TASP0277308

TASP0277308 is a sphingosine-1-phosphate receptor 1 (S1P1) antagonist (IC50 = 4.2 nM). It is selective for S1P1 over S1P3, S1P4, and S1P5 (IC50s = >10,000, >10,000, and 8,756 nM, respectively). TASP0277308 inhibits S1P-induced [35S]GTPgammaS binding and forskolin-induced cAMP production in HEK293 cells expressing human S1P1 (IC50s = 7.8 and 4.3 nM, respectively). It inhibits S1P-induced migration of CHO cells expressing human S1P1 (IC50 = 18 nM). In vivo, TASP0277308 (100 mg/kg) induces lymphopenia in mice. It reduces bone erosion in a mouse model of collagen-induced arthritis. Intrathecal administration of TASP0277308 (3 or 10 nmol/animal) reduces flinching and guarding behaviors in a mouse model of cancer-induced bone pain.Formal Name: 3,4-dichloro-N-[(1R)-1-[4-ethyl-5-[3-(4-methyl-1-piperazinyl)phenoxy]-4H-1,2,4-triazol-3-yl]ethyl]-benzenesulfonamide. CAS Number: 945725-50-8. Molecular Formula: C23H28Cl2N6O3S. Formula Weight: 539.5. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Sparingly soluble: 1-10 mg/ml, Methanol: Slightly soluble: 0.1-1 mg/ml. SMILES: ClC1=CC=C(S(N[C@H](C)C2=NN=C(OC3=CC(N4CCN(C)CC4)=CC=C3)N2CC)(=O)=O)C=C1Cl. InChi Code: InChI=1S/C23H28Cl2N6O3S/c1-4-31-22(16(2)28-35(32,33)19-8-9-20(24)21(25)15-19)26-27-23(31)34-18-7-5-6-17(14-18)30-12-10-29(3)11-13-30/h5-9,14-16,28H,4,10-13H2,1-3H3/t16-/m1/s1. InChi Key: MVOULGOLHZCXLD-MRXNPFEDSA-N.