WB403

製品番号: HY-120565 純度: 99.16%: Data Sheet SDS COA 取扱説明書
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WB403 is an orally active TGR5 activator with an EC₅₀ of 5.5 μM against human TGR5. WB403 activates TGR5 to stimulate downstream signaling pathways, promote GLP-1 secretion, improve glucose tolerance in mice with type 2 diabetes, and reduce levels of fasting blood glucose, postprandial blood glucose and HbA1c. WB403 increases pancreatic β-cell mass and restores the distribution of α-cells and β-cells in islets. WB403 is applicable to the research of type 2 diabetes.

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WB403 構造式

CAS 番号 : 1594041-84-5

容量	価格（税別）	在庫状況	数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 107	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 107	在庫あり	Estimated Time of Arrival: December 31
Solid
5 mg	$98	在庫あり	Estimated Time of Arrival: December 31
10 mg	$155	在庫あり	Estimated Time of Arrival: December 31
25 mg	$310	在庫あり	Estimated Time of Arrival: December 31
50 mg	$490	在庫あり	Estimated Time of Arrival: December 31
100 mg	$780	在庫あり	Estimated Time of Arrival: December 31
200 mg		お問い合わせ
500 mg		お問い合わせ

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* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

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参考文献
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製品説明

体外実験

WB403 (1-20 μM; 16 h) dose-dependently activates human TGR5 in transiently transfected 293T cells with an EC₅₀ of 5.5 μM, as measured by a CRE-luciferase reporter assay^[1].
WB403 (10 μM; 30 min) significantly stimulates active GLP-1 secretion from human NCI-H716 enteroendocrine cells^[1].

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

ELISA Assay^[1]

Cell Line:	293T cells (transiently transfected with pTGR5)
Concentration:	0, 1, 5, 10, 20, 50 μM
Incubation Time:	30 min
Result:	Dose-dependently stimulated TGR5-mediated cAMP accumulation, with statistically significant increases observed at all tested concentrations relative to the DMSO (+TGR5) control. Showed no stimulation in control 293T cells transfected with an empty plasmid.

Parmacokinetics

Species	Dose	Route	T_1/2	C₀	AUC_0-t	AUC_0-∞	T_max	C_max	Bioavailability
Rat^[1]	40 mg/kg	i.v.	166 min	25.7 μg/mL	24.99 μg·h/mL	26.89 μg·h/mL	/	/	/
Rat^[1]	40 mg/kg	p.o.	176.4 min	/	2.28 μg·h/mL	3.22 μg·h/mL	84.0 min	0.98 μg/mL	12.0 %

体内実験

WB403 (50-100 mg/kg; p.o.; daily; 8 weeks) significantly reduces fasting and postprandial blood glucose levels, decreases HbA_1c levels, and restores islet area in type 2 diabetic ICR mice induced by high-fat diet/Streptozotocin (HY-13753)^[1].
WB403 (50-100 mg/kg; p.o.; daily; for 4 consecutive weeks) significantly reduces fasting and postprandial blood glucose levels, decreases HbA1c, increases insulin levels, restores the normal distribution of islet cells, and expands islet area in spontaneous type 2 diabetic db/db mice^[1].
WB403 (50-100 mg/kg; p.o.; single administration) significantly improves glucose tolerance and increases serum GLP-1 levels in normal ICR mice^[1].

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

Animal Model:	ICR mice (male, 5 weeks old, high-fat diet + streptozotocin-induced type 2 diabetes)^[1]
Dosage:	50 mg/kg; 100 mg/kg
Administration:	p.o.; daily; 8 weeks
Result:	Significantly decreased fasting blood glucose and postprandial blood glucose starting from the first week of intervention, with effects sustained throughout the 8-week treatment period. Significantly reduced serum HbA1c levels compared to vehicle controls. Restored pancreatic islet area to near-normal levels, reversing β-cell loss induced by streptozotocin. Decreased water intake, indicating improved hyperglycemia, while food intake and body weight did not vary significantly compared to vehicle controls.

Animal Model:	db/db (C57BL BKS cg-M+/+ lepr-/-) mice (male, 8 weeks old, spontaneous type 2 diabetes)^[1]
Dosage:	50 mg/kg; 100 mg/kg
Administration:	p.o.; daily; 4 weeks
Result:	Significantly decreased fasting blood glucose and postprandial blood glucose after 1 week of treatment, with effects sustained throughout the 4-week period. Significantly reduced serum HbA1c levels and increased serum insulin levels compared to vehicle controls. Decreased water intake, indicating improved hyperglycemia, while food intake and body weight did not vary significantly compared to vehicle controls. Reduced α-cell infiltration in the islet core, restoring the normal distribution pattern of α-cells (peripheral) and β-cells (core), and increased pancreatic islet area compared to vehicle controls.

Animal Model:	ICR mice (male, non-diabetic)^[1]
Dosage:	50 mg/kg; 100 mg/kg
Administration:	p.o.; single dose; 30 minutes before glucose challenge
Result:	Significantly improved glucose tolerance in normal mice, as shown by reduced blood glucose levels during oral glucose tolerance test and decreased area under the curve (AUC) compared to vehicle controls. Significantly increased serum GLP-1 concentrations compared to vehicle controls.

分子量

403.34

分子式

C₁₉H₁₉BrN₂OS

CAS 番号

1594041-84-5

Appearance

Solid

Color

Off-white to light yellow

SMILES

CCC1=NC=CC(C2=NC(C)=C(S2)COCC3=CC=C(C=C3)Br)=C1

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶剤 & 溶解度

体外:

DMSO : 10 mg/mL (24.79 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.4793 mL	12.3965 mL	24.7930 mL
5 mM	0.4959 mL	2.4793 mL	4.9586 mL
10 mM	0.2479 mL	1.2396 mL	2.4793 mL

View the Complete Stock Solution Preparation Table

* 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

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

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: ≥ 1 mg/mL (2.48 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1 mg/mL (2.48 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 1 mg/mL (2.48 mM); Clear solution

This protocol yields a clear solution of ≥ 1 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 (10.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

純度とドキュメンテーション

純度: 99.16%

Select Batch:

データシート (277 KB) SDS (251 KB)

COA (246 KB) HNMR (259 KB) RP-HPLC (260 KB) MS (68 KB)

取扱説明書 (2659 KB)

参考文献

[1]. Zheng C, et al. A Novel TGR5 Activator WB403 Promotes GLP-1 Secretion and Preserves Pancreatic β-Cells in Type 2 Diabetic Mice. PLoS One. 2015;10(7):e0134051. Published 2015 Jul 24. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.4793 mL	12.3965 mL	24.7930 mL	61.9824 mL
	5 mM	0.4959 mL	2.4793 mL	4.9586 mL	12.3965 mL
	10 mM	0.2479 mL	1.2396 mL	2.4793 mL	6.1982 mL
	15 mM	0.1653 mL	0.8264 mL	1.6529 mL	4.1322 mL
	20 mM	0.1240 mL	0.6198 mL	1.2396 mL	3.0991 mL

WB403 Related Classifications

Metabolic Disease

Molarity Calculator
Dilution Calculator

The molarity calculator equation

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

質量		濃度		体積		分子量 *
	=		×		×

The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）	×	体積 _（開始）	=	濃度 _（終了）	×	体積 _（終了）
	×		=		×
C1		V1		C2		V2

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

WB4031594041-84-5WB 403WB-403G protein-coupled Bile Acid Receptor 1G-protein coupled receptor 19GPCR19TGR5GPBAR1TGR5 activatortype 2 diabetes293T cellsNCI-H716 cellsICR micedb/db (C57BL BKS cg-M+/+ lepr-/-) miceInhibitorinhibitorinhibit

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