Home GPCR & G Protein GPCR19 agonist TGR5 Receptor Agonist For research use only.

TGR5 Receptor Agonist

Synonyms: TGR5, CCDC, MDK00245

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

TGR5 Receptor Agonist Chemical Structure

CAS No. 1197300-24-5

Purity & Quality Control

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

TGR5 Receptor Agonist Related Products

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
NCT04959864 Recruiting
Male Infertility
GYNOV|Laboratoire Drouot
 July 7 2021 Not Applicable

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

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


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In vivo
Batch:

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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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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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