GYKI-14451 sulfate

SKU:BHB21900248
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Overview
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GYKI-14451 sulfate (CAS 83861-29-4) is an inhibitor. Relevant to Metabolic Enzyme/Protease research. Molecular formula C25H39N6O7S0.5, molecular weight 551.65 g/mol.
CAS Number 83861-29-4
Molecular Weight 551.65 g/mol
Storage See Certificate of Analysis
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Catalog no. Size
HY-111318-50MG 50 mg
HY-111318-100MG 100 mg
HY-111318-250MG 250 mg
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  • Options: Size: 50 mg, 100 mg, 250 mg
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  • Storage: Please store the product under the recommended conditions in the Certificate of Analysis.
  • Shipping: Room temperature in continental US; may vary elsewhere.
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Field Specification
CAS no. 83861-29-4
Applications
  • Functional Assay (In Vitro)
Molecular weight 551.65
Molecular formula C25H39N6O7S0.5
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
Storage Refer to Certificate of Analysis (CoA) for storage conditions
Shipping Room temperature in continental US; may vary elsewhere.
Catalog no. (Mfr.) HY-111318
Main SKU BHB21900248
Inhibitors

Compound Overview

GYKI-14451 sulfate inhibits both thrombin and plasmin, blocking the thrombin-fibrinogen and plasmin-fibrin reactions. It inhibits fibrin clot lysis and prolongs fibrin clot lysis time in a dose-dependent manner, and it does not undergo N-terminal cyclization or spontaneous inactivation in neutral aqueous buffer. It can be used in studies of venous thrombosis and fibrinogen solidification[1]. It corresponds to the peptide sequence Boc-{d-Phe}-Pro-Arg-H (C25H39N6O7S0.5, MW 551.65).

Physical & Chemical Properties

CAS Number 83861-29-4
Molecular Formula C25H39N6O7S0.5
Molecular Weight 551.65 g/mol
Sequence Boc-{d-Phe}-Pro-Arg-H
Sequence (one-letter) Boc-{d-Phe}-PR-H
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
Signaling Pathway Metabolic Enzyme/Protease
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Shipping Room temperature in continental US; may vary elsewhere.

Literature Cited

Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under 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.

[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.

Safety

For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with your institution's chemical hygiene plan.

In Vitro

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

Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.

Q.Why is there no price listed?
A.Every size of this product is quoted on inquiry. Send us the size you need and we will come back with price and lead time.
Q.Can this be used in humans or for diagnostics?
A.No. This product is supplied For Research Use Only. It is not for diagnostic or therapeutic procedures and not for human or veterinary use.

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