A T-type calcium channel blocker
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ABT-639

Item No. 28742

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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(Learn about Variance in Solubility)
DMF: 14 mg/mlDMF:PBS (pH 7.2) (1:20): 0.04 mg/mlDMSO: 10 mg/mlEthanol: 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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $49

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    5 mg

    $190

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    10 mg

    $283

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    25 mg

    $645

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    Product Description

    ABT-639 is a T-type calcium channel blocker.1 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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Jarvis, M.F., Scott, V.E., 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. 89(4), 536-544 (2014).