URB937
Based on 1 Customer Validation
URB937 is an orally active and peripherally restricted FAAH inhibitor (IC50=26.8 nM) and increases anandamide levels. URB937 fails to affect FAAH activity in the brain (not penetrate the blood-brain barrier).
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- Pureza: 99.62%
- No. CAS: 1357160-72-5
- Fòrmula: C20H22N2O4
- Peso molecular:354.40
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
IC50: 26.8 nM (FAAH)[1].
URB937 is actively extruded from the CNS by the ATP-binding cassette (ABC) membrane transporter, Abcg2[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
URB937 (1 mg/kg, s.c.) suppresses pain responses elicited by i.p. injections of acetic acid[1].
URB937 in male rats (an oral dose 3 mg/kg, F = 36%) is absorbed at a moderate rate and displays a peak plasma concentration (Cmax) of 159.47 ng/ml, which was achieved one hour after administration. URB937 exhibits T1/2 of 60 min by an oral dose of 3 mg/kg[2].
URB937 produces a high degree of antinociception in female mice and rats in models of visceral and inflammatory pain. Moreover, the compound displayed a restricted access to placental and fetal tissues in pregnant mice and rats[3].
URB937 (1 mg/kg, every 2 days for 30 days) attenuates radiation-induced lung injury and increased endocannabinoid concentration in lung tissue[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Swiss Webster mice[1].
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Dosage:1 mg/kg.
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Administration:S.C.
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Result:Suppressesd pain responses elicited by i.p. injections of acetic acid.
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Animal Model:Adult Sprague Dawley male and female rats (250-300 g)[2].
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Dosage:0.3, 1, 3, 10 mg/kg (Pharmacokinetic Analysis).
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Administration:Single oral dose.
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Result:Inhibited liver FAAH activity with a median effective dose (ED50) of 0.9 mg/kg.
Inhibits FAAH in peripheral tissues and identify a possible biomarker for target engagement.
Chemical Information
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No. CAS 1357160-72-5
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Appearance Solid
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Peso molecular 354.40
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Fòrmula C20H22N2O4
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Color Off-white to light yellow
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SMILES
O=C(OC1=CC(C2=CC=CC(C(N)=O)=C2)=C(O)C=C1)NC3CCCCC3
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : ≥ 100 mg/mL (282.17 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.05 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.05 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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (273 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Jason R Clapper, et al. Anandamide suppresses pain initiation through a peripheral endocannabinoid mechanism. Nat Neurosci. 2010 Oct;13(10):1265-70. [Content Brief]
[2]. Valentina Vozella, et al. Pharmacokinetics, pharmacodynamics and safety studies on URB937, a peripherally restricted fatty acid amide hydrolase (FAAH) inhibitor, in rats. J Pharm Pharmacol. 2019 Dec;71(12):1762-1773. [Content Brief]
[3]. G Moreno-Sanz, et al. Pharmacological characterization of the peripheral FAAH inhibitor URB937 in female rodents: interaction with the Abcg2 transporter in the blood-placenta barrier. Br J Pharmacol. 2012 Dec;167(8):1620-8. [Content Brief]
[4]. Rui Li, et al. The Fatty Acid Amide Hydrolase Inhibitor URB937 Ameliorates Radiation-Induced Lung Injury in a Mouse Model. Inflammation. 2017 Aug;40(4):1254-1263. [Content Brief]
Complete Stock Solution Preparation Table
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.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.8217 mL | 14.1084 mL | 28.2167 mL | 70.5418 mL |
| 5 mM | 0.5643 mL | 2.8217 mL | 5.6433 mL | 14.1084 mL | |
| 10 mM | 0.2822 mL | 1.4108 mL | 2.8217 mL | 7.0542 mL | |
| 15 mM | 0.1881 mL | 0.9406 mL | 1.8811 mL | 4.7028 mL | |
| 20 mM | 0.1411 mL | 0.7054 mL | 1.4108 mL | 3.5271 mL | |
| 25 mM | 0.1129 mL | 0.5643 mL | 1.1287 mL | 2.8217 mL | |
| 30 mM | 0.0941 mL | 0.4703 mL | 0.9406 mL | 2.3514 mL | |
| 40 mM | 0.0705 mL | 0.3527 mL | 0.7054 mL | 1.7635 mL | |
| 50 mM | 0.0564 mL | 0.2822 mL | 0.5643 mL | 1.4108 mL | |
| 60 mM | 0.0470 mL | 0.2351 mL | 0.4703 mL | 1.1757 mL | |
| 80 mM | 0.0353 mL | 0.1764 mL | 0.3527 mL | 0.8818 mL | |
| 100 mM | 0.0282 mL | 0.1411 mL | 0.2822 mL | 0.7054 mL |
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