were collected, weighted, and analyzed for cyclic adenosine 3',5'-monophosphate (cAMP) levels and cystic burden and fibrosis;?serum creatinine and sodium were measured[1]. |
别名 | VPA-985, 利伐普坦, WAY-VPA 985 |
分子量 | 473.93 |
分子式 | C27H21ClFN3O2 |
CAS No. | 168079-32-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 150 mg/mL (316.50 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.11 mL | 10.5501 mL | 21.1002 mL | 52.7504 mL |
5 mM | 0.422 mL | 2.11 mL | 4.22 mL | 10.5501 mL | |
10 mM | 0.211 mL | 1.055 mL | 2.11 mL | 5.275 mL | |
20 mM | 0.1055 mL | 0.5275 mL | 1.055 mL | 2.6375 mL | |
50 mM | 0.0422 mL | 0.211 mL | 0.422 mL | 1.055 mL | |
100 mM | 0.0211 mL | 0.1055 mL | 0.211 mL | 0.5275 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
LIXIVAPTAN 168079-32-1 GPCR/G Protein Vasopressin Receptor VPA-985 inhibit 利伐普坦 Inhibitor VPA 985 VPA985 WAY-VPA 985 WAY-VPA-985 WAY-VPA985 inhibitor