AM095 (free acid) is a potentLPA1receptor antagonist withIC₅₀values of 0.98 and 0.73 μM for recombinant human or mouse LPA1 respectively.

IC50: 0.98 μM (human LPA1), 0.73 μM (mouse LPA1)

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^[1]. AM095 reduces LPA-induced vasorelaxation by appr 90% at 10 μM as compared to vehicle control^[2]. AM095 inhibits LPA-driven chemotaxis of CHO cells overexpressing mouse LPA1 (IC₅₀=778 nM) and human A2058 melanoma cells (IC₅₀=233 nM)^[3].

Pharmacological antagonism of LPA1 with AM095 significantly attenuates bleomycin-induced dermal fibrosis^[1]. 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^[3].

456.49

Solid

C₂₇H₂₄N₂O₅

1228690-36-5

Room temperature in continental US; may vary elsewhere.

DMSO : 67.3 mg/mL(147.43 mM;Need ultrasonic and warming)

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    90%corn oil

  Solubility: ≥ 2.25 mg/mL (4.93 mM); Clear solution

  此方案可获得 ≥ 2.25 mg/mL (4.93 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 22.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。