Mirabegron , ≥99% , 223673-61-8

Synonym(s):
2-(2-Amino-1,3-thiazol-4-yl)-N-[4-[2-[((2R)-2-hydroxy-2-phenylethyl)amino]ethyl]phenyl]acetamide;2-Amino-N-[4-[2-[[(2R)-2-hydroxy-2-phenylethyl]amino]ethyl]phenyl]-4-thiazoleacetamide;YM 178;YM178(R)-Mirabegron

CAS NO.：223673-61-8

Empirical Formula: C21H24N4O2S

Molecular Weight: 396.51

MDL number: MFCD11100356

EINECS: 800-126-3

PRODUCT Properties

• Melting point: 138-140°C
• Boiling point: 690.0±55.0 °C(Predicted)
• Density: 1.313
• storage temp.: Keep in dark place,Inert atmosphere,Store in freezer, under -20°C
• solubility: Chloroform (Slightly, Heated), Methanol (Slightly)
• form: Solid
• pka: 13.51±0.70(Predicted)
• color: White to Pale Yellow
• InChIKey: PBAPPPCECJKMCM-IBGZPJMESA-N
• SMILES: S1C=C(CC(NC2=CC=C(CCNC[C@H](O)C3=CC=CC=C3)C=C2)=O)N=C1N
• CAS DataBase Reference: 223673-61-8

Description and Uses

Betanis (Mirabegron) was approved in July 2011 by the Japanese Ministry of Health, Labour, and Welfare for the treatment of urgency, urinary frequency, and urinary urge urinary incontinence associated with overactive bladder (OAB). Mirabegron is synthesized by coupling 4-nitrophenethyl amine to (R)-2-hydroxy-2-phenylacetic acid. The resulting amide is reduced to an amine. The nitro group is then reduced and the resulting aniline is coupled to 2-(2-aminothiazol-4-yl) acetic acid to give mirabegron. Mirabegron has an EC₅₀ of 22 nM (intrinsic activity=0.8) for β3-AR with no detectable activity for β1- andβ2-AR (EC₅₀>10,000 nM). In an anesthetized rat rhythmic bladder contraction model in which bladder contractions are induced by saline, mirabegron at 3 mg/kg iv decreased the frequency of rhythmic bladder contraction without suppressing contraction amplitude. These data suggest that the activation of β3-AR increases bladder capacity without influencing the frequency of bladder contraction.

A potent bladder relaxant compound

Safety

• Symbol(GHS): GHS08
• Signal word: Warning
• Hazard statements: H361d
• Precautionary statements: P201-P202-P280-P308+P313-P405-P501