TrkA-IN-4

• CAT Number: I042382
• CAS Number: 3026111-74-7
• Molecular Formula: C27H21F3N4O5
• Molecular Weight: 538.47
• Purity: ≥95%
• Synonyms: acetyloxymethyl 5-[[3-(1-methylpyrazol-3-yl)-4-(trifluoromethyl)benzoyl]amino]-6-phenylpyridine-3-carboxylate
• InChI: InChI=1S/C27H21F3N4O5/c1-16(35)38-15-39-26(37)19-13-23(24(31-14-19)17-6-4-3-5-7-17)32-25(36)18-8-9-21(27(28,29)30)20(12-18)22-10-11-34(2)33-22/h3-14H,15H2,1-2H3,(H,32,36)
• InChIKey: FMICUWJKVYFTRQ-UHFFFAOYSA-N
• SMILES: CC(=O)OCOC(=O)C1=CC(=C(N=C1)C2=CC=CC=C2)NC(=O)C3=CC(=C(C=C3)C(F)(F)F)C4=NN(C=C4)C

TrkA-IN-4, a potent, orally active and allosteric TrkA inhibitor, is a proagent of TrkA-IN-3 (IC50=22.4 nM, HY-151948). TrkA-IN-4 exhibits potent antinociceptive effects[1].
TrkA-IN-4 (compound 39) demonstrates 65.1% and 46.3% of kinase inhibition towards TrkA at concentrations of 1 μM and 0.1 μM, respectively[1].
TrkA-IN-4 (compound 39) (0.9375-120 mg/kg; i.g.) exhibits stronger maximum antinociceptive effects 3 h after administration, with an ED50 of 7.836 mg/kg in hot plate testing on male mice[1].

Reference

[1]. Tang S, et, al. Design, development and evaluation of a prodrug-type TrkA-selective inhibitor with antinociceptive effects in vivo. Eur J Med Chem. 2023 Jan 5;245(Pt 2):114901.
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