1. Membrane Transporter/Ion Channel
  2. Calcium Channel

ABT-639 

Cat. No.: HY-19721 Purity: 99.15%
Handling Instructions

ABT-639 is a novel, peripherally acting, selective T-type Ca2+ channel blocker.

For research use only. We do not sell to patients.

ABT-639 Chemical Structure

ABT-639 Chemical Structure

CAS No. : 1235560-28-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 421 In-stock
Estimated Time of Arrival: December 31
1 mg USD 180 In-stock
Estimated Time of Arrival: December 31
5 mg USD 420 In-stock
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2520 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Description

ABT-639 is a novel, peripherally acting, selective T-type Ca2+ channel blocker.

IC50 & Target

Ca2+ Channel[1]

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].

Clinical Trial
Solvent & Solubility
In Vitro: 

DMSO : 10 mg/mL (21.93 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1934 mL 10.9671 mL 21.9342 mL
5 mM 0.4387 mL 2.1934 mL 4.3868 mL
10 mM 0.2193 mL 1.0967 mL 2.1934 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[1]

Rats[1]
The pharmacokinetic properties are determined in Sprague Dawley rats dosed intravenously with 5 μmol/kg ABT-639 prepared in 10% DMSO/90% poly ethylene glycol 400 (PEG400). The plasma levels of ABT-639 are determined using HPLC and mass spectrometry. Following oral administration (p.o.) of the ABT-639 (3, 10 and 30 mg/kg) prepared in 10% PEG400/10% Cremophor EL/80% Oleic Acid the levels of ABT-639 in plasma and brain are determined. Briefly, the brains are immediately removed and freed from blood vessels as much as possible. The resulting brain tissues are frozen at -20°C, followed by weighing and homogenization before analysis. The heparinized blood samples are also frozen (-20°C) until analysis. ABT-639 is separated from the blood and brain samples using protein precipitation with acetonitrile followed by quantification with liquid chromatography/mass spectroscopy. Plasma samples for concentration determinations from in vivo efficacy experiments are collected from each animal within 15 min following behavioral testing.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

455.91

Formula

C₂₀H₂₀ClF₂N₃O₃S

CAS No.

1235560-28-7

SMILES

O=S(C1=CC(C(N2C[[email protected]](CCC3)([H])N3CC2)=O)=C(Cl)C=C1F)(NC4=CC=CC=C4F)=O

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
ABT-639
Cat. No.:
HY-19721
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ABT-639

Cat. No.: HY-19721