Ki16198是Ki16425的甲酯,是LPA拮抗剂,抑制LPA1-和LPA3诱导的肌醇磷酸产生,Ki分别为0.34 μM和0.93 μM,对LPA2具有较弱的抑制作用,对LPA4, LPA5, LPA6没有抑制活性。
Ki16198 is the methyl ester of Ki16425, which is a LPA antagonist and inhibits LPA1- and LPA3-induced inositol phosphate production with Ki of 0.34 μM and 0.93 μM, respectively, shows weaker inhibition for LPA2, no activity at LPA4, LPA5, LPA6.
10 μM
2 mg/kg 口服处理
动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数 | |
例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。
[1] Komachi M, et al. Cancer Sci, 2012, 103(6), 1099-1104.
[2] Yukiko Tando,et al. The Role of Lysophosphatidic Acid on Airway Epithelial Cell Denudation in a Murine Heterotopic Tracheal Transplant Model. Transplant Direct. 2015 Oct; 1(9): e35. Published online 2015 Oct 19. doi: 10.1097/TXD.0000000000000542.
[3] Nicole C. et al. Promising Pharmacological Directions in the World of Lysophosphatidic Acid Signaling. Biomol Ther (Seoul) 2015 Jan; 23(1): 1–11. Published online 2015 Jan 1. doi: 10.4062/biomolther.2014.109.
分子式 C24H25ClN2O5S |
分子量 488.98 |
CAS号 355025-13-7 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 100 mg/mL |
Water <1 mg/mL |
Ethanol 40 mg/mL |
体内溶解度
注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。
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