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AZD2098

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Chemical Structure| 566203-88-1 同义名 : -
CAS号 : 566203-88-1
货号 : A924249
分子式 : C11H9Cl2N3O3S
纯度 : 99%+
分子量 : 334.178
MDL号 : MFCD31382158
存储条件:

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(314.2 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

无水乙醇: 5 mg/mL(14.96 mM),配合低频超声,并水浴加热至45℃助溶,注意:无水乙醇开封后,易挥发,也会吸收空气中的水分,导致溶解能力下降,请避免使用开封较久的乙醇

动物实验配方:
生物活性
描述 AZD-2098 is a selective CCR4 receptor antagonist with pIC50 value of 7.8. It is a candidate drug for asthma indications. AZD-2098 inhibited the cellular responses mediated by the hCCR4 receptor with pIC50 values of 7.5, 6.3 and 6.3 for inhibition of CCL22 Ca2+ response (measured by MDC-induced Ca2+ flux in CHO cells transfected with the human CCR4 receptor), inhibition of Th2 cell CCL22 driven chemotaxis in 0.3% HAS (measured by MDC-induced chemotaxis) and inhibition of Th2 cell CCL17 driven chemotaxis in 0.3% HAS (measured by TARC-induced chemotaxis). Oral administration of AZD-2098 at dose>0.75µmol/kg 1 hour prior to antigen challenge (then every 12 hours thereafter prior to termination 96 hours post challenge) reduced alveolitis and leukocyte trafficking in the microvasculature of sensitized rats.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.99mL

0.60mL

0.30mL

14.96mL

2.99mL

1.50mL

29.92mL

5.98mL

2.99mL

参考文献

[1]Kindon N, Andrews G, et al. Discovery of AZD-2098 and AZD-1678, Two Potent and Bioavailable CCR4 Receptor Antagonists. ACS Med Chem Lett. 2017 Sep 1;8(9):981-986.