Dalazatide (ShK-186) 是一种特异性的Kv1.3钾通道肽抑制剂。Dalazatide 可用于自身免疫性疾病，如多发性硬化症 (MS)、红斑狼疮、银屑病、类风湿性关节炎、1 型糖尿病和炎症性肠病的研究。
| 生物活性 | Dalazatide (ShK-186) is a specificKv1.3potassium channelpeptide inhibitor. Dalazatide can be used in the study of autoimmune diseases such as multiple sclerosis (MS), lupus erythematosus, psoriasis, rheumatoid arthritis, type 1 diabetes and inflammatory bowel disease[1][2][3]. |
体外研究
(In Vitro) | Dalazatide (ShK-186) (0-1000 pM) 以剂量依赖的方式阻断卵巢特异性 GFP+ 效应记忆 T (Tem) 细胞中的 Kv1.3 电流，Kd为 65 ± 5 pM[3]。
Dalazatide (0-100 nM; 3 days) 以剂量依赖的方式抑制 CCR7–T 细胞增殖[3]。
Dalazatide (100 nM; 30 min) 通过抑制钙信号通路固定炎症部位的效应记忆 T (Tem) 细胞，从而阻止 β1 整合素激活[3]。
Cell Proliferation Assay[3] | Cell Line: | CCR7–T cell[3] | | Concentration: | 0-100 nM | | Incubation Time: | 3 days | | Result: | Inhibited cell proliferation with an IC50of 180 ± 37 pM. |
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体内研究
(In Vivo) | Dalazatide (ShK-186) (100 μg/kg; s.c.; once) 在大鼠中抑制延迟型超敏反应，并抑制 Tem 细胞的体内运动和激活[3]。
| Animal Model: | Lewis rats rats, delayed-type hypersensitivity (DTH) model[3] | | Dosage: | 100 μg/kg | | Administration: | Subcutaneous injection, once | | Result: | Reduced DTH at all time points compared to rats given saline injections. Suppressed the proliferation of the Tem cells. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Solvent & Solubility | In Vitro: H2O Peptide Solubility and Storage Guidelines: 1. Calculate the length of the peptide. 2. Calculate the overall charge of the entire peptide according to the following table: | | Contents | Assign value | | Acidic amino acid | Asp (D), Glu (E), and the C-terminal -COOH. | -1 | | Basic amino acid | Arg (R), Lys (K), His (H), and the N-terminal -NH2 | +1 | | Neutral amino acid | Gly (G), Ala (A), Leu (L), Ile (I), Val (V), Cys (C), Met (M), Thr (T), Ser (S), Phe (F), Tyr (Y), Trp (W), Pro (P), Asn (N), Gln (Q) | 0 |
3. Recommended solution: | Overall charge of peptide | Details | | Negative (<0) | 1. Try to dissolve the peptide in water first.
2. If water fails, add NH4OH (<50 μL).
3. If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide. | | Positive (>0) | 1. Try to dissolve the peptide in water first.
2. If water fails, try dissolving the peptide in a 10%-30% acetic acid solution.
3. If the peptide still does not dissolve, try dissolving the peptide in a small amount of DMSO. | | Zero (=0) | 1. Try to dissolve the peptide in organic solvent (acetonitrile, methanol, etc.) first.
2. For very hydrophobic peptides, try dissolving the peptide in a small amount of DMSO, and then dilute the solution with water to the desired concentration. |
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