An S1P1 antagonist
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TASP0277308

Item No. 11340

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/mlMethanol: 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
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

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    10 mg

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    Product Description

    TASP0277308 is a sphingosine-1-phosphate receptor 1 (S1P1) antagonist (IC50 = 4.2 nM).1 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]GTPγS 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.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Fujii, Y., Hirayama, T., Ohtake, H., et al. Amelioration of collagen-induced arthritis by a novel S1P1 antagonist with immunomodulatory activities. J. Immunol. 188(1), 206-215 (2012).

    2. Grenald, S.A., Doyle, T.M., Zhang, H., et al. Targeting the S1P/S1PR1 axis mitigates cancer-induced bone pain and neuroinflammation. Pain 158(9), 1733-1742 (2017).