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  3. RORγt inverse agonist 14

RORγt inverse agonist 14 

Cat. No.: HY-132195
Handling Instructions

RORγt inverse agonist 14 (8e) is a potent, orally active and selective RORγt inverse agonist (EC50 of 2.5 nM) with anti-inflammatory activity. RORγt inverse agonist 14 is used in the study for rheumatoid arthritis and psoriasis.

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

RORγt inverse agonist 14 Chemical Structure

RORγt inverse agonist 14 Chemical Structure

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Description

RORγt inverse agonist 14 (8e) is a potent, orally active and selective RORγt inverse agonist (EC50 of 2.5 nM) with anti-inflammatory activity. RORγt inverse agonist 14 is used in the study for rheumatoid arthritis and psoriasis[1].

In Vivo

RORγt inverse agonist 14 (8e) exhibits t1/2 of 11 h by iv injection of 1 mg/kg. RORγt inverse agonist 14 (8e) exhibits tmax of 2 h, %F of 101 by oral administration of 4 mg/kg in mouse[1].
RORγt inverse agonist 14 (8e, 5-20 mg/kg) provides essentially the same arthritic score reduction as a murine equivalent of the marketed TNF decoy receptor etanercept[1].

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

Animal Model: Mouse model of psoriasis: acanthosis induced by IL-23[1].
Dosage: 5, 10, 20 mg/kg.
Administration: Orally twice daily.
Result: A dose-dependent reduction in ear thickening was observed.
Molecular Weight

678.61

Formula

C₂₆H₂₆F₈N₂O₆S₂

SMILES

O=C(N[[email protected]@H]1CC[[email protected]@]2(S(=O)(C3=CC=C(F)C=C3)=O)C4=C(N=C(C(C(F)(F)F)(F)C(F)(F)F)C=C4)CC[[email protected]]21[H])[[email protected]](C)(O)CS(=O)(C)=O

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Room temperature in continental US; may vary elsewhere.

Storage

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

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Keywords:

RORγt inverse agonist 14RORγt inverse agonist14RORγt inverse agonist-14RORRAR-related orphan receptorIL-17aIL-6LCN2rheumatoidarthritisTNFacanthosisInhibitorinhibitorinhibit

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Product Name:
RORγt inverse agonist 14
Cat. No.:
HY-132195
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