Conopeptide rho-TIA

CAS: 381725-58-2 F: C105H160N36O21S4 W: 2390.88

Conopeptide rho-TIA is a peptide derived from the venom contained in the predatory sea snail Conus tulipa, has highly se

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Bioactivity	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[1].
Invitro	Conopeptide rho-TIA (100 nM, 24-48 h) 以非竞争性、可逆的方式与人 α1B-Adrenergic Receptor，这表明conopeptide rho-TIA 可能是一种异位抑制剂[1]。Conopeptide rho-TIA (30 nM, 2 h) 对人 α1B-Adrenergic Receptor 是一种非竞争性抑制剂，而对α1A-Adrenergic Receptor 和 α1D-Adrenergic Receptor 亚型则是一种竞争性抑制剂[1]。Conopeptide rho-TIA (10 μM, one time) 抑制去甲肾上腺素引发的 α1 肾上腺素受体介导的胞浆 Ca2+ 浓度升高，但不影响突触前 α2 肾上腺素受体介导的反应[2]。
Name	Conopeptide rho-TIA
CAS	381725-58-2
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)
Shortening	FNWRCCLIPACRRNHKKFC-NH2 (Disulfide bridge: Cys5-Cys11, Cys6-Cys19)
Formula	C105H160N36O21S4
Molar Mass	2390.88
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[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. [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.