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

LY2444296 (Synonyms: FP3FBZ)

Cat. No.: HY-135230 Purity: 99.78%
Handling Instructions

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.

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

LY2444296 Chemical Structure

LY2444296 Chemical Structure

CAS No. : 1346133-11-6

Size Price Stock Quantity
5 mg USD 80 In-stock
Estimated Time of Arrival: December 31
10 mg USD 150 In-stock
Estimated Time of Arrival: December 31
50 mg USD 600 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1100 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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].

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.

1346133-11-6

SMILES

O=C(N)C1=CC=C(OC2=CC=C(CN3[[email protected]](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 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

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

Methanol : 5 mg/mL (12.24 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
10 mM 0.2448 mL 1.2242 mL 2.4483 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 2.

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

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

*All of the co-solvents are provided by MCE.
References
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Keywords:

LY2444296FP3FBZLY 2444296LY-2444296Opioid ReceptorKOPRInhibitorinhibitorinhibit

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Product name:
LY2444296
Cat. No.:
HY-135230
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