Cas No.: | 223673-61-8 |
Chemical Name: | Mirabegron |
Synonyms: | Mirabegron;2-(2-amino-1,3-thiazol-4-yl)-N-(4-{2-[(2-hydroxy-2-phenylethyl)amino]ethyl}phenyl)acetamide;2-Amino-N-[4-[2-[[(2R)-2-hydroxy-2-phenylethyl]amino]ethyl]phenyl]-4-thiazoleacetamide;[14C]-Mirabegron;N-(4-(2-(2-hydroxy-2-phenylethylamino)ethyl)phenyl)-2-(2-aminothiazol-4-yl)acetamide;2-Amino-N-[4-[2-[[(2R)-2-hydroxy-2-phenyl-ethyl]amino]-ethyl]phenyl]-4-thiazoleacetamide;4-Thiazoleacetamide, 2-amino-N-(4-(2-(((2R)-2-hydroxy-2-phenylethyl)amino)ethyl)phenyl)-;MIRABEQRON;YM 178;YM-178;2-(2-Amino-1,3-thiazol-4-yl)-N-[4-[2-[((2R)-2-hydroxy-2-phenylethyl)amino]ethyl]phenyl]acetamide;YM178(R)-Mirabegron;Mirabelon;Myrbetriq;Betanis;Mirabegron (YM178);YM178;MVR3JL3B2V;Betmiga;(R)-2-(2-aminothiazol-4-yl)-N-(4-(2-((2-hydroxy-2-phenylethyl)amino)ethyl)phenyl)acetamide;Myrbetriq (TN);2-(2-amino-1,3-thiazol-4-yl)-N-[4-(2-{[(2R)-2-hydroxy-2-phenylethyl]amino}ethyl)phenyl]acetamide;Mirabegron [USAN:INN];2-(2-amino-1,3-thiazol-4-yl)-N-[4-[2-[[(2R)- |
SMILES: | O=C(NC1=CC=C(CCNC[C@H](O)C2=CC=CC=C2)C=C1)CC3=CSC(N)=N3 |
Formula: | C21N4O2SH24 |
M.Wt: | 396.5059 |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | Mirabegron is a selective β3-adrenoceptor agonist with EC50 of 22.4 nM. |
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[1]. |
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%[1]. |