Hirudin

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Cat Number

PIPE-0132

CAS Number

113274-56-9

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Product Detail Description Scientific Support Customer Q&A

CAS Number

113274-56-9

Storage

Inert atmosphere, under -20℃

Synonyms

H-GLY-ASP-PHE-GLU-GLU-ILE-PRO-GLU-GLU-TYR-LEU-GLN-OH; GLY-ASP-PHE-GLU-GLU-ILE-PRO-GLU-GLU-TYR-LEU-GLN

Molecular Formula

C66H93N13O25

Molecular Weight

1468.52

Boiling Point

1913.6

Relative Density

1.384

pKa

3.25±0.10

General Description

Hirudin is a powerful natural peptide anticoagulant that was first isolated from the salivary glands of leeches. Hirudin's effectiveness is mainly due to its potent anticoagulant properties, which are independent of endogenous cofactors, effective at low doses, and do not cause the bleeding complications associated with other anticoagulants like heparin.

Mechanism of Action

Hirudin works by binding directly and with very high affinity to the catalytic cleft and exosite I of thrombin. This specific binding inhibits the proteolytic activity of thrombin, thereby preventing the conversion of fibrinogen to fibrin and subsequent blood clot formation.

Application

Hirudin is mainly used for its potent anticoagulant and antithrombotic properties in the treatment and prevention of thromboembolic disorders.

Hirudin arrests the growth of ovarian cancer cells (A2780) by disrupting the thrombin–PAR-1–PKCα–EMT axis. Thrombin cleaves the N-terminus of PAR-1, which unveils an N-terminus tethered ligand that auto-activates PAR-1. This recruits Gαq/11 and activates phospholipase Cβ, resulting in the formation of diacylglycerol which phosphorylates PKCα. Phospho-PKCα translocates to the nucleus, where it stabilizes Snail, a master transcriptional repressor of E-cadherin and an activator of CDH2 and Vimentin. Hirudin sterically blocks access to PAR-1. PKCα is unphosphorylated, Snail mRNA rapidly decreases and mesenchymal genes CDH2 and Vimentin are transcriptionally repressed. Loss of these EMT drivers maintain A2780 cells in an epithelial, non-proliferative state.
Hirudin is a specific molecular off-switch for the thrombin-EMT circuit in ovarian cancer cells. These data suggest that Hirudin is worthy of further consideration as an anti-cancer agent for the treatment of ovarian cancer.

Fig. 1 Mechanism of action for Hirudin against ovarian cancer. (Kou J.; et al. 2024)

References

Kou J, et al. Mechanism of hirudin-mediated inhibition of Proliferation in Ovarian Cancer cells. Molecular biotechnology, 2024, 66(5): 1062-1070.

What is the primary function of Hirudin?

Hirudin is the strongest known natural and specific inhibitor of thrombin (Factor IIa), providing powerful anticoagulant and antithrombotic effects.

Does Hirudin offer benefits for microcirculation and metabolism?

Yes, Hirudin helps improve microcirculation, assists in the absorption of hematomas, and promotes metabolism.

What is the molecular composition of Hirudin?

Hirudin is a small polypeptide composed of 65-66 amino acids, a defining characteristic of its potent and specific biological activity.

What is the purity of your Hirudin?

We guarantee the specific purity of our Hirudin meeting industry standards.