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LY2795050

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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

LY2795050

🥰Excellent
Purity: 97.77%
Catalog No. TQ0091Cas No. 1346133-08-1
LY2795050 is a novel specific κ-Opioid Receptor antagonist (IC50: 0.72 nM).
Pack SizePriceAvailabilityQuantity
1 mg$48In Stock
2 mg$68In Stock
5 mg$118In Stock
10 mg$190In Stock
25 mg$313In Stock
50 mgInquiryIn Stock
1 mL x 10 mM (in DMSO)$129In Stock
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Purity:97.77%
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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 Weight407.89
FormulaC23H22ClN3O2
Cas No.1346133-08-1
SmilesNC(=O)c1ccc(Oc2ccc(CN3CCC[C@H]3c3cccnc3)cc2)c(Cl)c1
Relative Density.1.287 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -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
1mg5mg10mg50mg
1 mM2.4516 mL12.2582 mL24.5164 mL122.5821 mL
5 mM0.4903 mL2.4516 mL4.9033 mL24.5164 mL
10 mM0.2452 mL1.2258 mL2.4516 mL12.2582 mL
20 mM0.1226 mL0.6129 mL1.2258 mL6.1291 mL
50 mM0.0490 mL0.2452 mL0.4903 mL2.4516 mL
100 mM0.0245 mL0.1226 mL0.2452 mL1.2258 mL

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Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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