製品番号: HY-19933

Vibegron

(別名: MK-4618)

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

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.

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純度: 98.09%
CAS 番号: 1190389-15-1
分子式: C₂₆H₂₈N₄O₃
分子量:444.53

保管条件:

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)

Vibegron 構造式

CAS 番号: 1190389-15-1

容量

価格（税別）

在庫状況

数量

Amount: USD 0.00

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体内実験
- 臨床実験
化学情報
Publications (1)
溶剤 & 溶解度
- 体外
- 体内
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target

β3 adrenoceptor

1.1 nM (EC₅₀)

Adrenergic Receptor アイソフォーム固有の製品をすべて表示 :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	0.57 nM Compound: 7; vibegron; MK-4618	Agonist activity at rhesus monkey beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay Agonist activity at rhesus monkey beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay	[PMID: 26709102]
CHO	EC₅₀	1.1 nM Compound: 7; vibegron; MK-4618	Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay	[PMID: 26709102]
CHO	EC₅₀	1.6 nM Compound: 7; vibegron; MK-4618	Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serum Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serum	[PMID: 26709102]
CHO	EC₅₀	11 nM Compound: 7; vibegron; MK-4618	Agonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay Agonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay	[PMID: 26709102]
CHO	EC₅₀	122 nM Compound: 7; vibegron; MK-4618	Agonist activity at rat beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serum Agonist activity at rat beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serum	[PMID: 26709102]
CHO	EC₅₀	7.1 nM Compound: 7; vibegron; MK-4618	Agonist activity at rhesus monkey beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serum Agonist activity at rhesus monkey beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serum	[PMID: 26709102]
CHO	EC₅₀	86 nM Compound: 7; vibegron; MK-4618	Agonist activity at rat beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay Agonist activity at rat beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay	[PMID: 26709102]
HEK293	IC₅₀	>10 μM Compound: 7; vibegron; MK-4618	Inhibition of human SERT expressed in HEK293 cells preincubated for 30 mins followed by fluorescent substrate addition measured after 30 mins by plate reader analysis Inhibition of human SERT expressed in HEK293 cells preincubated for 30 mins followed by fluorescent substrate addition measured after 30 mins by plate reader analysis	[PMID: 26709102]

体内実験

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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).

臨床実験

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

化学情報

CAS 番号 1190389-15-1
性状 Solid
分子量 444.53
分子式 C₂₆H₂₈N₄O₃
Color White to off-white
SMILES

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
別名

MK-4618
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

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)

Publications (1)

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Naunyn Schmiedebergs Arch Pharmacol

Target and off-target effects of vibegron on smooth muscle contraction of human detrusor and prostate tissues. [Abstract]

2025 Nov 3. PMID: 41184650

溶剤 & 溶解度

体外:

DMSO : 95 mg/mL (213.71 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2496 mL

11.2478 mL

22.4957 mL

5 mM

0.4499 mL

2.2496 mL

4.4991 mL

10 mM

0.2250 mL

1.1248 mL

2.2496 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

モル濃度計算機

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 4.75 mg/mL (10.69 mM); Clear solution

This protocol yields a clear solution of ≥ 4.75 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (47.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 4.75 mg/mL (10.69 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 4.75 mg/mL.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (47.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 4.75 mg/mL (10.69 mM); Clear solution

This protocol yields a clear solution of ≥ 4.75 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (47.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

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COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
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MS (2659 KB)
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OR (2659 KB)
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Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[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. [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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2496 mL	11.2478 mL	22.4957 mL	56.2392 mL
	5 mM	0.4499 mL	2.2496 mL	4.4991 mL	11.2478 mL
	10 mM	0.2250 mL	1.1248 mL	2.2496 mL	5.6239 mL
	15 mM	0.1500 mL	0.7499 mL	1.4997 mL	3.7493 mL
	20 mM	0.1125 mL	0.5624 mL	1.1248 mL	2.8120 mL
	25 mM	0.0900 mL	0.4499 mL	0.8998 mL	2.2496 mL
	30 mM	0.0750 mL	0.3749 mL	0.7499 mL	1.8746 mL
	40 mM	0.0562 mL	0.2812 mL	0.5624 mL	1.4060 mL
	50 mM	0.0450 mL	0.2250 mL	0.4499 mL	1.1248 mL
	60 mM	0.0375 mL	0.1875 mL	0.3749 mL	0.9373 mL
	80 mM	0.0281 mL	0.1406 mL	0.2812 mL	0.7030 mL
	100 mM	0.0225 mL	0.1125 mL	0.2250 mL	0.5624 mL

Keywords

Vibegron

1 Cited Publications

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Vibegron

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

MedChemExpress（MCE）の使用を引用している文献 Vibegron

Adrenergic Receptor アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (1)

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

Vibegron

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

MedChemExpress（MCE）の使用を引用している文献 Vibegron

Adrenergic Receptor アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (1)

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

Vibegron 関連分類

HY-19933 関連分類