ARN19702 |
Catalog No.GC63794
One-Click Copy Product Info
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ARN19702는 인간 NAAA에 대해 IC50이 230nM인 선택적, 경구 활성, 가역적, 뇌 침투성 N-아실에탄올아민 산 아미다제(NAAAA) 억제제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1971937-18-4
Sample solution is provided at 25 µL, 10mM.
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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[1][2].
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. Cmax (ng/mL)1660±166613±68 Tmax (min)(5.0)30 CL (mL/min/Kg)33.2±1.649±8 t1/2 (min)73.9±3.7104±16 AUCplasma (h×ng/mL)1366.8±68.3988±157 AUCbrain (h×ng/mL)404.3±109.1181±28 F (%)-72±11
[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.
[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.
| Cas No. | 1971937-18-4 | SDF | |
| Formula | C21H22FN3O3S2 | M.Wt | 447.55 |
| Solubility | DMSO : 100 mg/mL (223.44 mM; Need ultrasonic) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2344 mL | 11.1719 mL | 22.3439 mL |
| 5 mM | 446.9 μL | 2.2344 mL | 4.4688 mL |
| 10 mM | 223.4 μL | 1.1172 mL | 2.2344 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >97.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 24 reference(s) in Google Scholar.)