ABT-639

CAS NO.：1235560-28-7
Empirical Formula: C20H20ClF2N3O3S
Molecular Weight: 455.91
MDL number: MFCD29924737
Update Date: 2024-11-01 18:44:47

What is ABT-639?

Description

ABT-639 is a selective T-type calcium channel blocker with efficacy in a wide range of preclinical models of nociceptive and neuropathic pain.ABT-639 produces robust antinociceptive activity in experimental pain models at doses that do not significantly alter psychomotor or hemodynamic function in the rat.

Description

ABT-639 is a T-type calcium channel blocker. It inhibits inactivated-state Ca_v3.2 channels with an IC₅₀ value of 2.3 μM and inactivated-state Ca_v3.1 and Ca_v3.3 channels by 50 and 39%, respectively, when used at a concentration of 10 μM. ABT-639 selectively inhibits inactivated-state T-type calcium currents over resting-state currents in rat dorsal root ganglion (DRG) neurons (IC₅₀s = 7.6 and >30 μM, respectively). It reverses the hind limb grip force deficit in a rat model of osteoarthritic pain induced by monoiodoacetic acid (MIA; ED₅₀ = 2 mg/kg). ABT-639 also increases the paw withdrawal threshold in rat spinal nerve ligation (SNL) and chronic constriction injury (CCI) models of neuropathic pain in a dose-dependent manner and attenuates cold allodynia in the CCI rat model when administered at doses greater than or equal to 3 mg/kg.

storage

Store at -20°C

References

Zhang, Q., et al. "Optimization of ADME Properties for Sulfonamides Leading to the Discovery of a T-Type Calcium Channel Blocker, ABT-639."Acs Medicinal Chemistry Letters6.6(2015):150429091057009.
Serra, J, et al. "Effects of a T-type calcium channel blocker, ABT-639, on spontaneous activity in C-nociceptors in patients with painful diabetic neuropathy: a randomized controlled trial. " Pain 156.11(2015):2175.
http://www.medkoo.com/products/6989

Properties of ABT-639

Boiling point:	612.2±65.0 °C(Predicted)
Density	1.51±0.1 g/cm3(Predicted)
storage temp.	Store at -20°C
solubility	DMSO:9.71(Max Conc. mg/mL);21.3(Max Conc. mM) DMF:14.0(Max Conc. mg/mL);30.71(Max Conc. mM) DMF:PBS (pH 7.2) (1:20):0.04(Max Conc. mg/mL);0.09(Max Conc. mM) Ethanol:0.5(Max Conc. mg/mL);1.1(Max Conc. mM)
form	A solid
pka	6.80±0.10(Predicted)
color	White to off-white