A T-type calcium channel blocker; inhibits inactivated-state Cav3.2 channels (IC50 = 2.3 μM) and inactivated-state Cav3.1 and Cav3.3 channels by 50 and 39%

ABT-639 – 25 mg

Brand:
Cayman
CAS:
1235560-28-7
Storage:
-20
UN-No:
Non-Hazardous - /

ABT-639 is a T-type calcium channel blocker.{48606} It inhibits inactivated-state Cav3.2 channels with an IC50 value of 2.3 μM and inactivated-state Cav3.1 and Cav3.3 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.  

 

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Description

A T-type calcium channel blocker; inhibits inactivated-state Cav3.2 channels (IC50 = 2.3 μM) and inactivated-state Cav3.1 and Cav3.3 channels by 50 and 39%, respectively, at 10 μM; selectively inhibits inactivated-state T-type calcium currents over resting-state currents in rat DRG neurons (IC50s = 7.6 and >30 μM, respectively); reverses the hind limb grip force deficit in a rat model of MIA-induced osteoarthritic pain (ED50 = 2 mg/kg); dose-dependently increases the paw withdrawal threshold in rat SNL and CCI models of neuropathic pain; attenuates cold allodynia in the CCI rat model at ≥3 mg/kg

Formal name: 4-chloro-2-fluoro-N-(2-fluorophenyl)-5-[[(8aR)-hexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]carbonyl]-benzenesulfonamide

Synonyms: 

Molecular weight: 455.9

CAS: 1235560-28-7

Purity: ≥98%

Formulation: A solid

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