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Fuscoside

Name: Fuscoside
Brand: TargetMol
SKU: T4355
Price: 52 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T4355Cas No. 131631-89-5

Alias OPC 21268

Fuscoside (OPC-21268) is a non-peptide arginine vasopressin (AVP) receptor VI antagonist with an IC50 value of 0.4 μM[2].

Fuscoside

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Purity: 99.66%

Catalog No. T4355Alias OPC 21268Cas No. 131631-89-5

Fuscoside (OPC-21268) is a non-peptide arginine vasopressin (AVP) receptor VI antagonist with an IC50 value of 0.4 μM[2].

Pack Size	Price	USA Warehouse	Global Warehouse
2 mg	$52	In Stock	In Stock
5 mg	$80	In Stock	In Stock
10 mg	$108	In Stock	In Stock
25 mg	$182	In Stock	In Stock
50 mg	$256	In Stock	In Stock
100 mg	$442	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$80	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products.If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.

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Purity:99.66%

Appearance:Solid

Color:White

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COA HPLC HNMR

Product Introduction

Fuscoside AI Summary

Fuscoside exhibits a high binding affinity for the Vasopressin V1a receptor, particularly in rat liver tissues, with a Ki value of 23.5 nM, and a much lower affinity for the V1a receptor in human liver tissues, with a Ki value of 14000.0 nM. It demonstrates significant selectivity for Vasopressin V2 receptors over V1a receptors in rat kidney membranes (selectivity ratio > 430) and displaces [3H]-Arginine Vasopressin in rat liver with an IC50 of 440.0 nM. Additionally, Fuscoside shows moderate affinity for oxytocin receptors in rat and human uterus tissues, with Ki values of 230.0 nM and 170.0 nM, respectively. In vivo studies indicate its potential to inhibit AVP-induced pressor response in pithed rats at a dose of 0.34 mg.kg-1 by 50%. Furthermore, Fuscoside exhibits antiviral activity by inhibiting SARS-CoV-2-induced cytotoxicity in both VERO-6 and Caco-2 cells and also acts as a modest inhibitor of human HDAC6 activity, showcasing a varied biological activity profile depending on the assay conditions and substrates used..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Fuscoside (OPC-21268) is a non-peptide arginine vasopressin (AVP) receptor VI antagonist with an IC50 value of 0.4 μM[2].
Targets&IC50	V1 receptor(rat):25 nM, V1 receptor(human):8800 nM
In vitro	Fuscoside (OPC-21268) can replace 50% of the specific AVP binding concentration (IC50), including 0.4 μM for VI receptors and 100 μM for V2 receptors; at the same time, the inhibition constant (Ki) of Fuscoside (OPC-21268) for V1 receptors is 0.14 μM[2].
In vivo	METHODS: OPC-21268 was injected intravenously into dogs and rats at doses of 0.3, 1.0, and 3.0 mg/kg to study its antagonistic effects on arginine vasopressin (AVP)-induced vasoconstrictor responses in spinally anesthetized dogs. RESULTS OPC-21268 produced a right-parallel shift of the AVP dose-response curve in a dose-dependent manner; doses of OPC-21268 were similar to those that inhibited AVP-induced vasoconstrictor responses in rats; OPC-21268 acted as a V1-AVP receptor antagonist in peripheral resistance vessels of dogs and rats. [1]
Synonyms	OPC 21268

Chemical Properties

Molecular Weight	449.54
Formula	C₂₆H₃₁N₃O₄
Cas No.	131631-89-5
Smiles	CC(=O)NCCCOc1ccc(cc1)C(=O)N1CCC(CC1)N1C(=O)CCc2ccccc12
Relative Density.	1.221g/cm3

Storage & Solubility Information

Storage

In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 60 mg/mL (133.47 mM), Sonication is recommended.

Ethanol: 11.24 mg/mL (25 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.45 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	2.2245 mL	11.1225 mL	22.2450 mL	111.2248 mL
5 mM	0.4449 mL	2.2245 mL	4.4490 mL	22.2450 mL
10 mM	0.2224 mL	1.1122 mL	2.2245 mL	11.1225 mL
20 mM	0.1112 mL	0.5561 mL	1.1122 mL	5.5612 mL

DMSO

	1mg	5mg	10mg	50mg
50 mM	0.0445 mL	0.2224 mL	0.4449 mL	2.2245 mL
100 mM	0.0222 mL	0.1112 mL	0.2224 mL	1.1122 mL

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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