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 α1B-Adrenergic Receptor. Conopeptide rho-TIA acts a competitive inhibitor at human α1A-Adrenergic Receptor and α1D-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.
For research use only. We do not sell to patients.
- CAS No.: 381725-58-2
- Formula: C105H160N36O21S4
- Molecular Weight:2390.88
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Adrenergic Receptor Isoforms
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Biological Activity
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α1B Adrenergic Receptor |
α1A Adrenergic Receptor |
α1D Adrenergic Receptor |
Conopeptide rho-TIA (100 nM, 24-48 h) binds in a noncompetitive, reversible manner to the human α1B-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 α1B-Adrenergic Receptor, whereas at α1A-Adrenergic Receptor and α1D-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.
Chemical Information
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CAS No. 381725-58-2
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Molecular Weight 2390.88
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Formula C105H160N36O21S4
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Sequence
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)
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Sequence Shortening
FNWRCCLIPACRRNHKKFC-NH2 (Disulfide bridge: Cys5-Cys11, Cys6-Cys19)
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)