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Purity: ≥98%
Desrciption: URB-937 is a potent and novel FAAH inhibitor and increases anandamide levels, with an IC50 of 26.8 nM. URB937 fails to affect FAAH activity in the brain.
| ln Vitro |
The CNS's ATP-binding cassette (ABC) membrane transporter Abcg2 actively extrudes URB937 [3].
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|---|---|
| ln Vivo |
Anandamide levels in peripheral organs are raised in mice administered URB937 (1 mg/kg, i.p.) but not in the forebrain or hypothalamus [1]. Acetic acid injected intraperitoneally (URB937, 1 mg/kg, subcutaneous injection) decreases the pain response [1]. After an hour of oral dosage (3 mg/kg, F = 36%), URB937 in male rats was absorbed at a moderate rate and reached its peak plasma concentration (Cmax) of 159.47 ng/ml. When taken orally, URB937 has a T1/2 of 60 minutes at a dose of 3 mg/kg [2]. In models of visceral pain and inflammatory pain, URB937 has strong analgesic effects in female mice and rats. Moreover, the substance only partially penetrates the placenta and fetal tissues of rats and mice undergoing pregnancy [3]. Increased endocannabinoid concentrations in lung tissue and decreased radiation-induced lung damage are two effects of URB937 (1 mg/kg every 2 days for 30 days) [4].
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| Animal Protocol |
Animal/Disease Models: Swiss Webster mouse[1].
Doses: 1 mg/kg. Route of Administration: SC Experimental Results: Inhibition of pain response induced by intraperitoneal (ip) injection of acetic acid. Animal/Disease Models: Adult Sprague Dawley male and female rats (250-300 g) [2]. Doses: 0.3, 1, 3, 10 mg/kg (pharmacokinetic/PK/PK analysis). Route of Administration: Single oral dose. Experimental Results: Inhibited liver FAAH activity, the half effective dose (ED50) was 0.9 mg/kg. Inhibit FAAH in peripheral tissues and identify possible biomarkers of target engagement. |
| References |
[1]. Jason R Clapper, et al. Anandamide suppresses pain initiation through a peripheral endocannabinoid mechanism. Nat Neurosci. 2010 Oct;13(10):1265-70.
[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. [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. [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. |
| Molecular Formula |
C20H22N2O4
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|---|---|
| Molecular Weight |
354.406
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| Exact Mass |
354.158
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| Elemental Analysis |
C, 67.78; H, 6.26; N, 7.90; O, 18.06
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| CAS # |
1357160-72-5
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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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| InChi Key |
CMEQHOXCIGFZNJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H22N2O4/c21-19(24)14-6-4-5-13(11-14)17-12-16(9-10-18(17)23)26-20(25)22-15-7-2-1-3-8-15/h4-6,9-12,15,23H,1-3,7-8H2,(H2,21,24)(H,22,25)
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| Chemical Name |
3'-carbamoyl-6-hydroxy-[1,1'-biphenyl]-3-yl cyclohexylcarbamate
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| Synonyms |
URB937 URB-937 URB 937
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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 : ~250 mg/mL (~705.42 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.87 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 20.8 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: ≥ 2.08 mg/mL (5.87 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 20.8 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: ≥ 2.08 mg/mL (5.87 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 | 2.8216 mL | 14.1080 mL | 28.2159 mL | |
| 5 mM | 0.5643 mL | 2.8216 mL | 5.6432 mL | |
| 10 mM | 0.2822 mL | 1.4108 mL | 2.8216 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.
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