Echistatin, α1 isoform

Pricing Availability Delivery Time Qty
Cat.No. 3202 - Echistatin, alpha1 isoform | Glu-Cys-Glu-Ser-Gly-Pro-Cys-Cys-Arg-Asn-Cys-Lys-Phe-Leu-Lys-Glu-Gly-Thr-Ile-Cys-Lys-Arg-Ala-Arg-Gly-Asp-Asp-Met-Asp-Asp-Tyr-Cys-Asn-Gly-Lys-Thr-Cys-Asp-Cys-Pro-Arg-Asn-Pro-His-Lys-Gly-Pro-Ala-Thr | CAS No. 154303-05-6
Description: αVβ3 and glycoprotein IIb/IIIa (integrin αIIbβ3) inhibitor
Datasheet
Citations (2)

Biological Activity

Potent irreversible αVβ3 integrin antagonist (Ki = 0.27 nM). Disrupts attachment of osteoclasts to bone and inhibits bone reabsorption (IC50 = 0.1 nM). Prevents ADP-induced platelet aggregation via inhibition of glycoprotein IIb/IIIa (GpIIb/IIIa, αIIbβ3) receptors (IC50 = 30 nM) in vitro.

Technical Data

M. Wt 5417.1
Formula C217H341N71O74S9
Sequence ECESGPCCRNCKFLKEGTICKRARGDDMDDYCNGKTCDCPRNPHKGPAT

(Modifications: Disulfide bridge between 2 - 11, 7 - 32, 8 - 37, 20 - 39)

Storage Store at -20°C
CAS Number 154303-05-6
PubChem ID 90488810
InChI Key KZMZKUVIDVBQGX-UHFFFAOYSA-N
Smiles [H]N[C@@H](CCC(O)=O)C(=O)N[C@H]1CSSC[C@@H]2NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@@H]3CSSC[C@@H]4NC(=O)[C@@H](NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CSSC[C@H](NC(=O)[C@@H]5CCCN5C(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CCC(O)=O)NC1=O)C(=O)N3)NC(=O)[C@H](CC1=CC=C(O)C=C1)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(O)=O)NC(=O)CNC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CSSC[C@H](NC(=O)[C@H](CC(O)=O)NC4=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC1=CNC=N1)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H]([C@@H](C)O)C(O)=O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC1=CC=CC=C1)NC(=O)[C@H](CCCCN)NC2=O)[C@@H](C)O)[C@@H](C)CC)[C@@H](C)O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

SolubilitySoluble to 1 mg/ml in water

Preparing Stock Solutions

The following data is based on the product molecular weight 5417.1. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 0.18 mL 0.92 mL 1.85 mL
5 mM 0.04 mL 0.18 mL 0.37 mL
10 mM 0.02 mL 0.09 mL 0.18 mL
50 mM 0 mL 0.02 mL 0.04 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

Musial et al (1990) Inhibition of platelet adhesion to surfaces of extracorporeal circuits by disintegrins RGD-containing peptides from viper venoms. Circulation 82 261 PMID: 2364514

Sato et al (1990) Echistatin is a potent inhibitor of bone resorption in culture. J.Cell.Biol. 111 1713 PMID: 2211834

Kumar et al (1997) Biochemical characteriation of the binding of echistatin to integrin αVβ3 receptor. J.Pharmacol.Exp.Ther. 283 843 PMID: 9353406


If you know of a relevant reference for Echistatin, α1 isoform, please let us know.

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Keywords: αVβ3 alphaVβ3 beta3 glycoprotein IIb/IIIa αIIbβ3 alphaIIbβ3 inhibitors inhibits Integrin Receptors Adhesion Molecules Echistatin alpha1 isoform Echistatina1 alphavbeta3 Integrins

2 Citations for Echistatin, α1 isoform

Citations are publications that use Tocris products. Selected citations for Echistatin, α1 isoform include:

Schrader et al (2011) Matrix stiffness modulates proliferation, chemotherapeutic response, and dormancy in hepatocellular carcinoma cells. Biomed Res Int 53 1192 PMID: 21442631

Lin et al (2013) Angiopoietin-like 3 induces podocyte F-actin rearrangement through integrin α(V)β3/FAK/PI3K pathway-mediated Rac1 activation. PLoS One 2013 135608 PMID: 24294595


Do you know of a great paper that uses Echistatin, α1 isoform from Tocris? If so please let us know.

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