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ADWX 1
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
ADWX 1图片
包装:100μg
市场价:4841元

Kv1.3 channel blocker,potent and selective
Canonical SMILESCCC(C(/N=C(O)/C/N=C(O)/C(N)C(C)C)/C(O)=N/C(/C(O)=N/C(/C(O)=N/C(/C(O)=N/C(/C(O)=N\C(/C(O)=N/C(/C(O)=N/C(/C(O)=N/C(/C(O)=N\C(/C(O)=N/C(C(O)=NC(C(O)=NC(C1=O)CCCCN)CC(C)C)CSSCC2/C(O)=N/C(/C(O)=N/C(/C(O)=N/C(C(N3CCCC3/C(O)=N/C(C(O)=O)CCCCN)=O)C(O)C)CSSCC(N=C(O
分子式C169H281N57O46S7
分子量4071.85
溶解度Soluble to 2 mg/ml in Water
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

ADWX 1 is a potent and selective inhibitor of KV1.3 channel with IC50 values of 1.89 pM and 0.65 nM for Kv1.3 and Kv1.1, respectively [1].

Potassium voltage-gated channel (KV1.3 channel) is a potassium channel and plays an important role in regulating Ca2+ signaling and the resting membrane potential. KV1.3 is an attractive target for immunomodulation of T cell-mediated autoimmune diseases [1].

ADWX 1 is a potent and selective KV1.3 channel inhibitor. In the transiently transfected HEK293 cells, ADWX-1 inhibited potassium channel with IC50 values of 1.89 pM and 0.65 nM for Kv1.3 and Kv1.1, respectively [1].

In a rat experimental autoimmune encephalomyelitis (EAE) model, ADWX-1 lowered the clinical scores and significantly reduced inflammatory infiltrates. Also, ADWX-1 reduced the levels of IL-2 and IFN-γ. In MBP-stimulated PBMCs from ADWX-1-treated EAE rats, IL-2 secretion was decreased significantly. In the EAE model, the CD4+CCR7- TEM cells were inhibited by ADWX-1. Also, ADWX-1 inhibited IL-2 secretion by CD4+CCR7- TEM cells through the NF-B- and NF-AT-dependent way [2].

References:
[1].  Han S, Yi H, Yin SJ, et al. Structural basis of a potent peptide inhibitor designed for Kv1.3 channel, a therapeutic target of autoimmune disease. J Biol Chem, 2008, 283(27): 19058-19065.
[2].  Li Z, Liu WH, Han S, et al. Selective inhibition of CCR7(-) effector memory T cell activation by a novel peptide targeting Kv1.3 channel in a rat experimental autoimmune encephalomyelitis model. J Biol Chem, 2012, 287(35): 29479-29494.

 
 
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