ABT-639

SKU: orb1303871

Description

ABT-639 is a selective small molecule inhibitor of T-type voltage-gated calcium channels. It is a valuable research tool for investigating the role of these channels in neurological disorders such as neuropathic pain and epilepsy, as demonstrated in various in vitro and in vivo preclinical studies.

Research Area

Metabolism Research, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1235560-28-7
• MW: 455.91
• Purity: 99.77% (May vary between batches)
• Formula: C₂₀H₂₀ClF₂N₃O₃S
• SMILES: [H][C@]12CCCN1CCN(C2)C(=O)c1cc(c(F)cc1Cl)S(=O)(=O)Nc1ccccc1F
• Target: Calcium Channel
• Solubility: DMSO:55 mg/mL (120.64 mM)

Bioactivity

• In Vivo:
  Following oral administration ABT-639 produces dose-dependent antinociception in a rat model of knee joint pain (ED50 = 2 mg/kg, p.o.). ABT-639 (10-100 mg/kg, p.o.) also increases tactile allodynia thresholds in multiple models of neuropathic pain. The antinociceptive profile of ABT-639 provides novel insights into the role of peripheral T-type (Cav3.2) channels in chronic pain states.
• In Vitro:
  ABT-639 is significantly less active at other Ca2+ channels (e.g. Cav1.2 and Cav2.2) (IC50 > 30 μM). ABT-639 has high oral bioavailability (%F = 73), low protein binding (88.9%) and a low brain:plasma ratio (0.05:1) in rodents.

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

CalciumChannel, ABT 639, ABT639, ABT-639, Calcium Channel, Ca2+ channels, Ca channels, inhibit, Inhibitor

Compound Identifiers

PubChem CID

46851313