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.
|Source||Sci Rep (2018). Figure 5. TGR5|
|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|
|Solubility (25°C)||DMSO ≥ 30 mg/mL|
Powder -20°C 3 years ; 4°C 2 years
In solvent -80°C 6 months ; -20°C 1 month
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Related GPCR19/TGR5 Products|
|Ursodeoxycholic acid sodium
Ursodeoxycholic acid (Ursodeoxycholate) sodium is a secondary bile acid issued from the transformation of (cheno)deoxycholic acid by intestinal bacteria, acting as a key regulator of the intestinal barrier integrity and essential for lipid metabolism.
SB756050 is a selective TGR5 agonist. SB756050 has the potential for type 2 diabetes treatment.
|Deoxycholic acid sodium salt
Deoxycholic acid sodium salt activates the G protein-coupled bile acid receptor TGR5.
SBI-115 is a TGR5 (GPCR19) antagonist, it decreases hepatic cystogenesis with polycystic liver diseases via inhibiting TGR5.
INT-777 is a potent TGR5 agonist with EC50 of 0.82 μM.
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