Products

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 α_1-adrenoreceptor (α_1A-, α_1B- and α_1D-AR). It acts

non-competitively onto α_1B-adrenoreceptor but competitively on α_1A-adrenoreceptor and α_1D-

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

human α_1B-adrenoreceptor over α_1A-adrenoreceptor and α_1D-adrenoreceptor. The IC₅₀ values for Rho-

conotoxin TIA for inhibition of ¹²⁵I-BE were 18 nM for human α_1A-AR, 2 nM for α_1B-AR and 25 nM for

α_1D-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