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TGR5 Receptor Agonist

Cat. No. M2588
TGR5 Receptor Agonist Structure
Size Price Availability Quantity
10mM*1mL in DMSO USD 95  USD95 In stock
2mg USD 60  USD60 In stock
5mg USD 90  USD90 In stock
10mg USD 150  USD150 In stock
25mg USD 280  USD280 In stock
50mg USD 500  USD500 In stock
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Quality Control & Documentation
Biological Activity

TGR5 Receptor Agonist is a potent TGR5(GPCR19) agonist, showed improved potency in the U2-OS cell assay (pEC50 = 6.8) and in melanophore cells (pEC50 = 7.5).TGR5 Receptor Agonist has good physicochemical properties.But it has no measurable activity against three of the common cytochrome P450 (CYP450) isoforms (1A2, 2C9, and 2D6) or hERG dofetilide binding (pIC50 <4.3).GR5 receptor agonists are potentially useful therapeutics for metabolic disorders like type II diabetes and its associated complications.

Customer Product Validations & Biological Datas
Source Sci Rep (2018). Figure 5. TGR5
Method TGR5KO cells
Cell Lines NRVMs
Concentrations 10–100 μM
Incubation Time 10–15 mins
Results NMVMs in culture show spontaneous contraction. Incubation with INT-777, in the range of 10–100 μM, does not change the contraction rate of NMVMs in both wild type and TGR5KO cells
Chemical Information
Molecular Weight 361.22
Formula C18H14Cl2N2O2
CAS Number 1197300-24-5
Solubility (25°C) DMSO ≥ 30 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.


[1] Evans KA,et al. J Med Chem. Discovery of 3-aryl-4-isoxazolecarboxamides as TGR5 receptor agonists.

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Keywords: TGR5 Receptor Agonist supplier, GPCR19/TGR5, inhibitors, activators

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