Dalazatide (Synonyms: ShK-186)

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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.

For research use only. We do not sell to patients.

Dalazatide Chemical Structure

CAS No. : 1081110-69-1

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Other Forms of Dalazatide:

Dalazatide TFA In-stock

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Purity & Documentation
References
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Description

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 K_d 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[3]

Cell Line:	CCR7⁻ T cell^[3]
Concentration:	0-100 nM
Incubation Time:	3 days
Result:	Inhibited cell proliferation with an IC₅₀ of 180 ± 37 pM.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Clinical Trial

Molecular Weight

4442.08

Formula

C₁₈₄H₂₉₆N₅₇O₅₅PS₇

CAS No.

1081110-69-1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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.

Purity & Documentation

Handling Instructions (2659 KB)

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]

Dalazatide Related Classifications

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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Dalazatide1081110-69-1ShK-186ShK186ShK 186Potassium ChannelKcsAmultiple sclerosis (MS)lupus erythematosuspsoriasisrheumatoid arthritistype 1 diabetesinflammatory bowel diseaseInhibitorinhibitorinhibit

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