ABT-639

SKU: orb1226702

Description

ABT-639 is a novel, peripherally acting, selective T-type calcium channel blocker; blocks recombinant human Cav 3.2 in a voltage-dependent fashion (IC50=2 uM), attenuates LVA currents in rat DRG neurons (IC50=8 uM); less active at other Ca2+ channels (IC50> 30 uM); effectively reduces nociceptive and neuropathic pain in rats; high oral bioavailability.Pain Phase 2 Clinical(In Vivo):ABT-639 blocks recombinant human T-type (Cav3.2) Ca2+ channels in a voltage-dependent fashion (IC50=2 μM) and attenuates low voltage-activated (LVA) currents in rat DRG neurons (IC50=8 μM). ABT-639 is significantly less active at other Ca2+ channels (e.g. Cav1.2 and Cav2.2) (IC50>30 mM). ABT-639 has high oral bioavailability (%F=73), low protein binding (88.9%) and a low brain:plasma ratio (0.05:1) in rodents. 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 (e.g. spinal nerve ligation, CCI, and vincristine-induced, and capsaicin secondary hypersensitivity). ABT-639 does not attenuate hyperalgesia in inflammatory pain models induced by complete Freund’s adjuvant or carrageenan. At higher doses (e.g. 100-300 mg/kg) ABT-639 does not significantly alter hemodynamic or psychomotor function. The antinociceptive profile of ABT-639 provides novel insights into the role of peripheral T-type (Cav3.2) channels in chronic pain states.

Key Properties

• CAS Number: 1235560-28-7
• MW: 455.9059
• Purity: >98% (HPLC)
• Formula: C₂₀H₂₀ClF₂N₃O₃S
• SMILES: O=S(C1=CC(C(N2C[C@](CCC3)([H])N3CC2)=O)=C(Cl)C=C1F)(NC4=CC=CC=C4F)=O
• Target: Calcium Channel
• Solubility: DMSO: 10 mg/mL

Bioactivity

• In Vivo:
  ABT-639 blocks recombinant human T-type (Cav3.2) Ca2+ channels in a voltage-dependent fashion (IC50 = 2 μM) and attenuates low voltage-activated (LVA) currents in rat DRG neurons (IC50 = 8 μM). ABT-639 is significantly less active at other Ca2+ channels (e. g. Cav1.2 and Cav2.2) (IC50>30 mM). ABT-639 has high oral bioavailability (%F = 73), low protein binding (88.9%) and a low brain: plasma ratio (0.05: 1) in rodents. 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 (e. g. spinal nerve ligation, CCI, and vincristine-induced, and capsaicin secondary hypersensitivity). ABT-639 does not attenuate hyperalgesia in inflammatory pain models induced by complete Freund’s adjuvant or carrageenan. At higher doses (e. g. 100-300 mg/kg) ABT-639 does not significantly alter hemodynamic or psychomotor function. The antinociceptive profile of ABT-639 provides novel insights into the role of peripheral T-type (Cav3.2) channels in chronic pain states.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

ABT639 | ABT 639

Quick Database Links

Gene Symbol

Calcium Channel