JNJ-28583113

SKU: orb1982627

Description

JNJ-28583113 is a brain-penetrant TRPM2 antagonist that promotes GSK3α/β phosphorylation, conferring protection against oxidative stress-induced cell death. It suppresses pro-inflammatory microglial activation, making it a valuable tool for in vitro and in vivo research in neurodegenerative and neuroinflammatory disease models.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 2765255-93-2
• MW: 366.38
• Purity: 98.57%
• Formula: C₁₉H₂₁F₃N₂O₂
• SMILES: O=C(OCC)CN1N=C(C=2C=CC(=CC2)C(F)(F)F)C3=C1CCCCC3
• Target: TRP/TRPV Channel
• Solubility: DMSO:80 mg/mL (218.35 mM)

Bioactivity

• Target IC50:
  TRPM2 (human):126 nM|TRPM2 (rat):25 nM
• In Vivo:
  JNJ-28583113 (10 mg/kg, injected subcutaneously) is brain permeable, reaches 400 ng/ml in the brain compartment, and is rapidly metabolized in plasma.
• In Vitro:
  JNJ-28583113 is a potent TRPM2 antagonist, blocking TRPM2 leads to phosphorylation of GSK3α and β subunits. JNJ-28583113 blocks TRPM2 in chimpanzees, rats, and humans with IC50 values of 100 nM, 25 nM, and 126 nM, respectively.

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

JNJ28583113

Compound Identifiers

PubChem CID

164628567