TRPC4/5-IN-3

TRPC4/5-IN-3 (Compound 32) is the orally active inhibitor for transient receptor potential canonical channel 4/5 (TRPC4/5) with IC50 of 3.6 nM and 5.5 nM. TRPC4/5-IN-3 inhibits hERG channel with IC50 of 6.5 µM. TRPC4/5-IN-3 exhibits good metabolic stability in human/rat/mouse liver microsomes. TRPC4/5-IN-3 exhibits antidepressant and anxiolytic activity in mouse models, exhibits good pharmacokinetic characteristics in mouse with an oral bioavailability of 87%[1].

Product Specifications

CAS Number

[3053390-98-7]

UNSPSC

12352005

Target

TRP Channel

Related Pathways

Membrane Transporter/Ion Channel; Neuronal Signaling

Field of Research

Neurological Disease

Purity

99.65

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C1C2=C(N(C)C(N1CCCO)=O)N=C(C3(CCC(F)(CC3)F)F)N2CC4=CC=C(C=C4F)F

Molecular Formula

C22H23F5N4O3

Molecular Weight

486.44

References & Citations

[1]Song Z, et al., Property-Based Design of Xanthine Derivatives as Potent and Orally Available TRPC4/5 Inhibitors for Depression and Anxiety. J Med Chem. 2025 Feb 27;68 (4) :4694-4720.