Mirabegron (YM178)
Mirabegron (YM178) is the first selective β3-adrenoceptor (β3-AR) agonist with EC50 value of 22.4 nM which is clinically effective for overactive bladder [1].
β3-AR, one of three β-adrenoceptors (β-AR) subtypes, is sparsely distributed in the humans, and functional responses regulated by have been discovered in human brown and white fat cells, and gall bladder, stomach, small intestine, prostate, colon, and bladder [1].
Mirabegron (YM178) exhibits significant selectivity for β-ARs. When tested with Chinese hamster ovary expressing human β-ARs, EC50 values of Mirabegron for β1-ARs, β2-ARs and β3-ARs were 22.4 nM, 10000 nM or more, respectively. The ratio of intrinsic activities of Mirabegron (YM178) versus maximal response induced by isoproterenol of nonselective β-AR agonist was 0.8 for human β3-AR, 0.1 for human β1-AR, and 0.1 for human β2-AR [1].
In anesthetized rats, Mirabegron (YM178) at a dose of 3 mg/kg i.v. reduced the frequency of rhythmic bladder contraction caused by intravesical filling with saline without inhibiting its amplitude. By contrast, Oxybutynin apparently raised the frequency of rhythmic bladder contraction and reduced its amplitude at doses of 0.272 mg/kg i.v. or more [1].
Reference:
[1]. Takasu T, Ukai M, Sato S, et al. Effect of (R)-2-(2-aminothiazol-4-yl)-4'-{2-[(2-hydroxy-2-phenylethyl)amino]ethyl} acetanilide (YM178), a novel selective beta3-adrenoceptor agonist, on bladder function. The Jounal of pharmacology and experimental therapeutic. 2007, 321(2):642-7.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 396.51 |
| Cas No. | 223673-61-8 |
| Formula | C21H24N4O2S |
| Solubility | insoluble in H2O; ≥16.13 mg/mL in EtOH; ≥19.83 mg/mL in DMSO |
| Chemical Name | 2-(2-amino-1,3-thiazol-4-yl)-N-[4-[2-[[(2R)-2-hydroxy-2-phenylethyl]amino]ethyl]phenyl]acetamide |
| SDF | Download SDF |
| Canonical SMILES | C1=CC=C(C=C1)C(CNCCC2=CC=C(C=C2)NC(=O)CC3=CSC(=N3)N)O |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment:[1] | |
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Cell lines |
Chinese hamster ovary (CHO) cells expressing human β3-adrenoceptor (AR) |
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Reaction Conditions |
10-10 ~ 10-4 M for 10 min incubation |
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Applications |
Mirabegron concentration-dependently increased the accumulation of cyclic AMP (cAMP) in CHO cells expressing human β3-AR, with an EC50 value of 22.4 nM. Mirabegron had little agonistic effect on β1-AR and β2-AR, and did not induce cAMP elevation in untransfected CHO cells. |
| Animal experiment:[1] | |
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Animal models |
Male (350 to 400 g) and female (225 to 290 g) Wistar rats |
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Dosage form |
3 mg/kg Administered intravenously (i.v.) |
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Applications |
Mirabegron at a dose of 3 mg/kg i.v. decreased the frequency of rhythmic bladder contraction induced by intravesical filling with saline without suppressing its amplitude in anesthetized rats. These findings suggest the suitability of mirabegron as a therapeutic drug for the treatment of symptoms of overactive bladder such as urinary frequency, urgency, and urge incontinence. |
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Note |
The technical data provided above is for reference only. |
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References: 1. Takasu T, Ukai M, Sato S, et al. Effect of (R)-2-(2-aminothiazol-4-yl)-4'-{2-[(2-hydroxy-2-phenylethyl)amino]ethyl} acetanilide (YM178), a novel selective beta3-adrenoceptor agonist, on bladder function. Journal of Pharmacology and Experimental Therapeutics, 2007, 321(2): 642-647. |
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