Size | Price | Stock | Qty |
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50mg |
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100mg |
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500mg |
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1g |
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Other Sizes |
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ln Vivo |
ARN19702 (3-10 mg/kg; oral; daily; for 7 days) reduces nociception associated with paclitaxel-induced neuropathy without inducing subacute antinociceptive tolerance in male rats [1] . In male mice, ARN19702 (0.1-30 mg/kg; p.o.) dose-dependently attenuates the spontaneous nociceptive response induced by intraplantar injection of formalin as well as intraplantar injection of carrageenan, paw incision, or sciatic nerve Hypersensitivity reaction caused by ligation[1]. ..ARN19702 (3-10 mg/kg; oral) exerts significant protective effects against multiple sclerosis in mice [2]. Pharmacokinetic properties of ARN19702 in mice 3 mg/kg, iv 3 mg/kg, po Cmax (ng/mL) 1660±166 613±68 Tmax (min) (5.0) 30 CL (mL/min/Kg ) 33.2±1.6 49 ±8 t1/2 (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
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Animal Protocol |
Animal/Disease Models: SD (SD (Sprague-Dawley)) rats (200-220 g) injected with paclitaxel [1]
Doses: 3 mg/kg and 10 mg/kg Route of Administration: Oral; injection. Daily; 7 days in a row (subchronic) Experimental Results: diminished nociception associated with paclitaxel-induced neuropathy. |
References |
[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. |
Molecular Formula |
C21H22FN3O3S2
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Molecular Weight |
447.543
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Exact Mass |
447.11
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Elemental Analysis |
C, 56.36; H, 4.96; F, 4.25; N, 9.39; O, 10.72; S, 14.33
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CAS # |
1971937-18-4
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Appearance |
Solid powder
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SMILES |
FC1=CC2=C(N=C(N3C[C@H](C)N(C(C4=CC=CC=C4S(CC)(=O)=O)=O)CC3)S2)C=C1
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InChi Key |
UKQOLPNYRVPCBM-AWEZNQCLSA-N
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InChi Code |
InChI=1S/C21H22FN3O3S2/c1-3-30(27,28)19-7-5-4-6-16(19)20(26)25-11-10-24(13-14(25)2)21-23-17-9-8-15(22)12-18(17)29-21/h4-9,12,14H,3,10-11,13H2,1-2H3/t14-/m0/s1
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Chemical Name |
(S)-(2-(ethylsulfonyl)phenyl)(4-(6-fluorobenzo[d]thiazol-2-yl)-2-methylpiperazin-1-yl)methanone
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Synonyms |
ARN19702; ARN 19702; ARN-19702;
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : ~100 mg/mL (~223.44 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.59 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.59 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.59 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.2344 mL | 11.1722 mL | 22.3444 mL | |
5 mM | 0.4469 mL | 2.2344 mL | 4.4689 mL | |
10 mM | 0.2234 mL | 1.1172 mL | 2.2344 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.