Smartox Biotechnology
 
작성일 : 14-11-24
[Smartox Biotechnology] G protein-coupled receptor (GPCR) blockers
Rho-Conotoxin-TIA, Blocker of α1-adrenoreceptor

 

 

Rho-Conotoxin-TIA, G protein-coupled receptor (GPCR) blockers

Blocker of α1-adrenoreceptor

 

 

Rho-conotoxin TIA has been isolated from the venom of the fish-hunting marine cone snail Conus

tulipa. Rho-conotoxin TIA is a selective antagonist of α1-adrenoreceptor (α1A-, α1B- and α1D-AR). It acts

non-competitively onto α1B-adrenoreceptor but competitively on α1A-adrenoreceptor and α1D-

adrenoreceptor. The most important residue for activity is Arg4. Rho-conotoxin TIA is 10-fold selective for

human α1B-adrenoreceptor over α1A-adrenoreceptor and α1D-adrenoreceptor. The IC50 values for Rho-

conotoxin TIA for inhibition of 125I-BE were 18 nM for human α1A-AR, 2 nM for α1B-AR and 25 nM for

α1D-AR.

 

Details

AA sequence:

 

 

Phe-Asn-Trp-Arg-Cys5-Cys6-Leu-Ile-Pro-Ala-Cys11-Arg-Arg-Asn-His-Lys-

Lys-Phe-Cys19-NH2

 

Disulfide bonds:

 

 

Cys5-Cys11 and Cys6-Cys19

 

Length (aa):

 

 

19

 

Formula:

 

 

C105H160N36O21S4

 

Molecular Weight:

 

 

2290.90. Da

 

Appearance:

 

 

White lyophilized solid

 

Solubility:

 

 

Aqueous buffer

 

Source:

 

 

Synthetic

 

Purity rate

 

 

> 97 %

 

 

Reference

1. Sharpe I., et al. (2003) Allosteric alpha1-Adrenoreceptor Antagonism by the Conopeptide rho-TIA. JBC. PMID: 12824165

 

 

Ordering information

Catalog No.

Product Name

Size

CON022

Rho-Conotoxin-TIA

0.1 mg, 0.5 mg & 1.0 mg

 

 

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