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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: 2025-08-25 17:25:35
  • 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
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
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