ABT-639 - CAS 1235560-28-7
Catalog number: B0084-474418
Category: Inhibitor
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Molecular Formula:
C20H20ClF2N3O3S
Molecular Weight:
455.91
COA:
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Targets:
Calcium Channel
Description:
ABT-639, a new blocker of selective T-type Ca2+ channel blocker, has been found to have potential effect against neuropathic and nociceptive pain in studies. It has already been discontinued in the treatment of diabetic neuropathies.
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-474418 300 mg $688 In stock
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Purity:
98%
Appearance:
Powder
Synonyms:
ABT-639; ABT 639; ABT-639 free base; UNII-0G7D0CQ88I; SCHEMBL400073; 0G7D0CQ88I
Solubility:
DMSO: ≥ 10 mg/mL
Storage:
-20ºC Freeze
MSDS:
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Application:
ABT-639 is a new blocker of selective T-type Ca2+ channel blocker that has been found to have potential effect against neuropathic and nociceptive pain in studies.
Shelf Life:
As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly
Quantity:
Milligrams-Grams
InChIKey:
AGPIHNZOZNKRGT-CYBMUJFWSA-N
InChI:
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
Canonical SMILES:
C1CC2CN(CCN2C1)C(=O)C3=CC(=C(C=C3Cl)F)S(=O)(=O)NC4=CC=CC=C4F
1.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.
Serra J;Duan WR;Locke C;Solà R;Liu W;Nothaft W Pain. 2015 Nov;156(11):2175-83. doi: 10.1097/j.pain.0000000000000249.
T-type calcium channels are a potential novel target for treatment of neuropathic pain such as painful diabetic neuropathy. ABT-639 is a peripherally acting highly selective T-type Ca(v)3.2 calcium channel blocker that has demonstrated analgesic efficacy in preclinical models and may have the potential to reduce spontaneous fiber activity. Microneurography is a unique technique that directly assesses the function of peripheral sensory afferents and measures abnormal spontaneous activity in single peripheral nociceptive C fibers. Abnormal spontaneous activity in C-nociceptors functions as a marker for spontaneous pain, as reduction of this activity could indicate analgesic efficacy. This randomized, double-blind controlled study evaluated the effects of a single 100-mg oral dose of ABT-639, compared with placebo, on abnormal spontaneous activity in peripheral C-nociceptors, measured for the first time by microneurography in adult patients with painful diabetic neuropathy. Lidocaine was included in this study and compared with placebo. Pharmacokinetics and safety of ABT-639 were evaluated. Thirty-nine patients were randomized, and a total of 56 analyzable C-nociceptors with spontaneous activity were identified in 34 patients.
2.A randomized double-blind, placebo-, and active-controlled study of T-type calcium channel blocker ABT-639 in patients with diabetic peripheral neuropathic pain.
Ziegler D;Duan WR;An G;Thomas JW;Nothaft W Pain. 2015 Oct;156(10):2013-20. doi: 10.1097/j.pain.0000000000000263.
T-type Cav3.2 calcium channels represent a novel target for neuropathic pain modulation. Preclinical studies with ABT-639, a peripherally acting highly selective T-type Cav3.2 calcium channel blocker, showed dose-dependent reduction of pain in multiple pain models. ABT-639 also demonstrated an acceptable safety profile at single- and multiple-dose levels evaluated in a clinical phase 1 study in healthy volunteers. The primary objective of this phase 2, multicenter, randomized, double-blind, placebo-controlled, and active-controlled study was to compare the analgesic efficacy and safety of ABT-639 with placebo in the treatment of diabetic neuropathic pain. Pregabalin, an approved treatment for painful diabetic neuropathy, was included as a positive control. A total of 194 patients were randomized and treated for 6 weeks; 62 patients received ABT-639 (100 mg twice daily), 70 patients received pregabalin (150 mg twice daily), and 62 patients received placebo. When assessing the mean changes from baseline in patient-recorded pain scores at the end of week 6, there was no significant difference observed for ABT-639 compared with placebo (-2.28 vs -2.36; P = 0.582). Pregabalin treatment resulted in a transient improvement in pain compared with placebo, which did not persist throughout the study.
3.A peripherally acting, selective T-type calcium channel blocker, ABT-639, effectively reduces nociceptive and neuropathic pain in rats.
Jarvis MF;Scott VE;McGaraughty S;Chu KL;Xu J;Niforatos W;Milicic I;Joshi S;Zhang Q;Xia Z Biochem Pharmacol. 2014 Jun 15;89(4):536-44. doi: 10.1016/j.bcp.2014.03.015. Epub 2014 Apr 12.
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 that decreased Ca(v)3.2 channel expression results in the loss of low voltage-activated (LVA) currents in dorsal root ganglion (DRG) neurons and attenuation of neuropathic pain in the chronic constriction injury (CCI) model. ABT-639 is a novel, peripherally acting, selective T-type Ca²⁺ channel blocker. ABT-639 blocks recombinant human T-type (Ca(v)3.2) Ca²⁺ channels in a voltage-dependent fashion (IC₅₀ = 2 μM) and attenuates LVA currents in rat DRG neurons (IC₅₀ = 8 μM). ABT-639 was significantly less active at other Ca²⁺ channels (e.g. Ca(v)1.2 and Ca(v)2.2) (IC₅₀ > 30 μM). 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 produced 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 increased tactile allodynia thresholds in multiple models of neuropathic pain (e.
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CAS 1235560-28-7 ABT-639

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