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Art. -Nr.: HY-P3507A

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Dalazatide TFA

(Synonyms: ShK-186 TFA)

Kundenbewertung

Based on 1 Customer Validation

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

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 99.92%
Formel: C₁₈₄H₂₉₆N₅₇O₅₅PS₇._xC₂HF₃O₂
Molecular Weight:4442.10 (free acid)

Speicherung:

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)

Dalazatide TFA Chemical Structure

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

Kv1.3^[1]

In Vitro

Dalazatide (ShK-186) (0-1000 pM) TFA 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) TFA inhibits CCR7⁻ T cell proliferation in a dose-dependent manner^[3].
Dalazatide (100 nM; 30 min) TFA 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) TFA 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.

Chemical Information

Appearance Solid
Molecular Weight 4442.10 (free acid)
Formel C₁₈₄H₂₉₆N₅₇O₅₅PS₇._xC₂HF₃O₂
Color White to off-white
Synonyms

ShK-186 TFA
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)
Sequence Shortening

H-{pY}-{AEEA}-RSCIDTIPKSRCTAFQCKHSMKYRLSFCRKTCGTC-NH2 (disulfide bridge:Cys5-Cys37,Cys14-Cys30,Cys19-Cys34)
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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)

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 100 mg/mL

H₂O : 100 mg/mL (Need ultrasonic)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (298 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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