Rho-Conotoxin-TIA

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Blocker of α1-adrenoreceptor

Rho-conotoxin TIA is a conopeptide that 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 Arg4Rho-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.

 

SKU: CON022 Category: Tags: ,

Description

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: 2390.90 Da
Appearance: White lyophilized solid
Solubility: aqueous buffer
CAS number: not available
Source: Synthetic
Purity rate: > 95 %

Allosteric alpha1-Adrenoreceptor Antagonism by the Conopeptide rho-TIA

Subtype-selective noncompetitive or competitive inhibition of human α1-Adrenergic receptors by rho-TIA

Differential Distribution of Functionalalpha1-Adrenergic Receptor Subtypes along the Rat Tail Artery

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    Rho-Conotoxin-TIA

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