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TGR5 Receptor Agonist GPCR19 agonist

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

Cat.No.S0193

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

Chemical Structure

Molecular Weight: 361.22

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Quality Control

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

Cited in Nature Medicine for its top-tier quality
COA
NMR
SDS
Datasheet

99.93

Related Targets	CXCR Hedgehog/Smoothened PKA Adrenergic Receptor AChR 5-HT Receptor Histamine Receptor Dopamine Receptor Ras KRas
Other GPCR19 Inhibitors	SBI-115 INT-777 SB-756050 BAR501

Chemical Information, Storage & Stability

Molecular Weight	361.22	Formula	C₁₈H₁₄Cl₂N₂O₂	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1197300-24-5	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	TGR5, CCDC, MDK00245			Smiles	CC1=C(C(=NO1)C2=CC=CC=C2Cl)C(=O)N(C)C3=CC=C(C=C3)Cl

Solubility

In vitro
Batch:

DMSO : 96 mg/mL (265.76 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 12 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

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.

Mechanism of Action

Targets/IC₅₀/Ki	GPCR19 (in melanophore cells assay) 7.5(pEC50) GPCR19 (in U2-OS cell assay) 6.8(pEC50)
In vitro	This compound (TGR5, CCDC, MDK00245, compd 6) shows improved potency in the U2-OS cell assay (pEC50=6.8) and in melanophore cells (pEC50=7.5).
In vivo	TGR5 Receptor Agonist (TGR5, CCDC, MDK00245, compd 6), a highly selective small molecule, shows significant improvements in hepatic portal vein GLP-1 secretion and reduction in portal vein glucose levels.
References	[1] https://pubmed.ncbi.nlm.nih.gov/19902954/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04959864	Recruiting	Male Infertility	GYNOV\|Laboratoire Drouot	July 7 2021	Not Applicable

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