Cat. No.: HY-145339

ARN19702

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ARN19702 is a selective, orally active, reversible, and brain-penetrant N-acylethanolamine acid amidase (NAAA) inhibitor with an IC₅₀ of 230 nM for human NAAA. ARN19702 has pain relief effects.

Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.

Pureté: 99.69%
CAS No.: 1971937-18-4
Formule: C₂₁H₂₂FN₃O₃S₂
Masse moléculaire:447.55

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

ARN19702 Chemical Structure

CAS No.: 1971937-18-4

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Activité biologique
- Description
- IC₅₀ & Target
- In Vivo
Chemical Information
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

IC50: 230 nM (human NAAA)^[2]

In Vivo

ARN19702 (3-10 mg/kg; po; daily; for 7 consecutive days) reduces nociception associated with Paclitaxel-induced neuropathy without development of subacute antinociceptive tolerance in male rats^[1].
In male mice, ARN19702 (0.1-30 mg/kg; po) attenuates in a dose-dependent manner the spontaneous nocifensive response elicited by intraplantar formalin injection and the hypersensitivity caused by intraplantar carrageenan injection, paw incision, or sciatic nerve ligation^[1].
. ARN19702 (3-10 mg/kg; po) produces remarkable protective effects against multiple sclerosis in mice^[2].
Pharmacokinetic properties of ARN19702 in mice

	3 mg/kg,i.v	3 mg/kg, p.o.
C_max (ng/mL)	1660±166	613±68
T_max (min)	(5.0)	30
CL (mL/min/Kg)	33.2±1.6	49±8
t_1/2 (min)	73.9±3.7	104±16
AUC_plasma (h×ng/mL)	1366.8±68.3	988±157
AUC_brain (h×ng/mL)	404.3±109.1	181±28
F (%)	-	72±11

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

Animal Model:

Sprague-Dawley rats (200-220 g) injected with Paclitaxel^[1]
Dosage:

3 mg/kg and 10 mg/kg
Administration:

Oral administration; daily; for 7 consecutive days (sub-chronic)
Result:

Reduced nociception associated with Paclitaxel-induced neuropathy.

Chemical Information

CAS No. 1971937-18-4
Appearance Solid
Masse moléculaire 447.55
Formule C₂₁H₂₂FN₃O₃S₂
Color White to off-white
SMILES

C[C@H]1CN(CCN1C(C2=C(C=CC=C2)S(CC)(=O)=O)=O)C(SC3=C4)=NC3=CC=C4F
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (223.44 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2344 mL

11.1719 mL

22.3439 mL

5 mM

0.4469 mL

2.2344 mL

4.4688 mL

10 mM

0.2234 mL

1.1172 mL

2.2344 mL

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.59 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

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

Solubility: ≥ 2.5 mg/mL (5.59 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

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

Solubility: ≥ 2.5 mg/mL (5.59 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (275 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Yannick Fotio, et al. Antinociceptive Profile of ARN19702, (2-Ethylsulfonylphenyl)-[(2S)-4-(6-fluoro-1,3-benzothiazol-2-yl)-2-methylpiperazin-1-yl]methanone, a Novel Orally Active N-Acylethanolamine Acid Amidase Inhibitor, in Animal Models. J Pharmacol Exp Ther. 2021 Aug;378(2):70-76. [Content Brief]

[2]. Marco Migliore Dr, et al. Second-Generation Non-Covalent NAAA Inhibitors are Protective in a Model of Multiple Sclerosis. Angew Chem Int Ed Engl. 2016 Sep 5;55(37):11193-11197. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2344 mL	11.1719 mL	22.3439 mL	55.8597 mL
	5 mM	0.4469 mL	2.2344 mL	4.4688 mL	11.1719 mL
	10 mM	0.2234 mL	1.1172 mL	2.2344 mL	5.5860 mL
	15 mM	0.1490 mL	0.7448 mL	1.4896 mL	3.7240 mL
	20 mM	0.1117 mL	0.5586 mL	1.1172 mL	2.7930 mL
	25 mM	0.0894 mL	0.4469 mL	0.8938 mL	2.2344 mL
	30 mM	0.0745 mL	0.3724 mL	0.7448 mL	1.8620 mL
	40 mM	0.0559 mL	0.2793 mL	0.5586 mL	1.3965 mL
	50 mM	0.0447 mL	0.2234 mL	0.4469 mL	1.1172 mL
	60 mM	0.0372 mL	0.1862 mL	0.3724 mL	0.9310 mL
	80 mM	0.0279 mL	0.1396 mL	0.2793 mL	0.6982 mL
	100 mM	0.0223 mL	0.1117 mL	0.2234 mL	0.5586 mL

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ARN19702

Metabolism/Protease Compound Library

CNS-Penetrant Compound Library

Orally Active Compound Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

ARN19702

Metabolism/Protease Compound Library

CNS-Penetrant Compound Library

Orally Active Compound Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

ARN19702 Related Classifications

HY-145339 Related Classifications