Mirabegron

Catalog No.S4009

Mirabegron is a selective β3-adrenoceptor agonist with EC50 of 22.4 nM.

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Mirabegron Chemical Structure

Mirabegron Chemical Structure
Molecular Weight: 396.51

Validation & Quality Control

Quality Control & MSDS

Product Information

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Product Description

Biological Activity

Description Mirabegron is a selective β3-adrenoceptor agonist with EC50 of 22.4 nM.
Targets β3-adrenoceptor [1]
IC50 22.4 nM(EC50)
In vitro Mirabegron concentration-dependently increases the accumulation of cAMP in CHO cells expressing human 3-adrenoceptors (ARs) with I.A. of 0.8. Mirabegron has little agonistic effect on 1- and 2-ARs. Mirabegron concentration-dependently relaxes rat and Human bladder smooth muscle strips precontracted with 10-6 M or 10-7 M carbachol with EC50 values of 5.1 μM and 0.78 μM, respectively. The maximal relaxant effects of Mirabegron are 94.0 % and 89.4% that of carbachol, respectively. [1] Mirabegron is a time-dependent inhibitor of CYP2D6 in the presence of NADPH as the IC50 value in human liver microsomes decreased from 13 to 4.3 μM after 30 min preincubation. Mirabegron acts partly as an irreversible or quasi-irreversible metabolism-dependent inhibitor of CYP2D6. [2]
In vivo Mirabegron produces a dose-dependent decrease in the frequency of rhythmic bladder contraction in anesthetized rats. 3 mg/kg i.v. Mirabegron suppresses the frequency to 2 counts/10 min. Mirabegron does not decrease the amplitude of rhythmic bladder contraction. [1] Mirabegron decreases primary bladder afferent activity and bladder microcontractions in rats. Mirabegron (0.3 and 1 mg/kg) inhibits mechanosensitive single-unit afferent activities (SAAs) of Aδ fibers in response to bladder filling. SAAs of C-fibers decrease only at 1 mg/kg Mirabegron treatment. Mirabegron administration suppresses the mean bladder pressure and the number of microcontractions during an isovolumetric condition of the bladder. [3] Mirabegron is efficient on facilitation of bladder storage. Mirabegron dose-dependently decreases the resting intravesical pressure. Mirabegron dose dependently decreases the frequency of nonvoiding contractions, considered an index of abnormal response in bladder storage. Mirabegron exhibits no significant effects on the amplitude of nonvoiding contractions, micturition pressure, threshold pressure, voided volume, residual volume, or bladder capacity. [4]
Features

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Takasu T, et al. J Pharmacol Exp Ther, 2007, 321(2), 642-647.

[2] Takusagawa S, et al. Xenobiotica, 2012, 42(12), 1187-1196.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-06-25)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02744430 Not yet recruiting Ureteral Obstruction|Flank Pain Baylor College of Medicine August 2016 Phase 2
NCT02787083 Not yet recruiting Cystitis, Interstitial Philadelphia Urosurgical Associates|Astellas Pharma Globa  ...more Philadelphia Urosurgical Associates|Astellas Pharma Global Development, Inc. July 2016 Phase 3
NCT02811289 Not yet recruiting Type 2 Diabetes Université de Sherbrooke July 2016 --
NCT02775539 Not yet recruiting Pulmonary Hypertension|Mirabegron|Heart Failure|Pulmonary Vascular Resistance Abnormality Fundación Centro Nacional de Investigaciones Cardiovascul  ...more Fundación Centro Nacional de Investigaciones Cardiovasculares Carlos III|Hospital Clinic of Barcelona|Hospital Universitario 12 de Octubre|Puerta de Hierro University Hospital|Fundació Institut de Recerca de lHospital de la Santa Creu i Sant Pau June 2016 Phase 2
NCT02751931 Not yet recruiting Neurogenic Detrusor Overactivity Astellas Pharma Europe B.V.|Astellas Pharma Inc April 2016 Phase 3

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Chemical Information

Download Mirabegron SDF
Molecular Weight (MW) 396.51
Formula

C21H24N4O2S

CAS No. 223673-61-8
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms YM 178
Solubility (25°C) * In vitro DMSO 79 mg/mL (199.23 mM)
Ethanol 8 mg/mL (20.17 mM)
Water <1 mg/mL (<1 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 4-Thiazoleacetamide, 2-amino-N-[4-[2-[[(2R)-2-hydroxy-2-phenylethyl]amino]ethyl]phenyl]-

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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