Description
What is Mirabegron?
Mirabegron is 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 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.
Function and Application
1.Mirabegron is a selective β3-adrenoceptor agonist with EC50 of 22.4 nM.
2.Uses for A potent bladder relaxant compound
3.Uses for Potent bladder relaxant and reagent for diabetes remedy.;Labeled Mirabegron, intended for use as an internal standard for the quantification of Mirabegron by GC- or LC-mass spectrometry.
| Product name | Mirabegron | |
| Reference | EDMF standard | |
| Test Items | Specifications | Results |
| Appearance | White or off-white crystalline powder | Off-white crystalline powder |
| Identification | 1)The infrared absorption spectrum is in accordance with the spectrum obtained with Mirabegron RS. | Conforms |
| 2)The retention time of the major peak in the chromatogram obtained with test solution conform to that in the chromatogram obtained with reference solution as Assay test. | Conforms | |
| Water | ≤0.5% | 0.1% |
| Sulfated ash | ≤0.1% | <0.1% |
| Isomer (HPLC) | ≤0.15% | 0.06% |
| Related substances (HPLC) | Phenethylamine amino thiazole≤0.15% | 0.12% |
| Amino compound≤0.15% | <LOD(LOD=0.02%) | |
| Any unspecified impurity≤0.10% | <LOQ(LOQ=0.05%) | |
| Total impurities≤0.5% | 0.12% | |
| Assay (HPLC) | 98.0%-102.0%(on anhydrous basis) | 99.3% |
| Elemental Impurities | Pd≤10ppm | <LOD(LOD=0.7ppm) |
| Residual Solvents (GC) | Methanol≤3000ppm | <LOD(LOD=45ppm) |
| Ethanol≤5000ppm | <LOQ(LOQ=100ppm) | |
| Dichloromethane≤600ppm | <LOD(LOD=18ppm) | |
| Ethyl acetate≤5000ppm | 20ppm | |
| Tetrahydrofuran≤720ppm | <LOD(LOD=2ppm) | |
| Toluene≤890ppm | <LOD(LOD=3ppm) | |
| Conclusion | Results for reference | |
