产品
编 号：F055822
分子式：C27H27F3N2O4
分子量：500.51
分子式：C27H27F3N2O4
分子量：500.51
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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1mg
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5mg
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10mg
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25mg
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50mg
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结构图
CAS No: 1175526-27-8
产品详情
生物活性：
AM211 is a potent, selective and orally bioavailable prostaglandin D2 (PGD2) receptor type 2 (DP2) antagonist, with IC50s of 4.9 nM, 7.8 nM, 4.9 nM, 10.4 nM for human, mouse, guinea pig, and rat DP2, respectively.
体内研究：
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 ED50 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.
体外研究：
AM211 is a potent, selective and orally bioavailable prostaglandin D2 (PGD2) receptor type 2 (DP2) antagonist, with IC50s 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 IC50 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 IC50 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.
AM211 is a potent, selective and orally bioavailable prostaglandin D2 (PGD2) receptor type 2 (DP2) antagonist, with IC50s of 4.9 nM, 7.8 nM, 4.9 nM, 10.4 nM for human, mouse, guinea pig, and rat DP2, respectively.
体内研究：
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 ED50 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.
体外研究：
AM211 is a potent, selective and orally bioavailable prostaglandin D2 (PGD2) receptor type 2 (DP2) antagonist, with IC50s 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 IC50 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 IC50 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.
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