Cas No.: | 1196045-28-9 |
Chemical Name: | (1r,4r)-4-((1-(quinolin-2-ylmethyl)-5-(trifluoromethyl)-1H-indole-7-carboxamido)methyl)cyclohexane-1-carboxylic acid |
Synonyms: | ASP 7657;ASP-7657 |
SMILES: | [C@@H](C(O)=O)1CC[C@H](CNC(C2C3=C(C=C(C(F)(F)F)C=2)C=CN3CC2C=CC3C(N=2)=CC=CC=3)=O)CC1 |
Formula: | C28H26F3N3O3 |
M.Wt: | 509.529 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | ASP7657 (ASP-7657) is a potent, selective, orally active prostaglandin EP4 receptor antagonist with Ki values of 6.02 nM and 2.21 nM for rat and human EP4 receptors, resepctively; potently inhibits the PGE2-induced cAMP increase in CHO cells expressing rat EP4 receptors and human lymphoblastoid T (Jurkat) cells, with IC50 values of 0.86 nM and 0.29 nM, respectively; does not inhibit the PGE2-induced intracellular calcium increase in HEK293 cells expressing rat EP1 and EP3 receptors, or cAMP increase in CHO cells expressing rat EP2 receptors; dose-dependently inhibits the PGE2-mediated inhibition of LPS-induced TNF-α release from rat whole blood culture, attenuates albuminuria in type 2 diabetic mice at dose of 0.1 mg/kg. |