Mirabegron

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Mirabegron 是一种选择性 β3-肾上腺素受体激动剂，EC50 为 22.4 nM。

Mirabegron is a selective β3-adrenoceptor agonist with EC50 of 22.4 nM.(In Vitro):Mirabegron (YM178) increases cyclic AMP accumulation in Chinese hamster ovary (CHO) cells expressing human β3-adrenoceptor (AR). EC50 value is 22.4 nM. EC50 values of Mirabegron for human β1- and β2-ARs are 10,000 nM or more, respectively. EC50 of Mirabegron in rat bladder strips precontracted with 10-6 M Carbachol (CCh) is 5.1 μM, whereas that in human bladder strips precontracted with 10-7 M CCh is 0.78 μM. Mirabegron concentration-dependently increases the accumulation of cAMP in CHO cells expressing human β3-ARs, with an EC50 value and I.A. of 22.4 nM and 0.8, respectively. Mirabegron has little agonistic effect on β1- and β2-ARs. Compared by EC50 value, Mirabegron is approximately one third as potent as isoproterenol. The maximal relaxant effects of Mirabegron are 94±1%, that of CCh, indicating that Mirabegron acts a full agonist in the rat bladder. The maximal relaxant effects of Mirabegron is 89.4±2.3%.(In Vivo):Mirabegron (YM178) produces a dose-dependent decrease in the frequency of rhythmic bladder contraction in anesthetized rats. In contrast, Mirabegron does not decrease the amplitude of rhythmic bladder contraction at up to 3 mg/kg i.v.. On the contrary, Oxybutynin significantly increases the frequency of rhythmic bladder contraction and decreased its amplitude at doses of 0.272 mg/kg i.v. or more.

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YM-178

Endocrinology/Hormones

Adrenergic Receptor

β3-adrenoceptor

Neurological Disease

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223673-61-8

396.51

C21H24N4O2S

>98% (HPLC)

Ethanol: 8 mg/mL (20.17 mM); DMSO: 79 mg/mL (199.23 mM)

O=C(NC1=CC=C(CCNC[C@H](O)C2=CC=CC=C2)C=C1)CC3=CSC(N)=N3

2-(2-Amino-1,3-thiazol-4-yl)-N-[4-(2-{[(2R)-2-hydroxy-2-phenylethyl]amino}ethyl)phenyl]acetamide

(-20℃)

With Ice Pack

≥ 2 years