TRPV4 agonist-1 free base

• CAT Number: I019464
• CAS Number: 2314467-59-7
• Molecular Formula: C25H22F2N4O2
• Molecular Weight: 448.46
• Purity: ≥95%
• Synonyms: 8-fluoro-3-[4-(4-fluorophenoxy)phenyl]-2-(4-methylpiperazin-1-yl)quinazolin-4-one
• InChI: InChI=1S/C25H22F2N4O2/c1-29-13-15-30(16-14-29)25-28-23-21(3-2-4-22(23)27)24(32)31(25)18-7-11-20(12-8-18)33-19-9-5-17(26)6-10-19/h2-12H,13-16H2,1H3
• InChIKey: NUGPMKZYSBKNPU-UHFFFAOYSA-N
• SMILES: CN1CCN(CC1)C2=NC3=C(C=CC=C3F)C(=O)N2C4=CC=C(C=C4)OC5=CC=C(C=C5)F

TRPV4 agonist-1 free base is a transient receptor potential vanilloid 4 (TRPV4) agonist with an EC50 of 60 nM in the hTRPV4 Ca2+ assay[1].
TRPV4 agonist-1 (Compound 36) exhibits significantly increased potency (ECmax: 20 nM in the SOX9 reporter assay). TRPV4 agonist-1 is inactive against TRPV1 channels[1].

Reference

[1]. Atobe M, et al. Discovery of Novel Transient Receptor Potential Vanilloid 4 (TRPV4) Agonists as Regulators of Chondrogenic Differentiation: Identification of Quinazolin-4(3 H)-ones and in Vivo Studies on a Surgically Induced Rat Model of Osteoarthritis. J Med Chem. 2019 Jan 28.
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