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RORγt Inverse agonist 10 

Cat. No.: HY-133552
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RORγt Inverse agonist 10 is a potent and orally bioavailable RORγt (retinoic acid receptor-related orphan nuclear receptor gamma t) inverse agonist, with an IC50 of 51 nM. RORγt is a major transcription factor of genes related to psoriasis pathogenesis such as IL-17A, IL-22, and IL-23R

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RORγt Inverse agonist 10 Chemical Structure

RORγt Inverse agonist 10 Chemical Structure

CAS No. : 2413986-35-1

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Description

RORγt Inverse agonist 10 is a potent and orally bioavailable RORγt (retinoic acid receptor-related orphan nuclear receptor gamma t) inverse agonist, with an IC50 of 51 nM. RORγt is a major transcription factor of genes related to psoriasis pathogenesis such as IL-17A, IL-22, and IL-23R[1]

IC50 & Target[1]

RORγt

51 nM (IC50)

In Vitro

RORγt Inverse agonist 10 has a good liver microsome stability (human CLint=0.010 mL/min/mg, mouse CLint=0.030 mL/min/mg)[1].
RORγt Inverse agonist 10 suppresses the IL-17A production in a dose-dependent manner with an IC50 of 130 nM in a human whole-blood assay[1].

In Vivo

RORγt Inverse agonist 10 (3-100 mg/kg; p.o.) shows robust and dose-dependent inhibitory effect on the IL-17A production in mouse IL-18/23-induced cytokine expression model[1].
RORγt Inverse agonist 10 (1.145 mg/kg; p.o.) shows a high AUC of 15000 nM*h and t1/2 of 3.6 hours[1].

Animal Model: C57/BL6 male mice, mouse IL-18/23-induced cytokine expression model[1]
Dosage: 3 mg/kg, 10 mg/kg, 30 mg/kg, 100 mg/kg
Administration: Oral administration
Result: Significantly inhibited the IL-17A production in a dose-dependent manner.
Animal Model: Mice[1]
Dosage: 1.145 mg/kg (Pharmacokinetic Analysis)
Administration: Oral administration
Result: AUC=15000 nM*h, t1/2=3.6 hours.
Molecular Weight

572.50

Formula

C₂₅H₂₆F₆N₆O₃

CAS No.

2413986-35-1

SMILES

C[[email protected]](N(C(CC(C(F)(F)F)C(F)(F)F)=O)CC1)C[[email protected]]1OC2=C(C)C(NC(C3=CN=C(C)C=C3)=O)=CN4C2=NC=N4

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Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

RORγt Inverse agonist 10RORγt Inverse agonist10RORγt Inverse agonist-10RORRAR-related orphan receptorRORγtretinoicacidreceptor-relatedorphannuclearreceptorpathogenesisIL-17AIL-22IL-23RInhibitorinhibitorinhibit

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RORγt Inverse agonist 10
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HY-133552
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