An antagonist of RORγt
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TMP920

Item No. 46471

Technical Information
Formal Name
4-[(3,5-dimethyl-4-isoxazolyl)methoxy]-N-[(2,4-dimethylphenyl)phenylmethyl]-benzeneacetamide
CAS Number
1421837-45-7
Molecular Formula
C29H30N2O3
Formula Weight
Purity
≥98%
A solid
SMILES
O=C(CC1=CC=C(C=C1)OCC2=C(C)ON=C2C)NC(C3=CC=C(C)C=C3C)C4=CC=CC=C4
InChi Code
InChI=1S/C29H30N2O3/c1-19-10-15-26(20(2)16-19)29(24-8-6-5-7-9-24)30-28(32)17-23-11-13-25(14-12-23)33-18-27-21(3)31-34-22(27)4/h5-16,29H,17-18H2,1-4H3,(H,30,32)
InChi Key
SHMBIDOWYJZWLB-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    TMP920 is an antagonist of retinoic acid receptor-related orphan receptor γt (RORγt; IC50 = 30 nM).1 It selectively inhibits RORγt-dependent transactivation over transactivation of 22 other nuclear receptors in HEK293 cells at 10 µM. TMP920 reduces the differentiation of primary naïve CD4+ T cells into T helper 17 (Th17) cells and reduces the levels of IL-17 in wild-type but not RORγt-deficient CD4+ T cells isolated from mice in a model of experimental autoimmune encephalomyelitis (EAE). It reduces CNS-infiltrating mononuclear cells, disease severity, and disease progression in a mouse model of EAE at 500 µg/animal.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Xiao, S., Yosef, N., Yang, J., et al. Small-molecule RORγt antagonists inhibit T helper 17 cell transcriptional network by divergent mechanisms. Immunity 40(4), 477-489 (2014).