TC-SP 14 is a potent and selective S1P1 agonist (EC50 values are 0.042 and 3.47 μM for human S1P1 and S1P3 respectively). Attenuates immune response to antigen challenge and reduces circulating blood lymphocyte counts in a rodent model of delayed-type hypersensitivity. Orally bioavailable.
| Molecular Weight | 450.5 |
| Formula | C25H20F2N2O2S |
| CAS Number | 1257093-40-5 |
| Form | Solid |
| Solubility (25°C) | DMSO 22.52 mg/mL (with gentle warming) |
| Storage | RT, dry |
| 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.
| Related S1P Receptor Products |
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| S1PR1 modulator 1
S1PR1 modulator 1 is a selective S1PR1 inhibitor, with a pIC50 of 7.6, with >40- and >80-fold selectivity, over the other S1PR isoforms S1PR2/3/4. |
| Ozanimod hydrochloride
Ozanimod (RPC-1063) hydrochloride, a sphingosine 1-phosphate (S1P) receptor modulator that binds with high affinity selectively to S1P receptor subtypes 1 (S1P1) and 5 (S1P5). Ozanimod hydrochloride has modulate effect for hS1P1 and hS1P5 receptor with EC50s of 1.03 nM and 8.6 nM, respectively. Ozanimod hydrochloride can be used for the research of relapsing multiple sclerosis (MS) . |
| Icanbelimod
Icanbelimod (S1p receptor agonist 1) is a potent and orally active S1P1 receptor agonist, exhibits an activity of inducing S1P1 internalization (EC50=9.83 nM). Icanbelimod has the potential for the study of arthritis and EAE (experimental autoimmune encephalitis). |
| S1P1 agonist III
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