ABT-639

ABT-639 is a T-type calcium channel blocker. 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.Formal Name: 4-chloro-2-fluoro-N-(2-fluorophenyl)-5-[[(8aR)-hexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]carbonyl]-benzenesulfonamide. CAS Number: 1235560-28-7. Molecular Formula: C20H20ClF2N3O3S. Formula Weight: 455.9. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 14 mg/ml, DMF:PBS (pH 7.2) (1:20): 0.04 mg/ml, DMSO: 10 mg/ml, Ethanol: 0.5 mg/ml. SMILES: FC1=C(S(NC2=CC=CC=C2F)(=O)=O)C=C(C(N3CCN(CCC4)[C@@]4([H])C3)=O)C(Cl)=C1. InChi Code: InChI=1S/C20H20ClF2N3O3S/c21-15-11-17(23)19(30(28,29)24-18-6-2-1-5-16(18)22)10-14(15)20(27)26-9-8-25-7-3-4-13(25)12-26/h1-2,5-6,10-11,13,24H,3-4,7-9,12H2/t13-/m1/s1. InChi Key: AGPIHNZOZNKRGT-CYBMUJFWSA-N.