ADWX 1
目录号 : GC11315Kv1.3 channel blocker,potent and selective
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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.
Cas No. | SDF | ||
Canonical SMILES | CCC(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 |
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1 mg | 5 mg | 10 mg | |
1 mM | 0.2456 mL | 1.2279 mL | 2.4559 mL |
5 mM | 0.0491 mL | 0.2456 mL | 0.4912 mL |
10 mM | 0.0246 mL | 0.1228 mL | 0.2456 mL |
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给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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