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LY2795050

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Purity:97.77%

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COA HNMR HPLC

LY2795050

Catalog No. TQ0091Cas No. 1346133-08-1

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

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

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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

Storage & Solubility Information

Storage

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

Solubility Information

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

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)

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DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

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Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

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