Mirabegron
Mirabegron
CAS: 223673-61-8
Molecular Formula: C21H24N4O2S
Mirabegron - Names and Identifiers
| Name | Mirabegron |
| Synonyms | YM 178 Mirabegron Mirabegron(YM 178) N-(4-(2-(2-hydroxy-2-phenylethylamino)ethyl)phenyl)-2-(2-aminothiazol-4-yl)acetamide 2-Amino-N-[4-[2-[[(2R)-2-hydroxy-2-phenylethyl]amino]ethyl]phenyl]-4-thiazoleacetamide 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)- 2-(2-amino-1,3-thiazol-4-yl)-N-(4-{2-[(2-hydroxy-2-phenylethyl)amino]ethyl}phenyl)acetamide 2-(2-aMino-1,3-thiazol-4-yl)-N-(4-{2-[(2-hydroxy-2-phenylethyl)aMino]ethyl}phenyl)acetaMide (2R)-2-(2-AMinothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)aMino]ethyl]acetic Acid Anilide |
| CAS | 223673-61-8 |
| EINECS | 800-126-3 |
| InChI | InChI=1/C21H24N4O2S/c22-21-25-18(14-28-21)12-20(27)24-17-8-6-15(7-9-17)10-11-23-13-19(26)16-4-2-1-3-5-16/h1-9,14,19,23,26H,10-13H2,(H2,22,25)(H,24,27) |
Mirabegron - Physico-chemical Properties
| Molecular Formula | C21H24N4O2S |
| Molar Mass | 396.51 |
| Density | 1.313 |
| Melting Point | 138-140°C |
| Boling Point | 690.0±55.0 °C(Predicted) |
| Flash Point | 371.1°C |
| Solubility | DMSO 79 mg/mL Water <1 mg/mL Ethanol 8 mg/mL |
| Vapor Presure | 5.45E-20mmHg at 25°C |
| Appearance | Pale yellow or yellow solid |
| Color | White to Pale Yellow |
| pKa | 13.51±0.70(Predicted) |
| Storage Condition | Keep in dark place,Inert atmosphere,Store in freezer, under -20°C |
| Refractive Index | 1.68 |
| Use | A potent bladder relaxant compound |
| In vitro study | Mirabegron concentration-dependently increased the accumulation of cAMP in CHO cells expressing the human B adrenoceptor (ARs), I.A. 0.8. Mirabegron has a minor antagonistic effect on 1-and 2-ARs. Concentration-dependent relaxation of rat and human bladder smooth muscle bands by Mirabegron, 10Mirabegron is a time-dependent inhibitor of CYP2D6, in the presence of NADPH, after 30 min preincubation, the IC50 value in human liver microsomes decreased from 13 to 4.3 μm. Mirabegron is a somewhat irreversible or similarly irreversible metabolically dependent inhibitor of CYP2D6. |
| In vivo study | Mirabegron dose-dependently reduces the frequency of rhythmic bladder contractions in anesthetized rats. Mirabegron administered intravenously at a dose of 3 mg/kg was able to inhibit the frequency of bladder contractions to 2 times/10 min. Mirabegron does not reduce the amplitude of rhythmic bladder contractions. Mirabegron reduces primary bladder afferent activity and bladder microcontraction in rats in vivo. Mirabegron (0.3 and 1 mg/kg) inhibited the afferent activity (SAAs) of mechanosensitivity units of Aδ fibers in response to bladder filling. SAAs of C fiber was reduced only under 1 mg/kg Mirabegron treatment. Mirabegron administration suppressed mean bladder pressure and the number of microcontractions under bladder isovolymic conditions. Mirabegron is able to effectively promote bladder storage. Mirabegron dose-dependently reduces resting intravesical pressure. Mirabegron dose-dependently reduces the frequency of non-empty contractions and is considered an indicator of abnormal responses in bladder storage. Mirabegron had no significant effect on the magnitude of nonempty contractions, starting pressure, urine output, residual volume, or bladder capacity. |
Mirabegron - Introduction
A potent bladder relaxant and reagent for diabetes remedy.
Last Update：2022-10-16 17:15:03
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