Mocravimod (KRP-203) hydrochloride is a potent, orally active sphingosine receptor S1P1 and S1P4 agonist with EC50s of 1 nM and 10 nM, respectively, and may be used in studies related to ulcerative colitis (UC).
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Source | Arterioscler Thromb Vasc Biol (2013). Figure 3. KRP-203 |
| Method | i.v. | |
| Cell Lines | LDL-R-/- mice | |
| Concentrations | 3.0 mg/kg | |
| Incubation Time | 16 weeks | |
| Results | In addition, reduced production of interleukin (IL)-2 and interferon (IFN)-γ, 2 cytokines released from activated CD4+ T cells in response to concanavalin A or phytohaemagglutinin, was noted in splenocytes obtained from KRP-203–treated mice |
| Molecular Weight | 480.45 |
| Formula | C24H26ClNO3S.HCl |
| CAS Number | 509088-69-1 |
| Solubility (25°C) | DMSO 10 mM |
| 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.
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