|[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|CsnPharm

CAS No.: 1228690-36-5

AM095 free acid Catalog No. CSN17359

Synonyms: AM095

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.

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生物活性

实验方案

技术信息

生物活性

描述LPA1 (LPA type 1 receptor), belonging to a family of at least six G protein-coupled receptors designated LPA1–6 as bioactive phospholipid, distributes widely on tissue and regulates a variety of physiological and pathological cellular functions. AM095 is a selective and potent LPA1 antagonist with IC50 values of 0.98 and 0.73μM for inhibition of GTP binding to Chinese hamster ovary (CHO) cell membranes overexpressing recombinant human or mouse LPA1, respectively. AM095 inhibited LPA-driven chemotaxis of CHO cells overexpressing mouse LPA1 and human A2058 melanoma cells with IC50 values of 778nM and 233nM, respectively. AM095 exhibited high oral bioavailability and was well tolerated in rats and dogs. Oral administration of AM095 at dose of 10mg/kg and 30mg/kg, BID, dose-dependently reduced LPA-stimulated histamine release in vivo. Attenuation of bleomycin-induced increases in collagen, protein, and inflammatory cell infiltration in bronchalveolar lavage fluid could be observed in mice post treatment with 30mg/kg and 60mg/kg AM095. Decreased kidney fibrosis was found in mouse unilateral ureteral obstruction model dosed of 30 mg/kg AM095 twice a day for 8 days. AM095 exhibited efficiency on preventing the pathogenesis of diabetic nephropathy by inhibiting TLR4/NF-κB and the NADPH oxidase system, consequently inhibiting the inflammatory signaling cascade in renal tissue of diabetic mice.
动物研究
剂量
Rat: 2 mg/kg^[1] (i.v.); 10 mg/kg^[1] (p.o.) Mice: 10 mg/kg, 30 mg/kg^[2] (p.o.)

给药途径
i.v., p.o.
参考文献

动物研究
剂量	Rat: 2 mg/kg^[1] (i.v.); 10 mg/kg^[1] (p.o.) Mice: 10 mg/kg, 30 mg/kg^[2] (p.o.)
给药途径	i.v., p.o.

[1] Swaney JS, Chapman C, et al. Pharmacokinetic and pharmacodynamic characterization of an oral lysophosphatidic acid type 1 receptor-selective antagonist. J Pharmacol Exp Ther. 2011 Mar;336(3):693-700.
[2] Lee JH, Sarker MK, et al. Lysophosphatidic acid receptor 1 inhibitor, AM095, attenuates diabetic nephropathy in mice by downregulation of TLR4/NF-κB signaling and NADPH oxidase. Biochim Biophys Acta Mol Basis Dis. 2019 Jun 1;1865(6):1332-1340.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 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

技术信息

CAS号

1228690-36-5

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C27H24N2O5

运输

蓝冰

分子量

456.49

别名

AM095

溶解度

DMSO	91.0 mg/mL (199.3 mM)
Water	Insoluble
Ethanol	3.0 mg/mL (6.6 mM)

动物实验配方

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