LY2795050
Based on 1 Customer Validation
LY2795050 is a short-acting selective κ(kappa)-opioid receptor (KOR) antagonist. LY2795050 has high affinity for the KOR with Ki value of 0.72 nM. LY2795050 can be used for the research of central nervous system dysfunction.
For research use only. We do not sell to patients.
- Purity: 98.12%
- CAS No.: 1346133-08-1
- Formula: C23H22ClN3O2
- Molecular Weight:407.89
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Ki: 0.72 nM (KOR); Kb: 0.63 nM (KOR)[1]
LY2795050 displays high affinity with a Ki value of 0.72 nM for the KOR and has antagonist activity with a Kb value of 0.63 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
LY2795050 (i.p., 0.032-0.1mg/kg, 0-150 min) has sexual dimorphism in some behavioral effects[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J mice[2]
(gonadally intact, adult, male and female) -
Dosage:0.032-0.1 mg/kg
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Administration:i.p., 0.032-0.1mg/kg, 30 min
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Result:Could dose-dependently prevent the self-grooming deficits caused by U50,488 with a 30-min pre-treatment.
Not effected in blocking the effects of U50,488 with smaller dose (0.032mg/kg) in either males or females.
Decreased immobility in the FST in males at a dose of 0.1mg/kg, but not in females, up to a dose of 0.32mg/kg.
Prevented and also reversed (at 0.32mg/kg) the locomotor-depressant effects of U50,488 (10mg/kg), in males and females.
Chemical Information
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CAS No. 1346133-08-1
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Appearance Solid
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Molecular Weight 407.89
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Formula C23H22ClN3O2
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Color White to off-white
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SMILES
O=C(N)C1=CC=C(OC2=CC=C(CN3[C@H](C4=CC=CN=C4)CCC3)C=C2)C(Cl)=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvent & Solubility
DMSO : 50 mg/mL (122.58 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
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
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (274 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Ming-Qiang Zheng, et al. Synthesis and evaluation of 11C-LY2795050 as a κ-opioid receptor antagonist radiotracer for PET imaging. J Nucl Med [Content Brief]
[2]. Eduardo R Butelman, et al. Profile of a short-acting κ-antagonist, LY2795050, on self-grooming behaviors, forced swim test and locomotor activity: sex comparison in mice. J Psychopharmacol. 2021 May;35(5):579-590. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4516 mL | 12.2582 mL | 24.5164 mL | 61.2910 mL |
| 5 mM | 0.4903 mL | 2.4516 mL | 4.9033 mL | 12.2582 mL | |
| 10 mM | 0.2452 mL | 1.2258 mL | 2.4516 mL | 6.1291 mL | |
| 15 mM | 0.1634 mL | 0.8172 mL | 1.6344 mL | 4.0861 mL | |
| 20 mM | 0.1226 mL | 0.6129 mL | 1.2258 mL | 3.0646 mL | |
| 25 mM | 0.0981 mL | 0.4903 mL | 0.9807 mL | 2.4516 mL | |
| 30 mM | 0.0817 mL | 0.4086 mL | 0.8172 mL | 2.0430 mL | |
| 40 mM | 0.0613 mL | 0.3065 mL | 0.6129 mL | 1.5323 mL | |
| 50 mM | 0.0490 mL | 0.2452 mL | 0.4903 mL | 1.2258 mL | |
| 60 mM | 0.0409 mL | 0.2043 mL | 0.4086 mL | 1.0215 mL | |
| 80 mM | 0.0306 mL | 0.1532 mL | 0.3065 mL | 0.7661 mL | |
| 100 mM | 0.0245 mL | 0.1226 mL | 0.2452 mL | 0.6129 mL |
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