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抑制剂/激活剂

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凋亡与自噬

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Mirabegron 米拉贝隆

Mirabegron (YM 178)是一种选择性的beta3-adrenoceptor（β3肾上腺素受体）激动剂，EC50为22.4 nM

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TK0442
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1mg

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50mg
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￥0.00

产品参数

CAS No.	223673-61-8
生物活性	Mirabegron is a selective β3-adrenoceptor agonist with EC50 of 22.4 nM.
分子式	C21H24N4O2S
分子量	396.51
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	Powder, -20°C ,3 years
溶解性数据	DMSO : 100 mg/mL (252.20 mM; Need ultrasonic)
体内研究	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.
体外研究	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 M Carbachol (CCh) is 5.1 μM, whereas that in human bladder strips precontracted with 10 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%.
文献	•Cell Metab. 2020 Aug 4;32(2):287-300.e7.•Cardiovasc Drugs Ther. 2021 Jun 21.•Patent. WO2015199097A1.
纯度及产品资料	98%

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