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  3. RORγt inverse agonist 13

RORγt inverse agonist 13 

Cat. No.: HY-131338
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RORγt inverse agonist 13 (Compound 3i) is a potent, orally active and selective RORγt inverse agonist, with improved drug-like properties, with an IC50 of 63.8 nM.

For research use only. We do not sell to patients.

RORγt inverse agonist 13 Chemical Structure

RORγt inverse agonist 13 Chemical Structure

CAS No. : 2170477-75-3

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Description

RORγt inverse agonist 13 (Compound 3i) is a potent, orally active and selective RORγt inverse agonist, with improved drug-like properties, with an IC50 of 63.8 nM[1].

IC50 & Target[1]

ROR-γ

63.8 nM (IC50)

In Vitro

RORγt inverse agonist 13 (Compound 3i) exhibits activity with an inhibition of 76% at 0.3 µM in Th17 cell differentiation assay[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

RORγt inverse agonist 13 (Compound 3i, 25 mg/kg, Orally, twice daily) demonstrats excellent in vivo PK profile in mice and good in vivo efficacy in an IMQ-induced psoriasis mice model[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Imiquimod (IMQ)-induced psoriasis mice model[1].
Dosage: 25 mg/kg.
Administration: Orally, twice daily.
Result: Brought in a significant reduction in clinical severity of psoriasis as measured through the ear erythema, back skin erythema and scaliness scales.
Animal Model: Male CD-1 Mice[1].
Dosage: 1 mg/kg (i.v.) and 5 mg/kg (p.o.)(Pharmacokinetic Analysis).
Administration: IV or PO, single dose.
Result: Cmax: 609.67 ng/mL (PO), 1550 ng/mL (IV).
T1/2: 3.63 h (PO), 3.04 h (IV).
Molecular Weight

513.29

Formula

C₂₃H₁₇Cl₂F₃N₂O₄

CAS No.

2170477-75-3

SMILES

O=C(O)CC1=CC=C(CNC(NC2=CC(Cl)=C(C3=CC=CC=C3OC(F)(F)F)C(Cl)=C2)=O)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
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Keywords:

RORγt inverse agonist 13RORγt inverse agonist13RORγt inverse agonist-13RORRAR-related orphan receptorInhibitorinhibitorinhibit

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RORγt inverse agonist 13
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HY-131338
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