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

Aticaprant (Synonyms: CERC-501; LY-2456302)

Cat. No.: HY-101718 Purity: 98.45%
Handling Instructions

Aticaprant (CERC-501) is a potent and centrally-penetrant kappa opioid receptor antagonist with a Ki of 0.807 nM.

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

Aticaprant Chemical Structure

Aticaprant Chemical Structure

CAS No. : 1174130-61-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 166 In-stock
Estimated Time of Arrival: December 31
1 mg USD 90 In-stock
Estimated Time of Arrival: December 31
5 mg USD 180 In-stock
Estimated Time of Arrival: December 31
10 mg USD 280 In-stock
Estimated Time of Arrival: December 31
20 mg USD 450 In-stock
Estimated Time of Arrival: December 31
50 mg USD 850 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

Aticaprant (CERC-501) is a potent and centrally-penetrant kappa opioid receptor antagonist with a Ki of 0.807 nM.

IC50 & Target

Ki: 0.807 nM (kappa opioid)[1]

In Vitro

Aticaprant (CERC-501) binds with high affinity to the human kappa opioid receptor with a 30-fold higher affinity over the human mu opioid receptor and 190-fold higher affinity over the human delta opioid receptor. Aticaprant (CERC-501) shows no appreciable affinity for several non-opioid cell surface G-protein-coupled receptor targets, including monoaminergic, muscarinic, cholinergic, and adrenergic receptors or ion channel/transporter binding targets or the central benzodiazepine binding site[1].

In Vivo

Aticaprant (CERC-501) has a rapid absorption (tmax=1-2 h) and good oral bioavailability (F=25%). Oral Aticaprant (CERC-501) administration selectively and potently occupies central kappa opioid receptors (ED50=0.33 mg/kg), without evidence of mu or delta receptor occupancy. LY2456302 potently blocks kappa-agonist-mediated analgesia and disruption of prepulse inhibition, without affecting mu-agonist-mediated effects at doses >30-fold higher. Aticaprant (CERC-501) produces antidepressant-like effects in the mouse forced swim test and enhances the effects of imipramine and citalopram. Aticaprant (CERC-501) reduces ethanol self-administration in alcohol-preferring rats[1]. Aticaprant (CERC-501) alleviates the nicotine withdrawal syndrome, as evidenced by decreased expression of nicotine withdrawal induced anxiety-related behavior, somatic signs, and CPA, and increased hotplate latency in nicotine withdrawn mice following pre-treatment[2].

Clinical Trial
Molecular Weight

418.50

Formula

C₂₆H₂₇FN₂O₂

CAS No.

1174130-61-0

SMILES

O=C(N)C1=CC=C(OC2=CC=C(CN3[[email protected]](C4=CC(C)=CC(C)=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: 

DMSO : ≥ 100 mg/mL (238.95 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3895 mL 11.9474 mL 23.8949 mL
5 mM 0.4779 mL 2.3895 mL 4.7790 mL
10 mM 0.2389 mL 1.1947 mL 2.3895 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 (5.97 mM); Clear solution

  • 2.

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

    Solubility: 2.5 mg/mL (5.97 mM); Suspended solution; Need ultrasonic

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (5.97 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Animal Administration
[1]

Rats: Three male cannulated rats are administered a single 1 mg/kg intravenous (IV) and 10 mg/kg oral (PO) dose of Aticaprant (CERC-501) to determine the pharmacokinetic parameters. Plasma samples are collected at 0.08 (IV only), 0.25, 0.5, 1, 2, 4, 8, 12 and 24 h post-dose and analyzed by liquid chromatography coupled to tandem mass spectral detection to determine the concentrations of Aticaprant (CERC-501)[1].

Mice: Male mice are administered a single 10 mg/kg PO dose of Aticaprant (CERC-501) to determine the pharmacokinetic parameters. Plasma samples are collected at 0.5, 1, 2, 4, 8, and 24 h post-dose and analyzed by LCeMS/MS to determine the concentrations of Aticaprant (CERC-501). The plasma and brain binding of Aticaprant (CERC-501) is determined by equilibrium dialysis at 1 μM[1].

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

References
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Keywords:

AticaprantCERC-501LY-2456302CERC501CERC 501LY2456302LY 2456302Opioid ReceptorInhibitorinhibitorinhibit

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