RORγt inverse agonist 37
RORγt inverse agonist 37 is an orally active RORγt inverse agonist with an IC50 of 10.8 nM against human targets. RORγt inverse agonist 37 destabilizes helix 12 of RORγt in the agonist-bound conformation, thereby inhibiting transcriptional activity. RORγt inverse agonist 37 inhibits the secretion of IL-17 in cells and in LPS-induced systemic inflammation mouse models. RORγt inverse agonist 37 improves disease-related symptoms in mouse models of psoriasiform dermatitis. RORγt inverse agonist 37 can be used in research related to psoriasiform dermatitis and systemic inflammation.
For research use only. We do not sell to patients.
- CAS No.: 3134806-34-8
- Formula: C31H33F5N2O5S
- Molecular Weight:640.66
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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 10.8 nM (IC50) |
IL-17 |
IL-17A |
RORγt inverse agonist 37 (Compound 8v) inhibits RORγt reporter gene activity in HEK293T cells following 16 h treatment, with an IC50 of 45 nM[1].
RORγt inverse agonist 37 (5 days) potently inhibits IL-17A secretion in hPBMC, with an IC50 of 7.4 nM[1].
RORγt inverse agonist 37 inhibits IL-17 production in human whole blood with an IC50 of 30 nM[1].
RORγt inverse agonist 37 exhibits moderate oral absorption potential in Caco-2 cells[1].
RORγt inverse agonist 37 weakly inhibits CYP2D6 (IC50 = 14.9 μM) and CYP2B6 (IC50 = 17.7 μM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
RORγt inverse agonist 37 (30 mg/kg; p.o.; twice daily; for 7 consecutive days) improves psoriasis-like symptoms in female BALB/c mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (male, SPF grade, 6-8 weeks old, LPS-induced IL-17 elevation model)[1]
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Dosage:15 mg/kg; 30 mg/kg
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Administration:p.o.; twice at 16 h and 1 h prior to LPS challenge
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Result:Reduced plasma IL-17 concentration from 183 pg/mL (model control) to 95 pg/mL at 15 mg/kg dose.
Reduced plasma IL-17 concentration from 183 pg/mL (model control) to 57 pg/mL at 30 mg/kg dose.
Confirmed a significant linear dose-response trend (p < 0.001).
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Animal Model:BALB/c (female, Imiquimod (HY-B0180)-induced skin inflammation model)[1]
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Dosage:30 mg/kg
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Administration:p.o.; twice daily; 7 consecutive days
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Result:Reduced ear weight compared to the vehicle-treated model group.
Reduced ear thickness compared to the vehicle-treated model group.
Chemical Information
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CAS No. 3134806-34-8
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Molecular Weight 640.66
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Formula C31H33F5N2O5S
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SMILES
O=C(N[C@H](C1=CC=C(S(=O)(CC)=O)C=C1)CO)C2=CC=C(N3[C@H](COC(F)F)CC[C@H](C4=CC=C(C(F)(F)F)C=C4)C3)C=C2
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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 37 Related Classifications
HY-183763 Related Classifications
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