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MedChemExpress - Model Vibegron -1190389-15-1
Vibegron (MK-4618) is a potent, highly selective and orally active β3-adrenoceptor agonist (EC50=1.1 nM). Vibegron can be used for severe urgency urinary incontinence related to overactive bladder[1][2][3].MCE products for research use only. We do not sell to patients.
Vibegron
MCE China:Vibegron
Brand:MedChemExpress (MCE)
Cat. No.HY-19933
CAS:1190389-15-1
Synonyms:MK-4618
Purity:98.26%
Storage:4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Shipping:Room temperature in continental US; may vary elsewhere.
Description:Vibegron (MK-4618) is a potent, highly selective and orally active β3-adrenoceptor agonist (EC50=1.1 nM). Vibegron can be used for severe urgency urinary incontinence related to overactive bladder.
In Vivo:Vibegron (1~12 μΜ; i.v.) exhibits dose dependent decreases in micturition pressure and increases in functional bladder capacity[3]. Vibegron (30 mg/kg; p.o.; 4 weeks) upregulates mRNA levels of type 1, type 3 collagen, TGF‐β1, and HIF‐1α[4]. Vibegron (1 and 10 mg/kg; i.v.; interval 30 minutes) (10 mg/kg) in oxo-M-treated rats makes bladder capacity significantly decreased compared with oxo-M-not treated rats (intravesical instillation of vehicle)[5].
IC50 & Target:β adrenergic receptor β3 adrenoceptor 1.1 nM (EC50)
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References:
[3]. Edmondson SD, et al. Discovery of Vibegron: A Potent and Selective β3 Adrenergic Receptor Agonist for the Treatment of Overactive Bladder. J Med Chem. 2016;59(2):609-623. [Content Brief]
[4]. Gotoh D, et al. Effects of a new β3-adrenoceptor agonist, vibegron, on neurogenic bladder dysfunction and remodeling in mice with spinal cord injury. Neurourol Urodyn. 2020;39(8):2120-2127. [Content Brief]
[5]. Furuta A, et al. Additive effects of intravenous and intravesical application of vibegron, a β3-adrenoceptor agonist, on bladder function in rats with bladder overactivity. Naunyn Schmiedebergs Arch Pharmacol. 2020;393(11):2073-2080. [Content Brief]
Brand introduction:
• MCE (MedChemExpress) has a global exclusive compound library of more than 200 kinds, and we are committed to providing the most comprehensive range of high-quality small molecule active compounds for scientific research customers around the world;
• More than 50,000 highly selective inhibitors and agonists are involved in various popular signaling pathways and disease areas;
• The products cover a variety of recombinant proteins, peptides, commonly used kits, more PROTAC, ADC and other characteristic products, widely used in new drug research and development, life science and other scientific research projects;
• Provide virtual screening, ion channel screening, metabolomics analysis detection analysis, drug screening and other professional technical services;
• It has a professional experimental center and strict quality control and verification system;
• Provide LC/MS, NMR, HPLC, chiral analysis, elemental analysis and other quality inspection reports to ensure the high purity and high quality of products;
• The biological activity of the products has been verified by the experiments of customers in various countries;
• A variety of top journals such as Nature, Cell, Science and pharmaceutical patents have included the scientific research results of MCE customers;
• Our professional team tracks the latest pharmaceutical and life science research and provides you with the latest active compounds in the world;
• It has established long-term cooperation with the world's major pharmaceutical companies and well-known scientific research institutions。
