E2138

エキスタチン

α1 isoform, ≥90% (HPLC)

• 実験式（ヒル表記法）: C₂₁₇H₃₄₁N₇₁O₇₄S₉
• CAS番号: 154303-05-6
• 分子量: 5417.05
• UNSPSC Code: 12352200
• MDL number: MFCD00081572
• Form: powder
• Assay: ≥90% (HPLC)
• Biological source: Echis carinatus

特性

• biological source: Echis carinatus
• assay: ≥90% (HPLC)
• form: powder
• technique(s): flow cytometry: suitable, inhibition assay: suitable
• storage temp.: −20°C

詳細

General description

Echistatin is a single chain 49 amino acid residue protein, which prevents the aggregation of platelets. It has an isoelectric point (pI) of 8.3 and a molecular weight of 5400. This peptide is present in the venom of Echis carinatus, which is a saw-scaled viper. It contains the arginine-glycine-aspartic (RGD) acid sequence, which is present in proteins that bind to glycoprotein IIb/IIIa complex. It shares the proline-arginine-asparagine-proline sequence with the Aα chain of human fibrinogen. This protein is a member of disintegrin family, which prevents cell adhesion. With regards to molecular weight, echistatins are the smallest member of disintegrin family, and contains four isoforms called, α1, α2, β and γ.

Application

Echistatin has been used:

• as an inhibitor of integrin function to study the role of microfibril-associated glycoprotein-1 (Magp1) in the morphogenesis of vascular structures
• for the preparation of microbubbles targeted to αvβ3 integrins in tumor angiogenesis imaging
• as a conjugate to αvβ3 in flow cytometric binding studies

Biochem/physiol Actions

Echistatin is a disintegrin, which prevents the aggregation of platelets. They interact with and prevent the binding of fibrinogen to their receptors on the membrane of platelets. It also inhibits platelet aggregation mediated by epinephrine, thrombin, collagen, or platelet-activating factor. Studies in isolated osteoclasts show that this peptide inhibits bone resorption by osteoclasts, most probably by damaging adhesion structures.

Disintegrin類は、マムシ毒から分離されたintegrin β1およびβ3インヒビタ-タンパク質の新規ファミリ-です。低分子量でシステイン残基に富むペプチドであり、Arg-Gly-Asp(RGD)配列を含みます。Integrinの機能に対する最も強力なインヒビタ-として知られています。Disintegrinは、メラノ-マ細胞や線維芽細胞とフィブロネクチンとの接着のような細胞外マトリックスへの細胞接着を阻害するほか、血小板凝集も強力に阻害します。

ディスインテグリンファミリ-メンバ-、インテグリンβ1およびβ3の新規阻害タンパク質、およびインテグリン機能の最も強力なインヒビタ-です。

安全性情報

• 保管分類: 11 - Combustible Solids
• 一体何が起きているの？: WGK 3
• 引火点 (F): Not applicable
• 引火点（°C）: Not applicable