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

RORγt inverse agonist 29 Chemical Structure

RORγt inverse agonist 29 Chemical Structure

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RORγt inverse agonist 29 Related Antibodies

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Description

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[1].

IC50 & Target[1]

RORγt

21 nM (IC50)

In Vitro

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 Related Antibodies
In Vivo

RORγt inverse agonist 29 (p.o., 100 mg/kg) reduces the total Psoriasis Area and the development of clinical symptoms in mouse Imiquimod-induced skin inflammation model[1].
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.

Animal Model: Mouse Imiquimod-induced skin inflammation model[1]
Dosage: 15 mg/kg, 50 mg/kg, 100 mg/kg
Administration: Oral administration, twice a day for 13 days.
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.
Animal Model: Rats (pharmacokinetic assay)[1]
Dosage: 0.3 mg/kg (i.v.), 1 mg/kg (p.o.)
Administration: Intravenous injection, oral administration
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
Molecular Weight

464.53

Formula

C25H24N2O5S
SMILES

CCS(=O)(C1=CN=C(C=C1)CC(NC2=CC3=C(C(CC(O3)CC4=CC=CC=C4)=O)C=C2)=O)=O
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 29 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 29RORγt inverse agonist29RORγt inverse agonist-29RORRAR-related orphan receptorInverse agonistautoimmuneinflammationTh17 cellpsoriasisskin inflammationInhibitorinhibitorinhibit

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