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Cat. No.: HY-111318

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GYKI-14451 sulfate

GYKI-14451 sulfate is an inhibitor of thrombin and plasmin. GYKI-14451 sulfate inhibits thrombin-fibrinogen and plasmin-fibrin reactions. GYKI-14451 sulfate inhibits fibrin clot lysis and prolongs fibrin clot lysis time in a dose-dependent manner. GYKI-14451 sulfate does not undergo N-terminal cyclization and spontaneous inactivation in neutral aqueous buffer. GYKI-14451 sulfate can be used in studies related to venous thrombosis and fibrinogen solidification.

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

CAS No.: 83861-29-4
Formula: C₂₅H₃₉N₆O₇S_0.5
Molecular Weight:551.65

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

GYKI-14451 sulfate Chemical Structure

CAS No.: 83861-29-4

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Use of MCE Products

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

Biological Activity
- Description
- In Vitro
Chemical Information
Purity & Documentation
References
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Biological Activity

Description

In Vitro

GYKI-14451 (0.27 μM; 1-5 days) sulfate maintains completely stable anticoagulant activity over 5 days, with an initial I₈₀ of 0.27 μM^[1].
GYKI-14451 sulfate potently inhibits plasmin, urokinase (UK)-mediated plasminogen activation, and tissue-type plasminogen activator (tPA)-mediated plasminogen activation in fibrin plate assays, with corresponding ID₅₀ values of 0.4 μg, 0.02 μg, and 0.11 μg per reaction system, respectively^[1].
GYKI-14451 (0.18-0.72 μM) sulfate dose-dependently prolongs the plasmin-mediated dissolution of fibrin clots formed in its presence, with dissolution times of 10 min at 0.18 μM, 20 min at 0.36 μM, and 40 min at 0.72 μM^[1].

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

Chemical Information

CAS No. 83861-29-4
Molecular Weight 551.65
Formula C₂₅H₃₉N₆O₇S_0.5
SMILES

O=S(O)(O)=O.CC(C)(C)OC(N[C@H](CC1=CC=CC=C1)C(N2[C@@H](CCC2)C(N[C@H](C=O)CCCNC(N)=N)=O)=O)=O
Sequence

Boc-{d-Phe}-Pro-Arg-H
Sequence Shortening

Boc-{d-Phe}-PR-H
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Bajusz S, et al. Highly active and selective anticoagulants: D-Phe-Pro-Arg-H, a free tripeptide aldehyde prone to spontaneous inactivation, and its stable N-methyl derivative, D-MePhe-Pro-Arg-H. Journal of medicinal chemistry. 1990 Jun;33(6):1729-35. [Content Brief]

[2]. Hidaka T, et al. Inhibition of polymorphonuclear leukocyte 5-lipoxygenase and platelet cyclooxygenase by alpha-(3,5-di-tert-butyl-4-hydroxybenzylidene)-gamma-butyrolacto ne (KME-4), a new anti-inflammatory drug. Japanese journal of pharmacology. 1985 Jul;38(3):267-72.

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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.

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100 mg

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