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Product Name: MK-4618
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Zhejiang Hangyu API Co., Ltd
China
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1190389-15-1

1190389-15-1 structure

1190389-15-1 structure

Name: MK-4618
Chemical Name: Vibegron
CAS Number: 1190389-15-1
Molecular Formula: C₂₆H₂₈N₄O₃
Molecular Weight: 444.526
Catalog: Signaling Pathways GPCR/G Protein Adrenergic Receptor
Create Date: 2018-06-23 12:44:01
Modify Date: 2024-01-02 16:10:36
Vibegron (MK-4618) is a potent, highly selective β3-adrenoceptor agonist (EC50=1.1 nM). Vibegron can be used for severe urgency urinary incontinence related to overactive bladder[1][2][3].

Name	Vibegron
Synonyms	M5TSE03W5U Pyrrolo[1,2-a]pyrimidine-6-carboxamide, 4,6,7,8-tetrahydro-N-[4-[[(2S,5R)-5-[(R)-hydroxyphenylmethyl]-2-pyrrolidinyl]methyl]phenyl]-4-oxo-, (6S)- (6S)-N-[4-({(2S,5R)-5-[(R)-Hydroxy(phenyl)methyl]-2-pyrrolidinyl}methyl)phenyl]-4-oxo-4,6,7,8-tetrahydropyrrolo[1,2-a]pyrimidine-6-carboxamide Vibegron

Description	Vibegron (MK-4618) is a potent, highly selective β3-adrenoceptor agonist (EC50=1.1 nM). Vibegron can be used for severe urgency urinary incontinence related to overactive bladder[1][2][3].
Related Catalog	Research Areas >> Others Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor
Target	β3 adrenoceptor:1.1 nM (EC50)
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]. Animal Model: Rat Dosage: 1~12 μΜ Administration: I.v. Result: Exhibited dose dependent decreases in micturition pressure and increases in functional bladder capacity. Animal Model: Female C57BL/6N mice (9 weeks old) Dosage: 30 mg/kg Administration: P.o.; 4 weeks Result: Upregulated mRNA levels of type 1, type 3 collagen, TGF‐β1, and HIF‐1α at 4 weeks. Animal Model: Female F344 rats (120–160 g) Dosage: 1 and 10 mg/kg Administration: I.v.; Interval 30 minutes Result: Vibegron (10 mg/kg) in oxo-M-treated rats made bladder capacity significantly decreased compared with oxo-M-not treated rats (intravesical instillation of vehicle).
References	[1]. Yoshida M, et al. Efficacy of vibegron, a novel β3-adrenoreceptor agonist, on severe urgency urinary incontinence related to overactive bladder: post hoc analysis of a randomized, placebo-controlled, double-blind, comparative phase 3 study. BJU Int. 2020;125(5):709-717. [2]. Yoshida M, et al. Efficacy of novel β3 -adrenoreceptor agonist vibegron on nocturia in patients with overactive bladder: A post-hoc analysis of a randomized, double-blind, placebo-controlled phase 3 study. Int J Urol. 2019;26(3):369-375. [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. [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. [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.

Density	1.4±0.1 g/cm3
Molecular Formula	C₂₆H₂₈N₄O₃
Molecular Weight	444.526
Exact Mass	444.216156
LogP	0.66
Index of Refraction	1.698