RORγt Inverse agonist 6 (compound 43) is a RORγt inverse agonist for the study of Th17-driven autoimmune diseases. RORγt Inverse agonist 6 (compound 43) suppresses IL-17A gene expression by IL-23 stimulation in vivo.

Product information

CAS Number: 1887161-80-9

Molecular Weight: 565.02

Formula: C28H29ClN6O5

Chemical Name: 6-({2-[(3-chloro-4-cyanophenyl)carbamoyl]morpholine-4-carbonyl}amino)-3-(cyclopropylmethyl)-2,4-dioxo-1-(propan-2-yl)-2,3,4,4a-tetrahydroquinazolin-1-ium

Smiles: CC(C)[N+]1C(=O)N(CC2CC2)C(=O)C2C=C(C=CC=12)NC(=O)N1C[C](OCC1)C(=O)NC1=CC=C(C#N)C(Cl)=C1 |^1:24|

InChiKey: VAOORWQRURJBNP-UHFFFAOYSA-O

InChi: InChI=1S/C28H28ClN6O5/c1-16(2)35-23-8-7-19(11-21(23)26(37)34(28(35)39)14-17-3-4-17)32-27(38)33-9-10-40-24(15-33)25(36)31-20-6-5-18(13-30)22(29)12-20/h5-8,11-12,16-17,21H,3-4,9-10,14-15H2,1-2H3,(H-,31,32,36,38)/p+1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 50 mg/mL (88.49 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vivo:

RORγt Inverse agonist 6 (compound 43) suppresses IL-17A gene expression by IL-23 stimulation in a mouse pharmacodynamics model. RORγt Inverse agonist 6 (compound 43) exhibits improved drug exposure (mouse AUC: 1289 ng•h/mL at 1 mg/kg, po). RORγt Inverse agonist 6 (compound 43, 30 mg/kg, po, b.i.d) inhibits the expression level of IL-17A by 59% compared to the vehicle after the oral administration at the tested dose.

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