Ex26 is a peripherally-restricted biphenylcarboxamide derivative that acts as a highly potent and subtype-selective S1P1 antagonist (IC50 = 0.93 nM against S1PR1 and >3.1 μM against S1PR2/3/4/5). Ex26 significantly elevates CpG-A-stimulated interferon (IFN) production in plasmacytoid dendritic cell culture (10 μM) and prevents S1P1 agonist-induced S1P1 receptor internalization and polyubiquitinylation in HEK cells (0.1-1,000 nM). Ex26 induces lymphocyte sequestration (ED50 = 0.06 mg/kg, i.p.) in lymph nodes and pulmonary edema (2 hr post 30 mg/kg i.p.) in mice, leading to the inhibition of lymphocyte and thymocyte egress (0.1 mg/kg/hr continuously for 3 days after a loading dose of 3 mg/kg). Ex26 has been shown to ameliorate experimental autoimmune encephalomyelitis (EAE) in a mouse MS model and elevate CpG-A-stimulated serum IFN upregulation in mice in vivo (30 mg/kg/d, i.p.).
| Molecular Weight | 494.98 |
| Formula | C28H28ClFN2O3 |
| CAS Number | 1233332-37-0 |
| Solubility (25°C) | DMSO: 25 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.
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