AGN 194078 is a selective RARα agonist with a Kd and EC50 of 3 and 112 nM, respectively.

Product information

CAS Number: 321995-62-4

Molecular Weight: 403.42

Formula: C22H23F2NO4

Chemical Name: 2,6-difluoro-4-(3-hydroxy-5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalene-2-amido)benzoic acid

Smiles: CC1(C)CCC(C)(C)C2=CC(C(=O)NC3=CC(F)=C(C(F)=C3)C(O)=O)=C(O)C=C12

InChiKey: BCKLKOYFMACAMZ-UHFFFAOYSA-N

InChi: InChI=1S/C22H23F2NO4/c1-21(2)5-6-22(3,4)14-10-17(26)12(9-13(14)21)19(27)25-11-7-15(23)18(20(28)29)16(24)8-11/h7-10,26H,5-6H2,1-4H3,(H,25,27)(H,28,29)

Technical Data

Appearance: Solid Power

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

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 Vitro:

AGN 194078 is a selective RARα agonist and binds to RARα with very high affinity, having a Kd value of 3 nM, while being unable to bind to RARβ and binding only very weakly (Kd=5600 nM) to RARγ. Furthermore, AGN 194078 maintains full transcriptional activity through RARα, with an EC50 value of 112 nM, but only activatedRARβ and RARγ with about 10% efficacy at the highest dose (1000 nM) tested.

Products are for research use only. Not for human use.