CAS:264622-53-9MRS 1706

MRS 1706 is a potent and selective adenosine A2B receptor inverse agonist with Ki of 1.39 nM.

规格	价格	促销价格	库存

18817579266

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18817579266

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实验数据

技术信息

CAS号

264622-53-9

储存条件

分子式

C27H29N5O5

运输

蓝冰

分子量

503.55

别名

溶解度

DMSO	6.4 mg/mL (12.7 mM)
Water	Insoluble

动物实验配方

生物活性

描述The adenosine receptor, one of the GPCR (G protein-coupled receptors) family members, is composed of four receptor subtypes: A₁, A_2A, A_2B, and A₃. The adenosine A_2B receptor has been implied in many physiological functions, and its antagonists may be used in the treatment of asthma, type-II diabetes, Alzheimer's disease, and cystic fibrosis. MRS 1706 acts as inverse agonist on the constitutively active human adenosine A_2B mutants with IC₅₀s of 98 ± 62, 43 ± 21, 54 ± 12 and 40 ± 32 nM for T42A, F84L, F84S, and F84L/S95G mutant, respectively. The agonistic effect of NECA on the wild-type adenosine A_2B receptor was antagonized by MRS 1706 in a concentration-dependent manner. The basal growth of yeast cells expressing T42A, F84L, F84S, or F84L/S95G mutant receptors was dose dependently reduced by MRS 1706 from 91 to 99%^[1].