SML2665

AGN194310

≥98% (HPLC)

• Synonym(e): 4-[2-[4-(4-Ethylphenyl)-2,2-dimethyl-2H-1-benzothiopyran-6-yl]ethynyl]benzoic acid, 4-[[4-(4-Ethylphenyl)-2,2-dimethyl-2H-1-benzothiopyran-6-yl]ethynyl]benzoic acid, AGN 194310, AGN-194310, IRX4310, VTP 194310
• Empirische Formel (Hill-System): C₂₈H₂₄O₂S
• CAS-Nummer: 229961-45-9
• Molekulargewicht: 424.55
• UNSPSC-Code: 12352200
• NACRES: NA.77

Eigenschaften

• Assay: ≥98% (HPLC)
• Form: powder
• Farbe: white to beige
• Löslichkeit: DMSO: 2 mg/mL, clear
• Lagertemp.: 2-8°C
• SMILES String: O=C(O)C1=CC=C(C#CC2=CC3=C(SC(C)(C=C3C4=CC=C(CC)C=C4)C)C=C2)C=C1
• InChI: 1S/C28H24O2S/c1-4-19-7-12-22(13-8-19)25-18-28(2,3)31-26-16-11-21(17-24(25)26)6-5-20-9-14-23(15-10-20)27(29)30/h7-18H,4H2,1-3H3,(H,29,30)
• InChIKey: LHUPKWKWYWOMSK-UHFFFAOYSA-N

Beschreibung

Biochem./physiol. Wirkung

AGN194310 (IRX4310; VTP 194310) is a retinoic acid receptor (RAR) antagonist that targets all three RAR subtypes with higher affinity (RARα/β/γ K_d = 3/2/5 nM) than all-trans retinoic acid/ATRA (RARα/β/γ K_d = 15/13/18 nM) without affecting RXR subtypes. AGN194310 effectively blocks RAR agonist TTNPB-induced transcription activity (using RARα, RARβ, or RARγ transfected cells) and prevents TTNPB toxicity in guinea pigs in vivo (by 79/84/94% at AGN194310/TTNPB ratios of 0.5/2/8). AGN194310 potentiates differentiation in osteoblast cultures (1 μM) and daily oral administration (0.5 mg/kg/d for a10-d period) is reported to cause impaired radial bone growth among 8-wk-old mice.

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable