MK-4618

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效且选择性的全 β3 肾上腺素受体激动剂，EC50 为 1.1 nM；对 β1 和 β2 受体没有活性 (EC50>20 uM)。

A potent and selective full β3 adrenergic receptor agonist with EC50 of 1.1 nM; displays no activity for β1 and β2 receptors (EC50>20 uM); dose-dependently increases bladder capacity, decreased micturition pressure, and increased bladder compliance in rhesus monkeys, dose-dependently increases the circulating glycerol and fatty acid levels in rhesus and rat in vivo; shows the potential for treatment of overactive bladder with M2/M3 antimuscarinics.Other Indication Phase 3 Clinical.

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Vibegron (1~12 μΜ; i.v.) exhibits dose dependent decreases in micturition pressure and increases in functional bladder capacity.Vibegron (30 mg/kg; p.o.; 4 weeks) upregulates mRNA levels of type 1, type 3 collagen, TGF‐β1, and HIF‐1α.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). Animal Model:RatDosage: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).

MK 4618 | MK4618 | Vibegron | KRP-114V | RVT-901

GPCR/G Protein

Adrenergic Receptor

Adrenergic Receptor

Other Indications

Other Disease

1190389-15-1

444.535

C26H28N4O3

>98% (HPLC)

In Vitro:?DMSO : 95 mg/mL (213.71 mM)

O=C([C@@H]1CCC2=NC=CC(N21)=O)NC3=CC=C(C[C@H]4N[C@@H]([C@H](O)C5=CC=CC=C5)CC4)C=C3

(S)-N-(4-(((2S,5R)-5-((R)-hydroxy(phenyl)methyl)pyrrolidin-2-yl)methyl)phenyl)-4-oxo-4,6,7,8-tetrahydropyrrolo[1,2-a]pyrimidine-6-carboxamide

(-20℃)

With Ice Pack

≥ 2 years