SML4099
ABT-639
≥98% (HPLC)
别名:
(R)-4-Chloro-2-fluoro-N-(2-fluorophenyl)-5-(octahydropyrrolo[1,2-a]pyrazine-2-carbonyl)benzenesulfonamide, 4-Chloro-2-fluoro-N-(2-fluorophenyl)-5-[(8aR)-hexahydropyrrolo[1,2-a]pyrazin-2(1H)-ylcarbonyl]benzenesulfonamide, ABT 639, ABT639
质量水平
方案
≥98% (HPLC)
表单
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
-10 to -25°C
SMILES字符串
Fc1c(cc(c(c1)Cl)C(=O)N3C[C@@H]4N(CC3)CCC4)[S](=O)(=O)Nc2c(cccc2)F
InChI key
AGPIHNZOZNKRGT-CYBMUJFWSA-N
生化/生理作用
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.
警示用语：
Warning
危险声明
危险分类
Acute Tox. 4 Oral - Skin Irrit. 2
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
此项目有
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
Elodie Picard et al.
British journal of pharmacology, 176(7), 950-963 (2019-02-05)
Abdominal pain associated with low-grade inflammation is frequently encountered in irritable bowel syndrome (IBS) and inflammatory bowel disease (IBD) during remission. Current treatments are not very effective and new therapeutic approaches are needed. The role of CaV 3.2 channels, which
Qingwei Zhang et al.
ACS medicinal chemistry letters, 6(6), 641-644 (2015-06-24)
The discovery of a novel peripherally acting and selective Cav3.2 T-type calcium channel blocker, ABT-639, is described. HTS hits 1 and 2, which have poor metabolic stability, were optimized to obtain 4, which has improved stability and oral bioavailability. Modification
Michael F Jarvis et al.
Biochemical pharmacology, 89(4), 536-544 (2014-04-15)
Activation of T-type Ca²⁺ channels contributes to nociceptive signaling by facilitating action potential bursting and modulation of membrane potentials during periods of neuronal hyperexcitability. The role of T-type Ca²⁺ channels in chronic pain is supported by gene knockdown studies showing
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