LY2795050

Cat. No.: HY-15708 Purity: 98.68%: FAQs
Data Sheet SDS COA Handling Instructions

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LY2795050 is a short-acting selective κ(kappa)-opioid receptor (KOR) antagonist. LY2795050 has high affinity for the KOR with K_i 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.

LY2795050 Chemical Structure

CAS No. : 1346133-08-1

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 209	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 209	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 76	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 190	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 310	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 740	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1100	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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•Related Screening Libraries:

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View All Opioid Receptor Isoform Specific Products:

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μ Opioid Receptor/MOR κ Opioid Receptor/KOR δ Opioid Receptor/DOR NOP Receptor/ORL1

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

Ki: 0.72 nM (KOR); Kb: 0.63 nM (KOR)^[1]

In Vitro

LY2795050 displays high affinity with a K_i value of 0.72 nM for the KOR and has antagonist activity with a K_b value of 0.63 nM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

LY2795050 (i.p., 0.032-0.1mg/kg, 30 min) prevents dose-dependent grooming deficits produced by U50,488 in male and female mice^[2].
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.

Animal Model:	C57BL/6J mice^[2] (gonadally intact, adult, male and female)
Dosage:	0.032-0.1 mg/kg
Administration:	i.p., 0.032-0.1mg/kg, 30 min
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.

Molecular Weight

407.89

Formula

C₂₃H₂₂ClN₃O₂

CAS No.

1346133-08-1

Appearance

Solid

Color

White to off-white

SMILES

O=C(N)C1=CC=C(OC2=CC=C(CN3[C@H](C4=CC=CN=C4)CCC3)C=C2)C(Cl)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

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)

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

View the 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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

Protocol 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

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.
Protocol 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

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.13 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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

Purity: 98.68%

Select Batch:

Data Sheet (273 KB) SDS (252 KB)

COA (248 KB) HNMR (263 KB) LCMS (268 KB) OR (170 KB)

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

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

LY2795050 Related Classifications

Neurological Disease

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

LY27950501346133-08-1LY 2795050LY-2795050Opioid Receptorκκ-receptorsex differencescentral nervous system dysfunctionInhibitorinhibitorinhibit

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