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AZD1981

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Chemical Structure| 802904-66-1 同义名 : -
CAS号 : 802904-66-1
货号 : A495831
分子式 : C19H17ClN2O3S
纯度 : 98+%
分子量 : 388.868
MDL号 : MFCD26936340
存储条件：

粉末 Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(270.01 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • GPR

    CRTh2 (DP2) receptor, IC50:4 nM
描述 AZD1981 is a powerful and selective antagonist of CRTh2, effectively competing with radio-labelled PGD2 for binding to the human DP2 receptor, exhibiting a high level of potency (pIC50 = 8.4)[1]. Further, in a guinea pig hind limb model, AZD1981 at 10 nM markedly reduced DK-PGD2-driven eosinophil mobilization by about 50%, a suppression that was complete at 100 nM[1]. AZD1981 demonstrated efficient cross-species DP2 receptor binding activity in mice, rats, guinea pigs, rabbits, and dogs. However, mouse, rat, and rabbit cell systems did not exhibit a response to DP2 agonists, whereas guinea pig and dog systems did, with AZD1981 inhibiting DP2-mediated changes in eosinophil shape and migration from bone marrow, particularly noted in guinea pigs[1]. No positive clinical outcomes were observed with the use of AZD1981 at a dosage of 1000 mg twice daily over a four-week period in individuals with moderate to severe COPD, although the drug was generally well-received without raising safety issues[3].
作用机制 AZD1981 could block PGD2 binding to human DP2.[2]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.57mL

0.51mL

0.26mL

12.86mL

2.57mL

1.29mL

25.72mL

5.14mL

2.57mL
参考文献

[1]Royer JF, et al. A novel antagonist of prostaglandin D2 blocks the locomotion of eosinophils and basophils. Eur J Clin Invest. 2008 Sep;38(9):663-71.

[2]Snell N, et al. Efficacy and safety of AZD1981, a CRTH2 receptor antagonist, in patients with moderate to severe COPD. Respir Med. 2013 Nov;107(11):1722-30.