- ABT-639
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- $30.00 / 2mg
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2025-11-10
- CAS:1235560-28-7
- Min. Order:
- Purity: 99.27%
- Supply Ability: 10g
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| | ABT-639 Basic information |
| Product Name: | ABT-639 | | Synonyms: | ABT-639;4-Chloro-2-fluoro-N-(2-fluorophenyl)-5-[[(8aR)-hexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]carbonyl]benzenesulfonamide;4-CHLORO-2-FLURO-N-(2-FLUOROPHENYL)-5-[(8AR)-HEXAHYDROPYRROLO[1,2-A]PYRAZIN-2(1H)-YLCARBONYL]BENZENESULFONAMIDE;ABT-639, CID 46851313;(R)-4-chloro-2-fluoro-N-(2-fluorophenyl)-5-(octahydropyrrolo[1,2-a]pyrazine-2-carbonyl)benzenesulfonamide;ABT-639 (ABT639;CS-2286;ABT-693 | | CAS: | 1235560-28-7 | | MF: | C20H20ClF2N3O3S | | MW: | 455.91 | | EINECS: | | | Product Categories: | | | Mol File: | 1235560-28-7.mol |  |
| | ABT-639 Chemical Properties |
| 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 |
| | ABT-639 Usage And Synthesis |
| 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 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. | | Uses | ABT-639 is a novel, peripherally acting, selective T-type Ca2+ channel blocker. | | 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[1]. | | IC 50 | T-type calcium channel | | 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.
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| | ABT-639 Preparation Products And Raw materials |
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