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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-Potassium Channel-Dalazatide TFA
Dalazatide TFA

Chemical Structure : Dalazatide TFA

CAS No.:

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Dalazatide TFA (ShK-186 TFA, ShK186 TFA)

货号: PC-28406Not For Human Use, Lab Use Only.

Dalazatide TFA (ShK-186) is a potent, selective inhibitor of voltage-gated potassium channel Kv1.3 with IC50 of 69 pM, exhibits enhanced selectivity for Kv1.3 over Kv1.1, alleviates obesity and insulin resistance.

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5 mg ￥4980 In stock
10 mg ￥7580 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Dalazatide TFA (ShK-186) is a potent, selective inhibitor of voltage-gated potassium channel Kv1.3 with IC50 of 69 pM, exhibits enhanced selectivity for Kv1.3 over Kv1.1, alleviates obesity and insulin resistance.
Dalazatide (ShK-186) reduced weight gain, adiposity, and fatty liver; decreased blood levels of cholesterol, sugar, HbA1c, insulin, and leptin; and enhanced peripheral insulin sensitivity.
Dalazatide (ShK-186) activated brown adipose tissue as evidenced by a doubling of glucose uptake, and increased β-oxidation of fatty acids, glycolysis, fatty acid synthesis, and uncoupling protein 1 expression.
Dalazatide (ShK-186) caused profound alterations in energy and lipid metabolism in obesity diet induced Kv1.3 expression in the liver.

物理化学性质&存储条件

分子量 4442.10 (free acid)
分子式 C184H296N57O55PS7.xC2HF3O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

H-{pY}-{AEEA}-Arg-Ser-Cys-Ile-Asp-Thr-Ile-Pro-Lys-Ser-Arg-Cys-Thr-Ala-Phe-Gln-Cys-Lys-His-Ser-Met-Lys-Tyr-Arg-Leu-Ser-Phe-Cys-Arg-Lys-Thr-Cys-Gly-Thr-Cys-NH2 (disulfide bridge:Cys5-Cys37,Cys14-Cys30,Cys19-Cys34) (TFA salt)

参考文献

1. Victor Chi, et al. Toxicon. 2012 Mar 15;59(4):529-46.

2. Wen-Jun Zhen, et al. Eur J Med Chem. 2026 Sep 19:320:119310.

3. Upadhyay SK, et al. Proc Natl Acad Sci U S A. 2013 Jun 11;110(24):E2239-48.

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