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MedChemExpress - Model Dalazatide - ...

MedChemExpress - Model Dalazatide - 1081110-69-1

Dalazatide (ShK-186) is a specific Kv1.3 potassium channel peptide 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].

Dalazatide

MCE China：Dalazatide

Brand：MedChemExpress (MCE)

Cat. No.HY-P3507

CAS：1081110-69-1

Synonyms：ShK-186

Purity：99.23%

Storage：Sealed storage, away from moisture Powder -80°C 2 years -20°C 1 year *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Dalazatide (ShK-186) is a specific Kv1.3 potassium channel peptide 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.

In Vitro：Dalazatide (ShK-186) (0-1000 pM) blocks the Kv1.3 current in the Ova-specific GFP+ effector memory T (Tem) cells in a dose-dependent manner with a Kd of 65 ± 5 pM[3]. Dalazatide (0-100 nM; 3 days) inhibits CCR7− T cell proliferation in a dose-dependent manner[3]. Dalazatide (100 nM; 30 min) immobilizes effector memory T (Tem) cells at inflammatory sites by suppressing calcium signaling and thereby preventing β1 integrin activation[3].

In Vivo：Dalazatide (ShK-186) (100 μg/kg; s.c.; once) inhibits delayed-type hypersensitivity and suppresses the in vivo motility and activation of Tem cells in rats[3].

Sequence：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)

References：

[1]. Olsen C, et al. Dalazatide (ShK-186), a first-in-class peptide inhibitor of Kv1. 3 potassium channels, demonstrates safety, tolerability and proof of concept of efficacy in patients with active plaque psoriasis. J. Invest. Dermatol., 2016, 136(8).

[2]. Stevens A M, et al. Thu0285 Dalazatide, an Inhibitor of the KV1. 3 Channel on Activated Effector Memory T Cells, Has Immunotherapy Potential in Systemic Lupus Erythematosus. 2016.

[3]. Matheu MP, et al. Imaging of effector memory T cells during a delayed-type hypersensitivity reaction and suppression by Kv1.3 channel block. Immunity. 2008 Oct 17;29(4):602-14. [Content Brief]

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