GFB-8438

SKU: orb1309631

Description

GFB-8438 is a potent, subtype-selective TRPC5 inhibitor with IC50 values of 0.18 µM (hTRPC5) and 0.29 µM (hTRPC4). This compound is a valuable research tool for studying TRPC channel function in neurological and renal disease models, both in vitro and in vivo.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 2304549-73-1
• MW: 386.76
• Purity: 99.58% (May vary between batches)
• Formula: C₁₆H₁₄ClF₃N₄O₂
• SMILES: FC(F)(F)c1ccccc1CN1CCN(CC1=O)c1cn[nH]c(=O)c1Cl
• Target: TRP/TRPV Channel
• Solubility: DMSO:27.5 mg/mL (71.1 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.17 mM)

Bioactivity

• Target IC50:
  TRPC4 (human):0.29 μM |TRPC5 (human):0.18 μM|TRPC5 (rat):0.18 μM
• In Vivo:
  GFB-8438is also efficacious in a hypertensive deoxycorticosterone acetate (DOCA)-salt rat model of FSGS, significantly reducing both total protein and albumin concentrations in urine
• In Vitro:
  GFB-8438 is a novel TRPC5 inhibitor. GFB-8438 protects mouse podocytes from injury induced by protamine sulfate (PS) in vitro.
• Animal Research:
  Sprague Dawley rats (DOCA-salt rat model of FSGS);30 mg/kg; Administration:s.c.; daily for 3 weeks

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

acetate, deoxycorticosterone, disease, cytoskeletal, GFB 8438, GFB8438, GFB-8438, hTRPC4, hTRPC5, Inhibitor, loss, kidney, mouse, inhibit, subtype, synaptopodin, remodeling, rTRPC5, selective, podocytes, Transient receptor potential channels, TRPV Channel, TRPVChannel, TRPC5, TRPChannel, TRP Channel

Compound Identifiers

PubChem CID

138471783