1. GPCR/G Protein
    Neuronal Signaling
  2. Opioid Receptor
  3. LY2795050

LY2795050 

Cat. No.: HY-15708 Purity: 98.12%
Handling Instructions

LY2795050 is a novel selective κ-opioid Receptor (KOR) antagonist (IC50=0.72 nM) and has the potential as a PET tracer to image KOR in vivo.

For research use only. We do not sell to patients.

LY2795050 Chemical Structure

LY2795050 Chemical Structure

CAS No. : 1346133-08-1

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 264 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 264 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 240 In-stock
Estimated Time of Arrival: December 31
10 mg USD 384 In-stock
Estimated Time of Arrival: December 31
50 mg USD 900 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1680 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Description

LY2795050 is a novel selective κ-opioid Receptor (KOR) antagonist (IC50=0.72 nM) and has the potential as a PET tracer to image KOR in vivo. IC50 Value: 0.72 nM (κ-opioid Receptor); 25.8 nM (κ-opioid) [1] Target: κ-opioid Receptor in vitro: LY2795050 displays full antagonist activity and high binding affinity and selectivity for KOR with a ki value of 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 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].

Molecular Weight

407.89

Formula

C23H22ClN3O2

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (122.58 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4516 mL 12.2582 mL 24.5164 mL
5 mM 0.4903 mL 2.4516 mL 4.9033 mL
10 mM 0.2452 mL 1.2258 mL 2.4516 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.13 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.13 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.13 mM); Clear solution

*All of the co-solvents are available by MCE.
References
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LY2795050
Cat. No.:
HY-15708
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