Quality Segment
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
-10 to -25°C
SMILES string
Fc1c(cc(c(c1)Cl)C(=O)N3C[C@@H]4N(CC3)CCC4)[S](=O)(=O)Nc2c(cccc2)F
InChI key
AGPIHNZOZNKRGT-CYBMUJFWSA-N
Biochem/physiol Actions
Orally active, peripherally acting, potent and Cav3.2-selective T-type calcium channel blocker with antinociception efficacy in vivo.
ABT-639 is an orally active, peripherally acting, potent and Cav3.2-selective T-type calcium channel blocker (hCav3.2 IC50 = 2 μM vs. >30 μM against Cav3.1/Cav3.3) that attenuates low-voltage-activated (LVA) currents in rat DRG neurons (IC50 = 7.6 μM). ABT-639 exhibits antinociception efficacy in a rat knee joint pain model (ED50 = 2 mg/kg, p.o.), and increases tactile allodynia thresholds in multiple models of neuropathic pain in vivo (10-100 mg/kg, p.o.) with no adverse effects on hemodynamic or psychomotor function even at doses as high as 300 mg/kg.
ABT-639 is an orally active, peripherally acting, potent and Cav3.2-selective T-type calcium channel blocker (hCav3.2 IC50 = 2 μM vs. >30 μM against Cav3.1/Cav3.3) that attenuates low-voltage-activated (LVA) currents in rat DRG neurons (IC50 = 7.6 μM). ABT-639 exhibits antinociception efficacy in a rat knee joint pain model (ED50 = 2 mg/kg, p.o.), and increases tactile allodynia thresholds in multiple models of neuropathic pain in vivo (10-100 mg/kg, p.o.) with no adverse effects on hemodynamic or psychomotor function even at doses as high as 300 mg/kg.
signalword
Warning
hcodes
Hazard Classifications
Acute Tox. 4 Oral - Skin Irrit. 2
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable