GFB-8438, Selective TRPC5 inhibitor

Product Details

Formal Name: 4-Chloro-5-(3-oxo-4-[[2-(trifluoromethyl)phenyl]methyl]piperazin-1-yl)-2,3-dihydropyridazin-3-one

Molecular Formula: C₁₆H₁₄ClF₃N₄O₂

Formula Weight: 386.8

CAS Number: 2304549-73-1

Purity: >98%

Formulation: Powder

Solubility: Soluble in DMSO (at least 25 mg/ml)

Storage: -20°C

Stability: ≥ 2 years.

Applications

Selective TRPC5 inhibitor

Functions

Potent (IC₅₀ = 180 nM Qpatch and 280 nM whole cells) and selective inhibitor of TRPC4 and 5. It displayed excellent selectivity against other TRP family members as well as NaV1.5, 50 kinases and 87 other receptor targets along with good pharmacokinetic properties. GFB-8438 protected mouse podocytes from injury induced by protamine sulfate and demonstrated efficacy in a hypertensive DOCA-salt rat model suggesting potential therapeutic use for the treatment of chronic kidney disease.

Application Procedures

First dissolved in DMSO (25 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20°C for up to 3 months.

Research use only.

Documents

• Datasheet (PDF)
• MSDS (PDF)