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AM211 is a potent, selective and orally bioavailable prostaglandin D2 (PGD2) receptor type 2 (DP2) antagonist, with IC 50 s of 4.9 nM, 7.8 nM, 4.9 nM, 10.4 nM for human, mouse, guinea pig, and rat DP2, respectively. In Vitro AM211 is a potent, selective and orally bioavailable prostaglandin D2 (PGD2) receptor type 2 (DP2) antagonist, with IC 50 s of 4.9 nM, 7.8 nM, 4.9 nM, 10.4 nM for human, mouse, guinea pig, and rat DP2, respectively. In the presence of 0.2% serum albumin, AM211 inhibits radiolabeled PGD2 binding to human, mouse, guinea pig, and rat DP2 with IC 50 values of 12.2, 20.1, 22.9, and 34.2 nM, respectively. AM211 displays high selectivity for DP2 versus other receptors in the prostanoid family, with IC 50 values for the inhibition of radioligand binding to human TP, IP, DP1, and FP of more than 100 μM. AM211 (100 μM) shows no activity at COX-1, COX-2 enzymes as well as PPAR family of nuclear receptors. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo AM211 (1, 10, and 30 mg/kg, p.o.) dose-dependently decreases in the number of DK-PGD2-induced peripheral blood leukocytes, with a calculated ED 50 of 0.85 mg/kg. AM211 (30 mg/kg) also decreases antigen-induced pulmonary inflammation in guinea pigs. AM211 (10 mg/kg, p.o.) causes significant decrease in ovalbumin (OVA)-induced sneezing in a mouse model of allergic rhinitis . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:IC50: 4.9 nM (Human DP2), 7.8 nM (Mouse DP2), 4.9 nM (Guinea pig DP2), 10.4 nM (Rat DP2)
中文名称
AM211, G 蛋白偶联受体 44 拮抗剂
英文名称
AM211
中文别名
-
英文别名
1175526-27-8 | 2-(2'-((3-benzyl-1-ethylureido)methyl)-6-methoxy-4'-(trifluoromethyl)-[1,1'-biphenyl]-3-yl)acetic acid | 1175526-27-8 (free acid) | AM211 free acid | SZB129M7SZ | AM211 | AM-211 | CHEMBL2181753
CAS号
1175526-27-8
分子式
C27H27F3N2O4
分子量
500.51 g/mol
精确质量
≥96%
PSA
78.900 Ų
Logp
4.9
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MedMol AM-211 98% 2mg

品牌:MedMol
货号:S88283-2mg
级别: -
货期:30天
已售 192 件
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