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AM095 free acid

AM095 free acid

AM095 free acid 是一种有效的 LPA1 受体拮抗剂，对重组人和小鼠 LPA1 的 IC50 值分别为 0.98 和 0.73 μM。

货号：
TK0585
规格：

1mg

2mg

5mg

10mg

50mg
价格：
￥0.00

产品参数

CAS No.	1228690-36-5
生物活性	AM095 (free acid) is a potent LPA1 receptor antagonist with IC50 values of 0.98 and 0.73 μM for recombinant human or mouse LPA1 respectively.
分子式	C27H24N2O5
分子量	456.49
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	Powder -20°C 3 years
溶解性数据	DMSO : 67.3 mg/mL (147.43 mM; Need ultrasonic and warming)
体内研究	Pharmacological antagonism of LPA1 with AM095 significantly attenuates bleomycin-induced dermal fibrosis. 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. AM095 dose-dependently reduces LPA-stimulated histamine release. AM095 attenuates bleomycin-induced increases in collagen, protein, and inflammatory cell infiltration in bronchalveolar lavage fluid. AM095 decreases kidney fibrosis in a mouse unilateral ureteral obstruction model.
体外研究	AM095 inhibits the LPA-induced calcium flux of CHO cells stably transfected with human or mouse LPA1. The IC50 for AM095 antagonism of LPA-induced calcium flux of human or mouse LPA1-transfected CHO cells is 0.025 and 0.023 μM, respectively. AM095 reduces LPA-induced vasorelaxation by appr 90% at 10 μM as compared to vehicle control. AM095 inhibits LPA-driven chemotaxis of CHO cells overexpressing mouse LPA1 (IC50=778 nM) and human A2058 melanoma cells (IC50=233 nM).
文献	•EBioMedicine. 2020 Feb;52:102652. •Biochem Biophys Res Commun. 2015 May 29;461(2):378-82. •Biomol Ther (Seoul). 2017 Mar 1;25(2):194-201. •Biomol Ther (Seoul). 2014 Feb;22(2):129-35. •Vet Microbiol. 2021, 109177. •Research Square Preprint. 2021 Aug.
纯度及产品资料	98%

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