2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor Immunology/Inflammation
  3. ROR Interleukin Related
  4. 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.

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RORγt inverse agonist 37

RORγt inverse agonist 37 Chemical Structure

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RORγt inverse agonist 37 Related Antibodies

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Description

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[1].

IC50 & Target[1]

RORγt

10.8 nM (IC50)

IL-17

 

IL-17A

 

In Vitro

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 Related Antibodies
Parmacokinetics
Species Dose Route T1/2 Tmax Cmax AUClast Vss CL F
Dog[1] 1 mg/kg i.v. 10.9 h 0.083 h 1540 ng/mL 6540 ng·h/mL 1.64 L/kg 2.07 mL/min/kg /
Dog[1] 5 mg/kg p.o. 17.2 h 2.67 h 871 ng/mL 12500 ng·h/mL / / 51 %
In Vivo

RORγt inverse agonist 37 (15-30 mg/kg; p.o.; administered once 16 h and 1 h prior to LPS challenge) dose-dependently inhibits LPS (HY-D1056)-induced IL-17 production in male BALB/c mice[1].
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.

Animal Model: BALB/c (male, SPF grade, 6-8 weeks old, LPS-induced IL-17 elevation model)[1]
Dosage: 15 mg/kg; 30 mg/kg
Administration: p.o.; twice at 16 h and 1 h prior to LPS challenge
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).
Animal Model: BALB/c (female, Imiquimod (HY-B0180)-induced skin inflammation model)[1]
Dosage: 30 mg/kg
Administration: p.o.; twice daily; 7 consecutive days
Result: Reduced ear weight compared to the vehicle-treated model group.
Reduced ear thickness compared to the vehicle-treated model group.
Molecular Weight

640.66

Formula

C31H33F5N2O5S
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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RORγt inverse agonist 37 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

RORγt inverse agonist 37RORγt inverse agonist37RORγt inverse agonist-37RORInterleukin RelatedRAR-related orphan receptorILRORγthuman liver microsomesCYP2D6HEK293T cellshERGBALB/c miceCYP2B6Caco-2 cellsmouse liver microsomeshPBMCsInhibitorinhibitorinhibit

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RORγt inverse agonist 37
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