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.
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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 |
| 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 |
| 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.
| 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
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
SBI-115 is a TGR5 (GPCR19) antagonist, it decreases hepatic cystogenesis with polycystic liver diseases via inhibiting TGR5. |
| INT-777
INT-777 is a potent TGR5 agonist with EC50 of 0.82 μM. |
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