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Cat. No.: HY-132195

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RORγt inverse agonist 14

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.

CAS No.: 2672496-70-5
Formula: C₂₆H₂₆F₈N₂O₆S₂
Molecular Weight:678.61

Storage:

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

Data Sheet (273 KB)

RORγt inverse agonist 14 Chemical Structure

CAS No.: 2672496-70-5

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Sample (0.1mg)

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Bioz

Biological Activity

Description

All ROR Isoforms :

In Vivo

RORγt inverse agonist 14 (8e) exhibits t_1/2 of 11 h by iv injection of 1 mg/kg. RORγt inverse agonist 14 (8e) exhibits t_max 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].

MedChemExpress (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.

Chemical Information

CAS No. 2672496-70-5
Molecular Weight 678.61
Formula C₂₆H₂₆F₈N₂O₆S₂
SMILES

O=C(N[C@@H]1CC[C@@]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[C@]21[H])[C@](C)(O)CS(=O)(C)=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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Qingjie Liu, et al. Azatricyclic Inverse Agonists of RORγt That Demonstrate Efficacy in Models of Rheumatoid Arthritis and Psoriasis. ACS Med Chem Lett. 2021 Apr 30;12(5):827-835. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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