LKT Labs

Biochemicals for Life Science Research

ABT 639

Product ID A064766
Cas No. 1235560-28-7
Purity ≥99%
Product Unit SizeCostQuantityStock
5 mg $165.00 In stock
25 mg $450.00 In stock
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Description

ABT-639 is an orally bioavailable, CaV3.2 T-type calcium channel blocker with potential anti-hyperalgesic activity. Upon oral administration, ABT-639 selectively binds to and blocks the CaV3.2 isoform of the low voltage-gated T-type calcium channels located in peripheral sensory neurons. This prevents the influx of calcium ions into the cell upon membrane depolarization. The inhibition of both neuronal hyperexcitability and firing of nociceptive, peripheral sensory neurons induces an anti-nociceptive effect. The expression of the CaV3.2 T-type channels plays a key role in nociceptive and neuropathic pain.
NCI Thesaurus (NCIt)

Product Info

Cas No.

1235560-28-7
Purity

≥99%
Formula

C20H20ClF2N3O3S
Formula Wt.

455.9
IUPAC Name

5-[(8aR)-3,4,6,7,8,8a-hexahydro-1H-pyrrolo[1,2-a]pyrazine-2-carbonyl]-4-chloro-2-fluoro-N-(2-fluorophenyl)benzenesulfonamide
Synonym

ABT639

Shipping and Storage

Store Temp

-20°C
Ship Temp

Ambient

Downloads

Info Sheet

A064766 Info Sheet PDF

References

Zhang Q, Xia Z, Joshi S, et al. Optimization of ADME properties for sulfonamides leading to the discovery of a T-type calcium channel blocker, ABT-639. ACS Med Chem Lett. 2015 Apr 28;6(6):641-644. PMID: 26101566

Jarvis M, Scott V, McGaraughty S, et al. A peripherally acting, selective T-type calcium channel blocker, ABT-639, effectively reduces nociceptive and neuropathic pain in rats. Biochem Pharmacol. 2014 Jun 15;89(4):536-544. PMID: 24726441

Ziegler D, Duan W, An G, et al. A randomized double-blind, placebo-, and active-controlled study of T-type calcium channel blocker ABT-639 in patients with diabetic peripheral neuropathic pain. Pain. 2015 Oct;156(10):2013-2020. PMID: 26067585

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