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Aticaprant

Name: Aticaprant
Brand: TargetMol
SKU: TQ0082
Price: 34 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. TQ0082Cas No. 1174130-61-0

Alias LY-2456302, CERC-501

Aticaprant (CERC-501) is a potent and centrally-penetrant antagonist of the kappa-opioid receptor (Ki: 0.807 nM).[2]

Aticaprant

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Purity: 99.97%

Catalog No. TQ0082Alias LY-2456302, CERC-501Cas No. 1174130-61-0

Aticaprant (CERC-501) is a potent and centrally-penetrant antagonist of the kappa-opioid receptor (Ki: 0.807 nM).[2]

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$34	In Stock	In Stock
2 mg	$48	In Stock	In Stock
5 mg	$80	In Stock	In Stock
10 mg	$128	In Stock	In Stock
25 mg	$272	In Stock	In Stock
50 mg	$428	In Stock	In Stock
100 mg	$639	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$89	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.97%

Appearance:Solid

Color:White

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COA LCMS HNMR

Product Introduction

Bioactivity

Description	Aticaprant (CERC-501) is a potent and centrally-penetrant antagonist of the kappa-opioid receptor (Ki: 0.807 nM).[2]
Targets&IC50	κ opioid:0.807 nM (Ki)
In vitro	Aticaprant(CERC-501) 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(CERC-501) shows no appreciable affinity for several non-opioid cell surface G-protein-coupled receptor targets [1].
In vivo	METHODS: Mice were given Aticaprant(CERC-501) (0.1 to 3 mg/kg, intraperitoneal injection) 30 minutes before the alcohol deprivation effect (ADE) test and naltrexone (0.3 or 1 mg/kg, intraperitoneal injection) 10 minutes before the test to observe the effect of aticaprant on the ADE effect. RESULTS 0.3 mg/kg of Aticaprant(CERC-501) and 1 mg/kg of naltrexone reduced the ADE alcohol intake of mice at 4 hours. [1]
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

Chemical Properties

Molecular Weight	418.5
Formula	C₂₆H₂₇FN₂O₂
Cas No.	1174130-61-0
Smiles	Cc1cc(C)cc(c1)[C@@H]1CCCN1Cc1ccc(Oc2ccc(cc2F)C(N)=O)cc1
Relative Density.	1.201 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 100 mg/mL (238.95 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (9.56 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.3895 mL	11.9474 mL	23.8949 mL	119.4743 mL
5 mM	0.4779 mL	2.3895 mL	4.7790 mL	23.8949 mL
10 mM	0.2389 mL	1.1947 mL	2.3895 mL	11.9474 mL
20 mM	0.1195 mL	0.5974 mL	1.1947 mL	5.9737 mL
50 mM	0.0478 mL	0.2389 mL	0.4779 mL	2.3895 mL
100 mM	0.0239 mL	0.1195 mL	0.2389 mL	1.1947 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

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

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