GSK 4112 is a selective Rev-Erbα agonist with an EC50 value of 0.4 μM, which can be used to explore the function of Rev-erbα in transcriptional repression, biological regulation of circadian rhythms and metabolic pathways.
| Molecular Weight | 396.89 |
| Formula | C18H21ClN2O4S |
| CAS Number | 1216744-19-2 |
| Form | Solid |
| Solubility (25°C) | DMSO 9.92 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.
[1] Dai, et al. Mol Pharmacol. Inhibition of TRPP3 channel by amiloride and analogs.
| Related REV-ERB Products |
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| SR12418
SR12418 is a REV-ERB-specific synthetic ligand with IC50 values of 68 nM for REV-ERBα and 119 nM for REV-ERBβ. SR12418 can be used in studies related to experimental autoimmune encephalomyelitis (EAE) and colitis. |
| SR-29065
SR-29065 is a selective REV-ERBα agonist for autoimmune disease research. |
| STL1267
STL1267 is a potent REV-ERB agonist that crosses the blood-brain barrier with a Ki value of 0.16 µM for REV-ERBα. STL1267 showed no cytotoxicity and inhibited BMAL1 gene expression. |
| SR9011 hydrochloride
SR9011 hydrochloride is a REV-ERBα/β agonist with IC50s of 790 nM and 560 nM for REV-ERBα and REV-ERBβ, respectively. |
| SR9011
SR9011 is a REV-ERBα/β agonist with IC50s of 790 nM and 560 nM for REV-ERBα and REV-ERBβ, respectively. |
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