CAS NO: | 1345614-59-6 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
1 g | 电议 |
生物活性 | AM095 is a selectiveLPA1receptor antagonist. TheIC50for AM095 antagonism of LPA-induced calcium flux of human or mouse LPA1-transfected CHO cells is 0.025 and 0.023 μM, respectively. | ||||||||||||||||
IC50& Target | LPA1receptor[1] | ||||||||||||||||
体外研究 (In Vitro) | AM095 is a potent LPA1receptor antagonist because it inhibits GTPγS binding to Chinese hamster ovary (CHO) cell membranes overexpressing recombinant human or mouse LPA1with IC50values of 0.98 and 0.73 μM, respectively. AM095 inhibits LPA-driven chemotaxis of CHO cells overexpressing mouse LPA1(IC50=778 nM) and human A2058 melanoma cells (IC50=233 nM). The IC50of AM095 in the human LPA1GTPγS binding assay is comparable with that of our previously published compound AM966 (IC50=0.98±0.17 μM) and the Debio-0719 compound (IC50=0.60±0.04 μM)[1]. AM095 inhibits the LPA-induced calcium flux of CHO cells stably transfected with human or mouse LPA1. The IC50for AM095 antagonism of LPA-induced calcium flux of human or mouse LPA1-transfected CHO cells is 0.025 and 0.023 μM, respectively[2]. | ||||||||||||||||
体内研究 (In Vivo) | AM095 has high oral bioavailability and a moderate half-life and is well tolerated at the doses tested in rats and dogs after oral and intravenous dosing. After oral (10 mg/kg) dosing in rats, AM095 plasma concentrations peaked at 2 h with a Cmaxof 41 μM, thereafter decreasing to 10 nM by 24 h. After intravenous (2 mg/kg) dosing, a Cmaxof 12 μM is observed within 15 min, which also decreased to approximately 10 nM by 24 h, yielding a t1/2of 1.79 h. In dogs, a single oral dose of 5 mg/kg yielded a peak plasma concentration of 21 μM within 15 min of dosing, which then decreased to 10 nM by 24 h. In contrast, an intravenous dose of 2 mg/kg resulted in a Cmaxof 11 μM within 15 min and decreased to 15 nM by 8 h, yielding a t1/2of 1.5 h[1]. | ||||||||||||||||
分子量 | 478.47 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C27H23N2NaO5 | ||||||||||||||||
CAS 号 | 1345614-59-6 | ||||||||||||||||
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 : 83.33 mg/mL(174.16 mM;Need ultrasonic) 配制储备液
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