| ADWX 1Kv1.3 channel blocker,potent and selective |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
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- Purity = 98.00%
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Chemical structure
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| Cas No. | SDF | Download 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)=NC(/C(O)=N/C(/C(O)=N/C(/C(O)=N/C(/C(O)=NC(/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 | ||
| Formula | C169H281N57O46S7 | M.Wt | 4071.85 |
| Solubility | Soluble to 2 mg/ml in H2O | Storage | Store at -20°C |
| Physical Appearance | White lyophilised solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
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.
