TGR5 Receptor Agonist 3

Name: TGR5 Receptor Agonist 3
Brand: MedChemExpress
SKU: HY-146453
Rating: 4.5 (1 reviews)

Cat. No.: HY-146453 Purity: 95.0%: Data Sheet
COA

SDS
Handling Instructions
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TGR5 Receptor Agonist 3 (Compound 19) is a soft-agent G-protein-coupled bile acid receptor 1 (GPBAR1, TGR5) agonist with reduced gallbladder-filling effects (favorable gallbladder safety), with EC50s of 16.4 and 209 nM for hTGR5 and mTGR5, respectively.

For research use only. We do not sell to patients.

TGR5 Receptor Agonist 3 Chemical Structure

CAS No. : 2643391-08-4

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	Get quote
200 mg	Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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Biological Activity
Purity & Documentation
References
Customer Review

Description

In Vitro

TGR5 Receptor Agonist 3 (compound 19) (10-50μM, 2 hours) activates TGR5 in fetal rat intestinal cells (FRIC) and NCI-H716 cells to promote GLP-1 secretion in a dose-dependent manner^[1].

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

In Vivo

TGR5 Receptor Agonist 3 (compound 19) has good targeting and can effectively activate TGR5, thus promoting the secretion of GLP-1 in plasma and regulating the homeostasis of glucose metabolism in male ICR mice^[1].
TGR5 Receptor Agonist 3 (compound 19) can be rapidly absorbed and metabolized in male ICR mice, and has a good safety profile^[1].
TGR5 Receptor Agonist 3 (compound 19) (oral gavage; 50 mg/kg; one hour) can be gavaged into overnight-fasted male ICR mice for one hour with a C_maxvalue of 0.003 μg/mL ^[1].
TGR5 Receptor Agonist 3 (compound 19) can reduce gallbladder-filling and safety in vivo^[1].

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

Molecular Weight

513.54

Formula

C₂₉H₂₇N₃O₆

CAS No.

2643391-08-4

Appearance

Solid

Color

White to off-white

SMILES

CCOCOC(C1=COC2=C1C=C(C=C2)OC3=C(C=NC=C3)C(N4CCN(C5=C4C=CC=C5)C6CC6)=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

DMSO : 80 mg/mL (155.78 mM; Need ultrasonic and warming; 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	1.9473 mL	9.7363 mL	19.4727 mL
5 mM	0.3895 mL	1.9473 mL	3.8945 mL
10 mM	0.1947 mL	0.9736 mL	1.9473 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.

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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In Vivo Dissolution Calculator

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Working solution concentration: mg/mL

Purity & Documentation

Purity: 95.0%

Select Batch:

Data Sheet (278 KB) SDS (252 KB)

COA (259 KB) HNMR (234 KB) RP-HPLC (256 KB) LCMS (146 KB)

Handling Instructions (2659 KB)

References

[1]. Fanghui Han, et al. Design of G-protein-coupled bile acid receptor 1 (GPBAR1, TGR5) soft drugs with reduced gallbladder-filling effects. Eur J Med Chem. 2020 Oct 1;203:112619. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.9473 mL	9.7363 mL	19.4727 mL	48.6817 mL
	5 mM	0.3895 mL	1.9473 mL	3.8945 mL	9.7363 mL
	10 mM	0.1947 mL	0.9736 mL	1.9473 mL	4.8682 mL
	15 mM	0.1298 mL	0.6491 mL	1.2982 mL	3.2454 mL
	20 mM	0.0974 mL	0.4868 mL	0.9736 mL	2.4341 mL
	25 mM	0.0779 mL	0.3895 mL	0.7789 mL	1.9473 mL
	30 mM	0.0649 mL	0.3245 mL	0.6491 mL	1.6227 mL
	40 mM	0.0487 mL	0.2434 mL	0.4868 mL	1.2170 mL
	50 mM	0.0389 mL	0.1947 mL	0.3895 mL	0.9736 mL
	60 mM	0.0325 mL	0.1623 mL	0.3245 mL	0.8114 mL
	80 mM	0.0243 mL	0.1217 mL	0.2434 mL	0.6085 mL
	100 mM	0.0195 mL	0.0974 mL	0.1947 mL	0.4868 mL