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SR 1001 is a retinoic acid receptor-related orphan receptor (ROR) α and γ inverse agonist (Ki values are 172 and 111 nM respectively). SR1001 demonstrates no activity at RORβ or LXR. SR1001 suppresses Th17 cell differentiation and cytokine expression and reduces the severity of disease in an animal model of mulitple sclerosis.
| 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.
| Molecular Weight | 477.4 |
| Formula | C15H13F6N3O4S2 |
| CAS Number | 1335106-03-0 |
| Purity | >98% |
| Solubility | DMSO 41 mg/mL |
| Storage | at -20°C |
Regulation of expression of citrate synthase by the retinoic acid receptor-related orphan receptor α (RORα).
Crumbley C, et al. PLoS One. 2012;7(4):e33804. PMID: 22485150.
Suppression of TH17 differentiation and autoimmunity by a synthetic ROR ligand.
Solt LA, et al. Nature. 2011 Apr 28;472(7344):491-4. PMID: 21499262.
| Related ROR Products |
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S18-000003 is a potent, effective and orally active inhibitor of retinoic acid receptor-related orphan receptor-gamma-t (RORγt), with an IC50 of 29 nM. |
| Neoruscogenin
Neoruscogenin is a bioavailable, potent, and high-affinity agonist of the nuclear receptor RORα (NR1F1). |
| Vimirogant
Vimirogant (also known as AGN-242428 and VTP-43742) is a potent, selective and orally active RORγt inhibitor. |
| GSK805
GSK805 is a potent, orally bioavailable RORγγ Inhibitor, with pIC50 of 8.4 and >8.2 for RORγ FRET assay and Th17 assay. |
| SR2211
SR2211 is a synthetic RORγ-selective modulator, functions as an inverse agonist, with a Ki of 105 nM and an IC50 of ~320 nM. |
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