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SR2211 is a synthetic RORγ-selective modulator that potently inhibits production of IL-17 in cells. In vitro, treatment of EL4 with SR2211 represses the IL-17 gene expression. Similarly, the expression of IL-23 receptor (Il23r) is significantly inhibited by SR2211. Treatment of EL-4 cells with SR2211 results in significant inhibition of IL-17 intracellular staining as compared to vehicle treated cells.
| 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 | 527.48 |
| Formula | C26H24F7N3O |
| CAS Number | 1359164-11-6 |
| Purity | >98% |
| Solubility | DMSO |
| Storage | at -20°C |
| 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. |
| SR 1001
SR 1001 is a RORα/γ inverse agonist with Ki values of 172 and 111 nM, respectively. |
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