Conopeptide rho-TIA

Name: Conopeptide rho-TIA
Brand: TargetMol
SKU: T80175
Rating: 4.5 (1 reviews)

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Catalog No. T80175Cas No. 381725-58-2

Conopeptide rho-TIA, a peptide from Conus tulipa venom, acts as a selective, noncompetitive inhibitor at the human α1B-Adrenergic Receptor and as a competitive inhibitor at the α1A and α1D-Adrenergic Receptors. Binding to these subtypes, conopeptide rho-TIA may inform the creation of new α1-Adrenergic Receptor subtype-selective drugs [1].

Conopeptide rho-TIA

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Catalog No. T80175Cas No. 381725-58-2

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Product Introduction

Bioactivity

Description

In vitro

Conopeptide rho-TIA at a concentration of 100 nM applied for 24-48 hours interacts with human α1B-Adrenergic Receptor non-competitively and reversibly, suggesting its potential role as an allosteric inhibitor [1]. At 30 nM for 2 hours, conopeptide rho-TIA acts as a non-competitive inhibitor for the α1B-Adrenergic Receptor but competitively inhibits the α1A and α1D-Adrenergic Receptor subtypes [1]. Additionally, a single application of 10 μM conopeptide rho-TIA inhibits the increase in cytoplasmic Ca2+ concentration mediated by the α1-Adrenergic Receptor activation by norepinephrine, without affecting the presynaptic α2-Adrenergic Receptor-mediated responses [2].

Chemical Properties

Molecular Weight	2390.88
Formula	C₁₀₅H₁₆₀N₃₆O₂₁S₄
Cas No.	381725-58-2
Smiles	C([C@@H](C(N[C@H](C(N[C@@H]1C(=O)N[C@@]2(C(=O)N[C@@H](CC(C)C)C(=O)N[C@@]([C@H](CC)C)(C(=O)N3[C@](C(=O)N[C@@H](C)C(=O)N[C@@](CSSC1)(C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC4=CN=CN4)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC5=CC=CC=C5)C(=O)N[C@H](C(N)=O)CSSC2)[H])(CCC3)[H])[H])[H])=O)CCCNC(=N)N)=O)NC([C@@H](NC([C@H](CC6=CC=CC=C6)N)=O)CC(N)=O)=O)C=7C=8C(NC7)=CC=CC8
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)
Sequence Short	FNWRCCLIPACRRNHKKFC (Disulfide bridge: Cys5-Cys11, Cys6-Cys19)

Storage & Solubility Information

Storage

keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc