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TGR5 Receptor Agonist

Cat. No. M2588
TGR5 Receptor Agonist Structure
Size Price Availability Quantity
10mM*1mL In DMSO USD 200 In stock
1mg USD 125 In stock
5mg USD 250 In stock
10mg USD 400 In stock
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Quality Control
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 361.22
Formula C18H14Cl2N2O2
CAS Number 1197300-24-5
Purity >98%
Solubility DMSO 50 mM
Storage at -20°C

Discovery of 3-aryl-4-isoxazolecarboxamides as TGR5 receptor agonists.
Evans KA,et al. J Med Chem. 2009 Dec 24;52(24):7962-5. PMID: 19902954.

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

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