4'-[3-甲基-4-[[[(1R)-1-苯基乙氧基]羰基]氨基]-5-异恶唑基]联苯-4-乙酸钠盐
4'-[3-甲基-4-[[[(1R)-1-苯基乙氧基]羰基]氨基]-5-异恶唑基]联苯-4-乙酸钠盐(AM-095)
CAS: 1345614-59-6
化学式: C27H25N2NaO5
| 中文名 | 4'-[3-甲基-4-[[[(1R)-1-苯基乙氧基]羰基]氨基]-5-异恶唑基]联苯-4-乙酸钠盐 |
| 英文名 | AM-095 |
| 别名 | 化合物AM095 4'-[3-甲基-4-[[[(1R)-1-苯基乙氧基]羰基]氨基]-5-异恶唑基]联苯-4-乙酸钠盐 |
| 英文别名 | AM095 AM-095 AM 095 AM095 sodium AM095 (Sodium Salt) AM095 hydrochloride sodium,2-[4-[4-[3-methyl-4-[[(1R)-1-phenylethoxy]carbonylamino]-1,2-oxazol-5-yl]phenyl]phenyl]acetate (2-[4-[4-[3-methyl-4-[[(1R)-1-phenylethoxy]carbonylamino]-1,2-oxazol-5-yl]phenyl]phenyl]acetic acid) sodium salt |
| CAS | 1345614-59-6 |
| 化学式 | C27H25N2NaO5 |
| 分子量 | 480.5 |
| 存储条件 | room temp |
| 外观 | 粉末 |
| 颜色 | white to beige |
| 体外研究 | AM095 is a potent LPA 1 receptor antagonist because it inhibits GTPγS binding to Chinese hamster ovary (CHO) cell membranes overexpressing recombinant human or mouse LPA 1 with IC 50 values of 0.98 and 0.73 μM, respectively. AM095 inhibits LPA-driven chemotaxis of CHO cells overexpressing mouse LPA 1 (IC 50 =778 nM) and human A2058 melanoma cells (IC 50 =233 nM). The IC 50 of AM095 in the human LPA 1 GTPγS binding assay is comparable with that of our previously published compound AM966 (IC 50 =0.98±0.17 μM) and the Debio-0719 compound (IC 50 =0.60±0.04 μM). AM095 inhibits the LPA-induced calcium flux of CHO cells stably transfected with human or mouse LPA 1 . The IC 50 for AM095 antagonism of LPA-induced calcium flux of human or mouse LPA 1 -transfected CHO cells is 0.025 and 0.023 μM, respectively. |
| 体内研究 | 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 C max of 41 μM, thereafter decreasing to 10 nM by 24 h. After intravenous (2 mg/kg) dosing, a C max of 12 μM is observed within 15 min, which also decreased to approximately 10 nM by 24 h, yielding a t 1/2 of 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 C max of 11 μM within 15 min and decreased to 15 nM by 8 h, yielding a t 1/2 of 1.5 h. |
![4'-[3-甲基-4-[[[(1R)-1-苯基乙氧基]羰基]氨基]-5-异恶唑基]联苯-4-乙酸钠盐](http://res.chembk.com/assets/str/2d/1/13/1345614-59-6.png)
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