Name: TGR5 Receptor Agonist
Brand: Selleck Chemicals
SKU: S0193
Rating: 5 (1 reviews)

TGR5 Receptor Agonist (TGR5, CCDC, MDK00245, compd 6) is a potent agonist of TGR5(GPCR19, GPBAR1, M-BAR). TGR5 Receptor Agonist shows improved potency with pEC50 of 6.8 and 7.5 in the U2-OS cell assay and in melanophore cells, respectively.

TGR5 Receptor Agonist Chemical Structure

CAS: 1197300-24-5

Selleck's TGR5 Receptor Agonist has been cited by 1 publication

Purity & Quality Control

Batch: S019301 DMSO] 96 mg/mL] false] Ethanol] 12 mg/mL] false] Water] Insoluble] false Purity: 99.93%

99.93

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Biological Activity

Description

TGR5 Receptor Agonist (TGR5, CCDC, MDK00245, compd 6) is a potent agonist of TGR5(GPCR19, GPBAR1, M-BAR). TGR5 Receptor Agonist shows improved potency with pEC50 of 6.8 and 7.5 in the U2-OS cell assay and in melanophore cells, respectively.

Targets

GPCR19 ^[1] (in melanophore cells assay)	GPCR19 ^[1] (in U2-OS cell assay)
7.5(pEC50)	6.8(pEC50)

In vitro
In vitro	TGR5 Receptor Agonist (TGR5, CCDC, MDK00245, compd 6) shows improved potency in the U2-OS cell assay (pEC50=6.8) and in melanophore cells (pEC50=7.5).^[1]
Cell Research	Cell lines	U2-OS cells and melanophore cells
	Concentrations	--
	Incubation Time	--
	Method	--

In Vivo
In vivo	TGR5 Receptor Agonist (TGR5, CCDC, MDK00245, compd 6), highly selective small molecule TGR5 receptor agonist, shows significant improvements in hepatic portal vein GLP-1 secretion and reduction in portal vein glucose levels.^[1]
Animal Research	Animal Models	Male beagle dogs (approx 10 kg)
	Dosages	1 mg/kg
	Administration	i.j.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT04959864	Recruiting	Male Infertility	GYNOV\|Laboratoire Drouot	July 7 2021	Not Applicable

References

[1] Karen A Evans, et al. J Med Chem. 2009 Dec 24;52(24):7962-5.

Chemical Information & Solubility

Molecular Weight	361.22	Formula	C₁₈H₁₄Cl₂N₂O₂
CAS No.	1197300-24-5	SDF	--
Smiles	CC1=C(C(=NO1)C2=CC=CC=C2Cl)C(=O)N(C)C3=CC=C(C=C3)Cl
Storage (From the date of receipt)	3 years -20°C powder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years -20°C powder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 96 mg/mL ( (265.76 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 12 mg/mL

Water : Insoluble

Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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