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ABT-639

Product Name
ABT-639
CAS No.
1235560-28-7
Chemical Name
ABT-639
Synonyms
ABT-639;ABT-693;CS-2286;ABT-639 (ABT639;ABT-639, CID 46851313;Calcium Channel,Ca channels,Ca2+ channels,inhibit,Inhibitor,ABT639,ABT-639;(R)-4-chloro-2-fluoro-N-(2-fluorophenyl)-5-(octahydropyrrolo[1,2-a]pyrazine-2-carbonyl)benzenesulfonamide;4-CHLORO-2-FLURO-N-(2-FLUOROPHENYL)-5-[(8AR)-HEXAHYDROPYRROLO[1,2-A]PYRAZIN-2(1H)-YLCARBONYL]BENZENESULFONAMIDE;4-Chloro-2-fluoro-N-(2-fluorophenyl)-5-[[(8aR)-hexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]carbonyl]benzenesulfonamide;Benzenesulfonamide, 4-chloro-2-fluoro-N-(2-fluorophenyl)-5-[[(8aR)-hexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]carbonyl]-
CBNumber
CB93121075
Molecular Formula
C20H20ClF2N3O3S
Formula Weight
455.91
MOL File
1235560-28-7.mol
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ABT-639 Property

Boiling point:
612.2±65.0 °C(Predicted)
Density 
1.51±0.1 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
DMSO:9.71(Max Conc. mg/mL);21.3(Max Conc. mM)
DMF:14.0(Max Conc. mg/mL);30.71(Max Conc. mM)
DMF:PBS (pH 7.2) (1:20):0.04(Max Conc. mg/mL);0.09(Max Conc. mM)
Ethanol:0.5(Max Conc. mg/mL);1.1(Max Conc. mM)
form 
A solid
pka
6.80±0.10(Predicted)
color 
White to off-white
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Cayman Chemical
Product number
28742
Product name
ABT-639
Packaging
1mg
Price
$44
Updated
2024/03/01
Cayman Chemical
Product number
28742
Product name
ABT-639
Packaging
25mg
Price
$586
Updated
2024/03/01
Cayman Chemical
Product number
28742
Product name
ABT-639
Packaging
5mg
Price
$172
Updated
2024/03/01
Cayman Chemical
Product number
28742
Product name
ABT-639
Packaging
10mg
Price
$257
Updated
2024/03/01
Tocris
Product number
6770
Product name
ABT639
Purity
≥98%(HPLC)
Packaging
10
Price
$220
Updated
2021/12/16
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ABT-639 Chemical Properties,Usage,Production

Description

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

Description

ABT-639 is a selective T-type calcium channel blocker with efficacy in a wide range of preclinical models of nociceptive and neuropathic pain.ABT-639 produces robust antinociceptive activity in experimental pain models at doses that do not significantly alter psychomotor or hemodynamic function in the rat.

Uses

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

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].

IC 50

T-type calcium channel

storage

Store at -20°C

References

Zhang, Q., et al. "Optimization of ADME Properties for Sulfonamides Leading to the Discovery of a T-Type Calcium Channel Blocker, ABT-639."Acs Medicinal Chemistry Letters6.6(2015):150429091057009.
Serra, J, et al. "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. " Pain 156.11(2015):2175.
http://www.medkoo.com/products/6989

ABT-639 Preparation Products And Raw materials

Raw materials

Preparation Products

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ABT-639 Suppliers

China 72 United States 9 Global 81
Shanghai Boyle Chemical Co., Ltd.
Tel
Fax
86-21-57758967
Email
sales@boylechem.com
Country
China
ProdList
2922
Advantage
55
Haoyuan Chemexpress Co., Ltd.
Tel
021-58950125
Fax
(86) 21-58955996
Email
info@chemexpress.com
Country
China
ProdList
7552
Advantage
61
HangZhou YuHao Chemical Technology Co., Ltd.
Tel
0571-82693216
Fax
0571-82880190
Email
info@yuhaochemical.com
Country
China
ProdList
2028
Advantage
58
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696，15000506266 15000506266
Fax
+86-21-52996696
Country
China
ProdList
4757
Advantage
55
Shanghaizehan biopharma technology co., Ltd.
Tel
021-61350663 13052117465
Fax
021-61350662
Email
sales@zehanbiopharma.com
Country
China
ProdList
984
Advantage
55
Shanghai YuanYe Biotechnology Co., Ltd.
Tel
021-61312847; 18021002903
Fax
QQ:3008007432
Email
3008007409@qq.com
Country
China
ProdList
71826
Advantage
60
ShangHai Biochempartner Co.,Ltd
Tel
177-54423994 17754423994
Fax
QQ:2853530913
Email
2853530910@QQ.com
Country
China
ProdList
8000
Advantage
62
Shanghai Rechem science Co., Ltd.
Tel
021-31433387 15618786686
Fax
QQ:1369748377
Email
sales@rechemscience.com
Country
China
ProdList
2989
Advantage
58
Shanghai Chaolan Chemical Technology Center
Tel
021-QQ：65489617 15618227136
Fax
21-5161 9052
Email
Sales@ATKchemical.com
Country
China
ProdList
9126
Advantage
58
Amadis Chemical Company Limited
Tel
571-89925085
Fax
0086-571-89925065
Email
sales@amadischem.com
Country
China
ProdList
131957
Advantage
58
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View Lastest Price from ABT-639 manufacturers

Career Henan Chemical Co
Product
4-Chloro-2-fluoro-N-(2-fluorophenyl)-5-[(8aR)-hexahydropyrrolo[1,2-a]pyrazin-2(1H)-ylcarbonyl]benzenesulfonamide 1235560-28-7
Price
US $1.00/KG
Min. Order
1g
Purity
Min98% HPLC
Supply Ability
g/kg /ton
Release date
2019-12-20

1235560-28-7, ABT-639Related Search:

CC-223

  • ABT-639
  • 4-Chloro-2-fluoro-N-(2-fluorophenyl)-5-[[(8aR)-hexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]carbonyl]benzenesulfonamide
  • 4-CHLORO-2-FLURO-N-(2-FLUOROPHENYL)-5-[(8AR)-HEXAHYDROPYRROLO[1,2-A]PYRAZIN-2(1H)-YLCARBONYL]BENZENESULFONAMIDE
  • ABT-639, CID 46851313
  • (R)-4-chloro-2-fluoro-N-(2-fluorophenyl)-5-(octahydropyrrolo[1,2-a]pyrazine-2-carbonyl)benzenesulfonamide
  • ABT-639 (ABT639
  • CS-2286
  • ABT-693
  • Benzenesulfonamide, 4-chloro-2-fluoro-N-(2-fluorophenyl)-5-[[(8aR)-hexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]carbonyl]-
  • Calcium Channel,Ca channels,Ca2+ channels,inhibit,Inhibitor,ABT639,ABT-639
  • 1235560-28-7
  • C20H20ClF2N3O3S