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LY2795050

Name: LY2795050
Brand: TargetMol
SKU: TQ0091
Price: 313 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. TQ0091Cas No. 1346133-08-1

LY2795050 is a novel specific κ-Opioid Receptor antagonist (IC50: 0.72 nM).

LY2795050

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Purity: 97.77%

Catalog No. TQ0091Cas No. 1346133-08-1

LY2795050 is a novel specific κ-Opioid Receptor antagonist (IC50: 0.72 nM).

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$48	In Stock	In Stock
2 mg	$68	In Stock	In Stock
5 mg	$118	In Stock	In Stock
10 mg	$190	In Stock	In Stock
25 mg	$313	In Stock	In Stock
50 mg	Preferential	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$129	In Stock	In Stock

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

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:97.77%

Appearance:Solid

Color:White

Resource Download

COA HPLC HNMR LCMS

Product Introduction

Bioactivity

Description	LY2795050 is a novel specific κ-Opioid Receptor antagonist (IC50: 0.72 nM).
Targets&IC50	κ opioid receptor:0.72 nM
In vitro	LY2795050 displays full antagonist activity and high binding affinity and selectivity for κ-opioid Receptor (Ki: 0.72 nM) [1].
In vivo	In the brain, (11)C-LY2795050 displayed fast uptake kinetics (regional activity peak times of <20 min) and an uptake pattern consistent with the distribution of κ-Opioid Receptor (KOR) in primates [1]. The LY2795050 ED50 at MOR was 119 μg/kg based on a 1-site model for 11C-carfentanil. The 1-site binding model was also deemed sufficient to describe the specific binding of 11C-LY2795050 at KOR. The ED50 at KOR estimated from the 1-site model was 15.6 μg/kg. Thus, the ED50 ratio for MOR:KOR was 7.6 [2].

Chemical Properties

Molecular Weight	407.89
Formula	C₂₃H₂₂ClN₃O₂
Cas No.	1346133-08-1
Smiles	NC(=O)c1ccc(Oc2ccc(CN3CCC[C@H]3c3cccnc3)cc2)c(Cl)c1
Relative Density.	1.287 g/cm3 (Predicted)

Storage & Solubility Information

Storage

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

Solubility Information

DMSO: 50 mg/mL (122.58 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.9 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

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.4516 mL	12.2582 mL	24.5164 mL	122.5821 mL
5 mM	0.4903 mL	2.4516 mL	4.9033 mL	24.5164 mL
10 mM	0.2452 mL	1.2258 mL	2.4516 mL	12.2582 mL
20 mM	0.1226 mL	0.6129 mL	1.2258 mL	6.1291 mL
50 mM	0.0490 mL	0.2452 mL	0.4903 mL	2.4516 mL
100 mM	0.0245 mL	0.1226 mL	0.2452 mL	1.2258 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