AM-095 free base|1228690-36-5|-陌孚医药/Medlife

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AM-095 free base

目录号: PC10587 纯度: ≥98%

CAS No. :1228690-36-5

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中文名称

AM-095 free base

中文别名

[4'-[3-甲基-4-[[[((R)-1-苯基乙基)氧基]羰基]氨基]异恶唑-5-基]联苯-4-基]乙酸;AM-095 抑制剂

英文名称

AM-095 free base

英文别名

2-[4-[4-[3-methyl-4-[[(1R)-1-phenylethoxy]carbonylamino]-1,2-oxazol-5-yl]phenyl]phenyl]acetic acid;[1,1'-Biphenyl]-4acetic acid,4'-[3-methyl-4-[[[(1R)-1-phenylethoxy]carbonyl]amino]-5-isoxazolyl]-;SureCN2288084;{4'-[3-Methyl-4-((R)-1-phenyl-ethoxycarbonylamino)-isoxazol-5-yl]-biphenyl-4-yl}-acetic acid;CHEMBL2182052;HY-16040;(4'-(3-methyl-4-((R)-1-phenyl-ethoxycarbonylamino)-isoxazol-5-yl)-biphenyl-4-yl)-acetic acid;AM-095 free base;AM095;KB-63701;(R)-2-(4'-(3-methyl-4-((1-phenylethoxy)carbonylamino)isoxazol-5-yl)biphenyl-4-yl)acetic acid;CS-1129;AM095 free acid;(R)-2-(4'-(3-methyl-4-((1-phenylethoxy)carbonylamino);AM-095 free acid;AM095 (free acid)

Cas No.

1228690-36-5

分子式

C₂₇H₂₄N₂O₅

分子量

456.49

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

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.

性状

Solid

IC50 & Target[1][2]

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

体外研究(In Vitro)

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).

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

参考文献

[1]. Castelino FV, et al. Amelioration of dermal fibrosis by genetic deletion or pharmacologic antagonism of lysophosphatidic acid receptor 1 in a mouse model of scleroderma. Arthritis Rheum. 2011 May;63(5):1405-15 [Information]

[2]. Ruisanchez E, et al. Lysophosphatidic acid induces vasodilation mediated by LPA1 receptors, phospholipase C, and endothelial nitric oxide synthase. FASEB J. 2014 Feb;28(2):880-90 [Information]

[3]. Swaney, J. S., et al. Pharmacokinetic and pharmacodynamic characterization of an oral lysophosphatidic acid type 1 receptor-selective antagonist. Journal of Pharmacology and Experimental Therapeutics (2011), 336(3), 693-700. [Information]

溶解度数据

体外研究:

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

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1906 mL	10.9531 mL	21.9063 mL
5 mM	0.4381 mL	2.1906 mL	4.3813 mL
10 mM	0.2191 mL	1.0953 mL	2.1906 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

建议依照次序添加每种溶剂： 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。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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