Description
RORγt Inverse agonist 8 is a potent, selective, orally bioavailable RORγt inverse agonist, with an IC50 of 19 nM for human RORγt-LBD.
Product information
CAS Number: 2079892-79-6
Molecular Weight: 475.59
Formula: C26H33N7O2
Chemical Name: N-(8-{[(3S)-4-cyclopentanecarbonyl-3-methylpiperazin-1-yl]methyl}-7-methylimidazo[1,2-a]pyridin-6-yl)-2-methylpyrimidine-5-carboxamide
Smiles: C[C@H]1CN(CC2C3=NC=CN3C=C(NC(=O)C3=CN=C(C)N=C3)C=2C)CCN1C(=O)C1CCCC1
InChiKey: GMRCLEMCHGYDSY-KRWDZBQOSA-N
InChi: InChI=1S/C26H33N7O2/c1-17-14-31(10-11-33(17)26(35)20-6-4-5-7-20)15-22-18(2)23(16-32-9-8-27-24(22)32)30-25(34)21-12-28-19(3)29-13-21/h8-9,12-13,16-17,20H,4-7,10-11,14-15H2,1-3H3,(H,30,34)/t17-/m0/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
RORγt Inverse agonist 8 (Cpd 1) is a potent RORγt inhibitor and binds to the ligand binding domain (LBD) of RORγt. RORγt Inverse agonist 8 (0-10μM ;24 hours) results in complete attenuation of IL-17A secretion in a concentration-dependent manner with an IC50 of 60 nM in HUT78 cells. RORγt Inverse agonist 8 selectively suppresses human Th17 and Tc17 cell differentiation. RORγt Inverse agonist 8 polarizes Th17 cells also blocks IL-17A production in a concentration-dependent manner with an IC50 of 92 nM. RORγt Inverse agonist 8 reduces Th17 cell-associated mRNA expression including IL17A, IL17F, IL26, IL23R and CCR6 in a concentration-dependent fashion. RORγt Inverse agonist 8 alters epigenetic regulation at the IL17A and IL23R gene promoters without impairing the DNA binding activity of RORγt.
In Vivo:
RORγt Inverse agonist 8 (15 mg/kg, 45 mg/kg ; i.g.; twice daily; for 7 days) ameliorates antigen-induced arthritis (AiA) responses in Lewis rats.
Products are for research use only. Not for human use.
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