AS2717638

Chemical Structure : AS2717638

CAS No.: 2148339-28-8

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货号: PC-23606Not For Human Use, Lab Use Only.

AS2717638 a potent, selective lysophosphatidic acid receptor 5 (LPA5, LPAR5) antagonist, inhibits LPA-induced cAMP accumulation in CHO cells expressing human LPA5 with IC50 of 38 nM.

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5 mg	￥2580	In stock
10 mg	￥3980	In stock
25 mg	￥5980	In stock
50 mg		Get quote
100 mg		Get quote

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生物&药学活性

AS2717638 a potent, selective lysophosphatidic acid receptor 5 (LPA5, LPAR5) antagonist, inhibits LPA-induced cAMP accumulation in CHO cells expressing human LPA5 with IC50 of 38 nM.
AS2717638 shows no activity against LPA-induced Ca2+ mobilization in cells expressing human LPA1, LPA2, and LPA3.
AS2717638 shows binding Ki of for 9.1, 16 and 7.3 nM for human, rat, and mouse LPA5 receptor respectively.
Oral administration of AS2717638 inhibited LPA5 agonist-induced allodynia in mice.
AS2717638 also significantly improved PGE2-, PGF2α-, and AMPA-induced allodynia, AS2717638 significantly ameliorated static mechanical allodynia and thermal hyperalgesia in rat models of chronic constriction injury (CCI)-induced neuropathic pain.
AS2717638 also showed analgesic effects in a rat model of inflammatory pain.

物理化学性质&存储条件

分子量	447.49
分子式	C25H25N3O5
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	6,7-dimethoxy-2-(5-methyl-1,2-benzoxazol-3-yl)-4-(piperidin-1-ylcarbonyl)isoquinolin-1(2H)-one

参考文献

1. Murai N, et al. Neuropharmacology. 2017 Nov;126:97-107.

AS2717638

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AS2717638

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