What is Mirabegron?
Miraperon is the first β3 adrenoceptor agonist used to treat overactive bladder, and its successful marketing has filled the blank of β adrenoceptor agonist in the treatment of overactive bladder.
Mirabegron powder is white to light yellow powder, soluble in chloroform (slight, heated) and methanol (slight).
| Product name | Mirabegron |
| CAS | 223673-61-8 |
| Molecular formula | C21H24N4O2S |
| Molecular weight | 396.51 |
| EINECS Number | 800-126-3 |
| Storage condition | Keep in dark place,Inert atmosphere,Store in freezer, under -20°C |
| Melting point | 138-140°C |
| Solubility | Soluble in chloroform (slight, heated) and methanol (slight) |
| Appearance | White to light yellow powder |
| Boiling point | 690.0±55.0 °C(Predicted) |
| Density | 1.313 |
What is the pharmacological action of Mirabegron?
Mirabegron relaxes bladder detrusor and increases its stability mainly by acting on β3 receptor. Three subtypes of β receptor (β1, B2 and β3) were found in human detrusor muscle cells and urethral epithelial cells, and the mRNA of β3 receptor was mainly expressed in human detrusor smooth muscle cells, accounting for 97% of β receptor mRNA in bladder tissue. The expression of β receptor mRNA and the function of its signal pathway suggest that β3 receptor plays a mainstay role in normal and diseased bladder.
Product Specification
| Item | Specification | Results |
| Description | White Powder | Powder |
| Identification | (1)304nm,260nm. | confirmed |
| Melting Point | 192℃~196℃ | 192℃~196℃ |
| Specific Rotation | +124°~+129° | +127.1° |
(HPLC) Related substances |
(1)(Single):≤0.5% | 0.31% |
| (2)(Total):≤1.0% | 0.59% | |
| Loss On Drying | ≤0.5% | 0.1% |
| Assay | ≥98.5% | 99.5% |
| Sieve analysis | ≤30μm | confirmed |
| Conclusion: | Conform with enterprise specification. | |
What is the efficacy of Mirabegron?
Mirabegron powder has a remarkable effect in treating the symptoms of overactive bladder. It can reduce the excessive contraction of bladder and effectively reduce the occurrence and severity of frequent urination, urgency and urinary incontinence. This enables patients to better control urination and improve their quality of life.
HTML5 atlas of Mirabegron
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Biological activity of Mirabegron:
| Describe | Mirabegron is a selective adrenergic receptor (β3-adrenoceptor) agonist with EC50 of 22.4 nM. |
| In vitro studies | Mirabegron (YM178) increases cyclic AMP accumulation in Chinese hamster ovary (CHO) cells expressing human β3-adrenergic receptor (AR). The EC50 value is 22.4 nM. Mirabegron has EC50 values of 10,000 nM or higher for human β1- and β2-AR, respectively. The EC50 of Mirabegron in rat bladder strips precontracted with 10-6M Carbachol (CCh) is 5.1 μM, while the EC50 in human bladder strips precontracted with 10-7M CCh is 0.78 μM. Mirabegron increases cAMP accumulation in CHO cells expressing human β3-AR in a concentration-dependent manner, with EC50 values and IA of 22.4 nM and 0.8, respectively. Mirabegron has little agonistic effect on β1- and β2-ARs. Compared with the EC50 value, Mirabegron is about one-third of isoproterenol. The maximum relaxant effect of Mirabegron was 94±1% of the maximum relaxant effect of CCh, indicating that Mirabegron acts as a full agonist in rat bladder. The maximum relaxant effect of Mirabegron was 89.4±2.3%. |
| In vivo studies | Mirabegron (YM178) produces a dose-dependent decrease in the frequency of rhythmic bladder contractions in anesthetized rats. In contrast, mirabegron does not decrease the amplitude of rhythmic bladder contractions up to 3 mg/kg iv. In contrast, oxybutynin significantly increases the frequency of rhythmic bladder contractions and decreases their amplitude at doses of 0.272 mg/kg iv or more. |
| Cell experiments | CHO cells (105) were seeded in each well of a 24-well culture plate and subcultured. Three days later, the medium was exchanged with 250 μL/well Hanks' balanced salt solution containing 0.1 mM 3-isobutyl-1-methylxanthine, pH 7.4. The cells were incubated with each compound (isoproterenol, Mirabegron, BRL37344 and CL316,243, final concentrations 10-10 to 10-4 M) at 37°C for 10 min, and then the incubation was terminated by adding 250 μL of 0.2 M HCl. The cAMP concentration in the reaction mixture was measured by radioimmunoassay using a 125I-cAMP assay system using a gamma counter. 50 microliters of the reaction mixture was incubated with 50 μL of the succinyl reagent at room temperature for 10 min, after which the reaction was terminated by adding 400 μL of the buffer solution. Fifty microliters of succinylated sample were incubated with 50 μL of 125 I-cAMP and 50 μL of anti-cAMP antibody at 4 °C for 24 h. At the end of the incubation period, 250 μL of activated charcoal suspension was added and centrifuged at 2800 g for 10 min at 4 °C. 250 microliters of supernatant were transferred to a tube and counted for 1 min using a gamma counter. The intrinsic activity (IA) of each β-adrenergic receptor agonist relative to isoproterenol was calculated using the maximum response of each compound. |
| Animal experiments | Rats Male (350 to 400 g) and female (225 to 290 g) Wistar rats were used. Mirabegron was administered in free form at doses of 0.03, 0.1, 0.3, 1, and 3 mg/kg, and oxybutynin was administered at doses of 0.0272, 0.0907, 0.272, 0.907, and 2.72 mg/kg. |
| References | Takasu T, 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. J Pharmacol Exp Ther. 2007 May;321(2):642-7. |
What are the side effects of Mirabegron?
Although Mirabegron powder is very effective for many patients, there may be some side effects during use. Common side effects include headache, gastrointestinal discomfort, dizziness and fatigue. These side effects are usually temporary and will gradually decrease with the use of the product. If these side effects persist or worsen, patients should consult a doctor in time.
How and where to buy Mirabegron powder wholesale?
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Note: This compound should be used for research purposes only. These claims have not been evaluated by the Food and Drug Administration. Please consult your doctor and learn about available studies before using them. This product is not intended to diagnose, treat, cure, or prevent any disease.
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