Conopeptide rho-TIA 

Conopeptide rho-TIA is a peptide derived from the venom contained in the predatory sea snail Conus tulipa, has highly selective and noncompetitive inhibitor at human α_1B-Adrenergic Receptor. Conopeptide rho-TIA acts a competitive inhibitor at human α_1A-Adrenergic Receptor and α_1D-Adrenergic Receptor. Conopeptide rho-TIA binds to each subtype and may provide useful information for the development of novel α₁-Adrenergic Receptor subtype-selective drugs^[1].

Conopeptide rho-TIA (100 nM, 24-48 h) binds in a noncompetitive, reversible manner to the human α_1B-Adrenergic Receptor, which suggests that conopeptide rho-TIA is likely to be an allosteric inhibitor^[1].
Conopeptide rho-TIA (30 nM, 2 h) is a noncompetitive inhibitor at human α_1B-Adrenergic Receptor, whereas at α_1A-Adrenergic Receptor and α_1D-Adrenergic Receptor subtypes it acts as a competitive inhibitor^[1].
Conopeptide rho-TIA (10 μM, one time) inhibits α₁-adrenorecepto-mediated increases in cytosolic Ca²⁺ concentration that were triggered by norepinephrine, but did not affect presynaptic α₂-adrenoreceptor-mediated responses^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

2390.88

C₁₀₅H₁₆₀N₃₆O₂₁S₄

381725-58-2

Phe-Asn-Trp-Arg-Cys-Cys-Leu-Ile-Pro-Ala-Cys-Arg-Arg-Asn-His-Lys-Lys-Phe-Cys-NH2 (Disulfide bridge: Cys5-Cys11, Cys6-Cys19)

FNWRCCLIPACRRNHKKFC-NH2 (Disulfide bridge: Cys5-Cys11, Cys6-Cys19)

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Chen Z, et al. Subtype-selective noncompetitive or competitive inhibition of human alpha1-adrenergic receptors by rho-TIA. J Biol Chem. 2004 Aug 20;279(34):35326-33.  [Content Brief]

  [2]. Sharpe IA, et al. Allosteric alpha 1-adrenoreceptor antagonism by the conopeptide rho-TIA. J Biol Chem. 2003 Sep 5;278(36):34451-7.  [Content Brief]