TGR5 Receptor Agonist

Catalog No.S0193 Batch:S019301

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Technical Data

Formula

C18H14Cl2N2O2
Molecular Weight 361.22 CAS No. 1197300-24-5
Solubility (25°C)* In vitro DMSO 96 mg/mL (265.76 mM)
Ethanol 12 mg/mL (33.22 mM)
Water Insoluble
In Vivo (Add solvents to the product individually and in order.)
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.
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description 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.
Targets
GPCR19
(in melanophore cells assay)		 GPCR19
(in U2-OS cell assay)
7.5(pEC50) 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.

Protocol (from reference)

Cell Assay:

[1]
  • Cell Lines

    U2-OS cells and melanophore cells

  • Concentrations

    --

  • Incubation Time

    --

  • Method

    --
Animal Study:

[1]
  • Animal Models

    Male beagle dogs (approx 10 kg)

  • Dosages

    1 mg/kg

  • Administration

    i.j.

References

  • https://pubmed.ncbi.nlm.nih.gov/19902954/

Sellecks TGR5 Receptor Agonist Has Been Cited by 1 Publication

Ursodeoxycholic Acid Suppresses The Malignant Progression of Colorectal Cancer Through TGR5-YAP Axis [ Research Square, 2021, 10.21203/rs.3.rs-274411/v1] PubMed: N/A

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Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.

SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.