RORγt Inverse agonist 8
RORγt Inverse agonist 8 is a potent, selective, orally bioavailable RORγt inverse agonist, with an IC50 of 19 nM for human RORγt-LBD.
For research use only. We do not sell to patients.
- CAS No.: 2079892-79-6
- Formula: C26H33N7O2
- Molecular Weight:475.59
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
IC50: 19 nM (RORγt)[1]
RORγt Inverse agonist 8 (Cpd 1) is a potent RORγt inhibitor and binds to the ligand binding domain (LBD) of RORγt[1].
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[1].
RORγt Inverse agonist 8 selectively suppresses human Th17 and Tc17 cell differentiation[1].
RORγt Inverse agonist 8 polarizes Th17 cells also blocks IL-17A production in a concentration-dependent manner with an IC50 of 92 nM[1].
RORγt Inverse agonist 8 reduces Th17 cell-associated mRNA expression including IL17A, IL17F, IL26, IL23R and CCR6 in a concentration-dependent fashion[1].
RORγt Inverse agonist 8 alters epigenetic regulation at the IL17A and IL23R gene promoters without impairing the DNA binding activity of RORγt[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female Lewis rats (190–220 g)[1]
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Dosage:15 mg/kg, 45 mg/kg
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Administration:Oral gavage; twice daily; for 7 days
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Result:Ameliorates antigen-induced arthritis (AiA) responses in Lewis rats.
Chemical Information
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CAS No. 2079892-79-6
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Molecular Weight 475.59
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Formula C26H33N7O2
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SMILES
O=C(C1=CN=C(C)N=C1)NC2=CN3C(C(CN4C[C@H](C)N(C(C5CCCC5)=O)CC4)=C2C)=NC=C3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
RORγt Inverse agonist 8 Related Classifications
HY-122737 Related Classifications
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