CAS NO: | 802904-66-1 |
包装 | 价格(元) |
10mM (in 1mL DMSO) | 电议 |
5mg | 电议 |
25mg | 电议 |
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 388.87 |
Cas No. | 802904-66-1 |
Formula | C19H17ClN2O3S |
Solubility | insoluble in H2O; insoluble in EtOH; ≥19.8 mg/mL in DMSO |
Chemical Name | 2-[4-acetamido-3-(4-chlorophenyl)sulfanyl-2-methylindol-1-yl]acetic acid |
Canonical SMILES | CC1=C(C2=C(N1CC(=O)O)C=CC=C2NC(=O)C)SC3=CC=C(C=C3)Cl |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
AZD1981是一种选择性的\口服生物可用的和有效的表达于Th2淋巴细胞上的同源趋化因子受体(CRTh2或DP2)拮抗剂,IC50值为4 nM[1].
AZD1981可抑制嗜酸性粒细胞迁移,pIC50值为7.6±0.1.AZD1981可阻断DP2+ T细胞系的趋化性,pIC50值为7.5±0.1.AZD1981可抑制PGD2结合小鼠\大鼠\兔\犬\豚鼠和人的DP2.AZD1981可抑制DP2诱导的犬和豚鼠粒细胞及人类血液中嗜酸性粒细胞和嗜碱性粒细胞的形变[2].
参考文献:
[1] Luker T1, Bonnert R, Brough S, Cook AR, Dickinson MR, Dougall I, Logan C, Mohammed RT, Paine S, Sanganee HJ, Sargent C, Schmidt JA,Teague S, Thom S. Substituted indole-1-acetic acids as potent and selective CRTh2 antagonists-discovery of AZD1981. Bioorg Med Chem Lett. 2011 Nov 1;21(21):6288-92.
[2] Schmidt JA1, Bell FM, Akam E, Marshall C, Dainty IA, Heinemann A, Dougall IG, Bonnert RV, Sargent CA. Biochemical and pharmacological characterization of AZD1981, an orally available selective DP2 antagonist in clinical development for asthma. Br J Pharmacol. 2013 Apr;168(7):1626-38.