| Bioactivity | ADWX 1 is a new peptide inhibitor that is potent and selective for Kv1.3 with an IC50 value of 1.89 pM. ADWX 1 inhibits Kv1.3 channel activity specifically to inhibit both the initial calcium signaling and NF-κB activation. ADWX 1 ameliorates the disease in rats of experimental autoimmune encephalomyelitis (EAE) models. ADWX 1 can be used to study T cell-mediated autoimmune diseases[1][2]. |
| Invitro | ADWX 1 (1，10 nM，1 h) 降低 IL-2 和 IFN-γ 水平，选择性抑制人CD4+ CCR7- TEM 细胞的激活[2]。ADWX 1 (1，10 nM，50 min) 降低来源于 EAE 大鼠中激活的 CD4+ CCR7- TCM 细胞的 [Ca2+] 水平[2]。ADWX 1 (1，10 nM，1 h) 抑制来源于 EAE 大鼠中髓鞘碱性蛋白 (myelin basic protein, MBP) (HY-P77995) 激活的 CD4+ CCR7- T 细胞中 NF-κB 的激活，并特异降低 Kv1.3 基因和蛋白的水平[2]。ADWX 1 (1，10 nM，3 天) 抑制 CD4+ CCR7- T 细胞中 Th17 的激活但不抑制分化[2]。 RT-PCR[2] Cell Line: |
| In Vivo | ADWX 1 (100 μg/kg/day，皮下注射，3天) 通过抑制 Sprague-Dawley 大鼠实验性自身免疫性脑脊髓炎(EAE) 模型中 IL-2 和 IFN-γ 的产生以及抑制 CCR7- TEM 细胞的增殖改善疾病[2]。ADWX 1 (5/10 mg/kg，口服，2 周) 未诱导大鼠行为或组织发生病理变化 (急性毒性实验)[2]。 Animal Model: |
| Name | ADWX 1 |
| Sequence | Val-Gly-Ile-Asn-Val-Lys-Cys-Lys-His-Ser-Arg-Gln-Cys-Leu-Lys-Pro-Cys-Lys-Asp-Ala-Gly-Met-Arg-Phe-Gly-Lys-Cys-Thr-Asn-Gly-Lys-Cys-His-Cys-Thr-Pro-Lys (Disulfide bonds: Cys7-Cys27, Cys13-Cys32, Cys17-Cys34) |
| Shortening | VGINVKCKHSRQCLKPCKDAGMRFGKCTNGKCHCTPK (Disulfide bonds: Cys7-Cys27, Cys13-Cys32, Cys17-Cys34) |
| Formula | C169H281N57O46S7 |
| Molar Mass | 4071.85 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Han S, et al. Structural basis of a potent peptide inhibitor designed for Kv1.3 channel, a therapeutic target of autoimmune disease. J Biol Chem. 2008 Jul 4;283(27):19058-65. [2]. Li Z, 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 Aug 24;287(35):29479-94. |