AM211,1175526-27-8

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

AM211

CAS No. : 1175526-27-8

MCE 国际站：AM211

产品活性：AM211 是一种有效的，选择性的，可口服的前列腺素受体 (DP2) 拮抗剂，对人，小鼠，豚鼠和大鼠的 DP2 的 IC₅₀ 值分别为 4.9 nM，7.8 nM，4.9 nM，10.4 nM。

研究领域：GPCR/G Protein

作用靶点：Prostaglandin Receptor

In Vitro: 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.

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 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.

相关产品：Bioactive Compound Library Plus  |  GPCR/G Protein Compound Library  |  Immunology/Inflammation Compound Library  |  Endocrinology Compound Library  |  Orally Active Compound Library  |  Angiogenesis-Related Compound Library  |  Membrane Protein-targeted Compound Library  |  Membrane Receptor-targeted Compound Library  |  Highly Selective Inhibitors Library  |  Prostaglandin E2  |  EIPA  |  Prostaglandin E1  |  Tranilast  |  PF-04418948  |  U-46619  |  Iloprost  |  Prostaglandin D2  |  ONO-AE3-208  |  Dinoprost  |  Palupiprant  |  Latanoprost  |  Selexipag  |  16,16-Dimethyl prostaglandin E2  |  Treprostinil  |  DG-041  |  Grapiprant  |  L-798106  |  GW627368  |  Fevipiprant  |  Asapiprant  |  AH 6809  |  L-161982  |  Laropiprant  |  Bimatoprost  |  CJ-42794  |  MF498  |  Beraprost sodium  |  Ramatroban

热门产品线：重组蛋白  |  化合物库  |  天然产物  |  荧光染料  |  PROTAC  |  同位素标记物

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Dye Reagents  |  PROTAC  |  Isotope-Labeled Compounds