Home Tools
Log in
Cart

Aticaprant

Catalog No. TQ0082   CAS 1174130-61-0
Synonyms: LY-2456302, CERC-501

Aticaprant (LY-2456302) (CERC-501) is a potent and centrally-penetrant antagonist of the kappa-opioid receptor (Ki: 0.807 nM).

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
Aticaprant Chemical Structure
Aticaprant, CAS 1174130-61-0
Pack Size Availability Price/USD Quantity
1 mg In stock $ 34.00
2 mg In stock $ 48.00
5 mg In stock $ 80.00
10 mg In stock $ 128.00
25 mg In stock $ 272.00
50 mg In stock $ 428.00
100 mg In stock $ 639.00
1 mL * 10 mM (in DMSO) In stock $ 89.00
Bulk Inquiry
Get quote
Select Batch  
Purity: 99.93%
Purity: 99.53%
Contact us for more batch information
Biological Description
Chemical Properties
Storage & Solubility Information
Description Aticaprant (LY-2456302) (CERC-501) is a potent and centrally-penetrant antagonist of the kappa-opioid receptor (Ki: 0.807 nM).
Targets&IC50 κ opioid:0.807 nM (Ki)
In vitro Aticaprant binds with a high affinity to the human kappa opioid receptor with a 30-fold higher affinity over the human mu-opioid receptor and a 190-fold higher affinity over the human delta-opioid receptor. Aticaprant shows no appreciable affinity for several non-opioid cell surface G-protein-coupled receptor targets [1].
In vivo Aticaprant has rapid absorption (tmax=1-2 h) and good oral bioavailability (F=25%). Aticaprant selectively and potently occupies central kappa opioid receptors (ED50: 0.33 mg/kg, p.o.), 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 produces antidepressant-like effects in the mouse forced swim test and enhances the effects of imipramine and citalopram. Aticaprant reduces ethanol self-administration in alcohol-preferring rats [1]. Aticaprant 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withdrawal-induced anxiety-related behavior, somatic signs, and CPA, and increased hotplate latency in nicotine withdrawn mice following pre-treatment [2].
Animal Research Three male cannulated rats are administered a single 1 mg/kg intravenous (IV) and 10 mg/kg oral (PO) dose of Aticaprant 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). Male mice are administered a single 10 mg/kg PO dose of Aticaprant to determine the pharmacokinetic parameters. Plasma samples are collected at 0.5, 1, 2, 4, 8, and 24 h post-dose and analyzed by LCMS/MS to determine the concentrations of Aticaprant. The plasma and brain binding of Aticaprant is determined by equilibrium dialysis at 1 μM [1].
Synonyms LY-2456302, CERC-501
Molecular Weight 418.5
Formula C26H27FN2O2
CAS No. 1174130-61-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (238.95 mM)

TargetMolReferences and Literature

1. Rorick-Kehn LM, et al. LY2456302 is a novel, potent, orally-bioavailable small molecule kappa-selective antagonist with activity in animal models predictive of efficacy in mood and addictive disorders. Neuropharmacology. 2014 Feb;77:131-44. 2. Jackson KJ, et al. Effects of orally-bioavailable short-acting kappa opioid receptor-selective antagonist LY2456302on nicotine withdrawal in mice. Neuropharmacology. 2015 Oct;97:270-4.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Clinical Compound Library Anti-Neurodegenerative Disease Compound Library Anti-Cancer Drug Library Clinical Compound Library NO PAINS Compound Library Antidepressant Compound Library Neurotransmitter Receptor Compound Library Bioactive Compounds Library Max ReFRAME Related Library Neuronal Signaling Compound Library

Related Products

Related compounds with same targets
Leuphasyl TFA LY2940094 LY255582 [DPro10] Dynorphin A (1-11)acetate,porcine Nociceptin (1-13) amide TFA [Leu5]-Enkephalin acetate(58822-25-6 free base) AT-121 hydrochloride ICI 199,441 hydrochloride

TargetMolDose Conversion

You can also refer to dose conversion for different animals. More

TargetMol In vivo Formulation Calculator (Clear solution)

Step One: Enter information below
Dosage
mg/kg
Average weight of animals
g
Dosing volume per animal
ul
Number of animals
Step Two: Enter the in vivo formulation
% DMSO
%
% Tween 80
% ddH2O
Calculate Reset

TargetMolCalculator

Molarity Calculator
Dilution Calculator
Reconstitution Calculation
Molecular Weight Calculator
=
X
X

Molarity Calculator allows you to calculate the

  • Mass of a compound required to prepare a solution of known volume and concentration
  • Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Concentration of a solution resulting from a known mass of compound in a specific volume
See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

X
=
X

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

=
/

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Aticaprant 1174130-61-0 Endocrinology/Hormones GPCR/G Protein Neuroscience Opioid Receptor inhibit LY-2456302 CERC501 Inhibitor CERC 501 CERC-501 LY2456302 LY 2456302 inhibitor

 

TargetMol