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TMP778

Chemical Structure : TMP778

CAS No.: 1422171-08-1

TMP778 (TMP-778;TMP 778)

Catalog No.: PC-60454Not For Human Use, Lab Use Only.

TMP778 (TMP-778) is a potent, selective RORγt inhibitor with IC50 of 7 nM in FRET assays and 63 nM in IL-17 promoter assays, with no inverse agonist activity.

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Biological Activity

TMP778 (TMP-778) is a potent, selective RORγt inhibitor with IC50 of 7 nM in FRET assays and 63 nM in IL-17 promoter assays, with no inverse agonist activity.
TMP778 blocks human Th17 and Tc17 cell differentiation and also acutely modulates IL-17A production and inflammatory Th17-signature gene expression (IL17a, IL17f, IL22, IL26, CCR6, and IL23) in mature human Th17 effector/memory T cells.
TMP778 inhibits IL-17A production in both human and mouse γδ T cells, also inhibits IL-23-induced IL-17A production.
TMP778 attenuates IMQ-induced skin inflammation in vivo.

Physicochemical Properties

M.Wt 494.591
Formula C31H30N2O4
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-(2-((3,5-dimethylisoxazol-4-yl)(hydroxy)methyl)benzofuran-5-yl)-N-((S)-(2,4-dimethylphenyl)(phenyl)methyl)acetamide

References

1. Skepner J, et al. J Immunol. 2014 Mar 15;192(6):2564-75.

2. Xiao S, et al. Immunity. 2014 Apr 17;40(4):477-89.

3. Skepner J, et al. Immunology. 2015 Jul;145(3):347-56.

4. Forcade E, et al. JCI Insight. 2017 Jun 15;2(12). pii: 92111.

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