RORγt inverse agonist 29
RORγt inverse agonist 29 is a potent, orally active and selective RORγt inverse agonist (IC50: 21 nM). RORγt inverse agonist 29 can be used in the research of skin inflammation and autoimmune diseases like psoriasis.
For research use only. We do not sell to patients.
- Formula: C25H24N2O5S
- Molecular Weight:464.53
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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
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RORγt 21 nM (IC50) |
RORγt inverse agonist 29 (compound b12) demonstrates high RORγt transcriptional inhibitory activity (IC50: 28 nM) in human Jurkat cells[1].
RORγt inverse agonist 29 (10 μM) shows good metabolic stabilities in in vitro human liver microsomes, with comparable half-life (T1/2: 4.46 h) and HLM (CLint(liver): 4.8 mL/min/kg)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
RORγt inverse agonist 29 (i.v., p.o., 0.3 or 1 mg/kg) displays an acceptable bioavailability and a half-life in rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mouse Imiquimod-induced skin inflammation model[1]
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Dosage:15 mg/kg, 50 mg/kg, 100 mg/kg
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Administration:Oral administration, twice a day for 13 days.
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Result:Inhibited IL-6 and IL-17A protein in the serum, with inhibition rate of 58.06% (IL-6) and 84.07% (IL-17A) at 100 mg/kg.
Reduced the histopathological symptoms on the back skin at dose of 100 mg/kg.
Alleviated symptoms including mononuclear and inflammatory cell infiltration, skin layer thickening, and dermal telangiectasia.
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Animal Model:Rats (pharmacokinetic assay)[1]
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Dosage:0.3 mg/kg (i.v.), 1 mg/kg (p.o.)
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Administration:Intravenous injection, oral administration
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Result:Pharmacokinetic profile of RORγt inverse agonist 29 (compound b12).
administration route T1/2 (h) Tmax (h) Cmax (ng/mL) AUC0-t (ng•h/mL) AUC0-∞ (ng•h/mL) F (%) i.v. (0.3 mg/kg) 5.8 2.4 88 156 162 p.o. (1 mg/kg) 6.5 3.1 105 340 352 65
Chemical Information
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Molecular Weight 464.53
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Formula C25H24N2O5S
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SMILES
CCS(=O)(C1=CN=C(C=C1)CC(NC2=CC3=C(C(CC(O3)CC4=CC=CC=C4)=O)C=C2)=O)=O
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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)
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