2. GPCR/G Protein Neuronal Signaling
  3. Opioid Receptor
  4. LY2444296

LY2444296 is an orally bioavailable, high-affinity and selective short-acting kappa opioid receptor (KOPR) antagonist, with a Ki value of ∼1 nM. LY2444296 exhibits anti-anxiety like effects.

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LY2444296 Chemical Structure

LY2444296 Chemical Structure

CAS No. : 1346133-11-6

Size Price Stock Quantity
Solution
10 mM * 1 mL in Ethanol USD 88 In-stock
Solid
5 mg USD 80 In-stock
10 mg USD 150 In-stock
50 mg USD 450 In-stock
100 mg USD 720 In-stock
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Based on 1 publication(s) in Google Scholar

LY2444296 Related Antibodies

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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

LY2444296 is an orally bioavailable, high-affinity and selective short-acting kappa opioid receptor (KOPR) antagonist, with a Ki value of ∼1 nM. LY2444296 exhibits anti-anxiety like effects[1][2].

IC50 & Target

Ki: ~1 nM (KOPR)[1]
In Vivo

LY2444296 displays anti-anxiety like effects in the EPM test[1].
LY2444296 (3 mg/kg; i.p.; 30 min before U69,593 administration) prevents behavioral and neuroendocrine effects caused by the reference kappa agonist U69,593 in cocaine-naïve rats[2].
LY2444296 reduces anxiety-like and depressive-like behaviors, as well as CORT release, in rats tested after chronic extended access cocaine self-administration, but not in cocaine-naïve rats[2].

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

Animal Model: Adult male Sprague Dawley rats (240–250 g)[2]
Dosage: 3 mg/kg
Administration: Injected intraperitoneally; 30 min before U69,593 administration
Result: Prevented behavioral and neuroendocrine effects caused by U69,593 in cocaine-naïve rats.
Molecular Weight

408.44

Formula

C24H22F2N2O2
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

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

Ethanol : 27.5 mg/mL (67.33 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4483 mL 12.2417 mL 24.4834 mL
5 mM 0.4897 mL 2.4483 mL 4.8967 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)

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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% EtOH    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.75 mg/mL (6.73 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (27.5 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 2

    Add each solvent one by one:  10% EtOH    90% Corn Oil

    Solubility: ≥ 2.75 mg/mL (6.73 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.75 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 EtOH stock solution (27.5 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)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

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
Ethanol 1 mM 2.4483 mL 12.2417 mL 24.4834 mL 61.2085 mL
5 mM 0.4897 mL 2.4483 mL 4.8967 mL 12.2417 mL
10 mM 0.2448 mL 1.2242 mL 2.4483 mL 6.1209 mL
15 mM 0.1632 mL 0.8161 mL 1.6322 mL 4.0806 mL
20 mM 0.1224 mL 0.6121 mL 1.2242 mL 3.0604 mL
25 mM 0.0979 mL 0.4897 mL 0.9793 mL 2.4483 mL
30 mM 0.0816 mL 0.4081 mL 0.8161 mL 2.0403 mL
40 mM 0.0612 mL 0.3060 mL 0.6121 mL 1.5302 mL
50 mM 0.0490 mL 0.2448 mL 0.4897 mL 1.2242 mL
60 mM 0.0408 mL 0.2040 mL 0.4081 mL 1.0201 mL
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LY2444296 Related Classifications

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:

LY24442961346133-11-6FP3FBZLY 2444296LY-2444296Opioid ReceptorKOPRInhibitorinhibitorinhibit

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