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Purity: ≥98%
URB597 (also known as KDS4103, URB-597; KDS-4103) is a novel, potent, selective, orally bioavailable fatty acid amide hydrolase (FAAH) inhibitor with antidepressant and analgesic activity. It inhibits FAAH with IC50 of 4.6 nM, it has no activity on other cannabinoid-related targets. In pre-clinical laboratory tests, researchers found URB597 increased the production of endocannabinoids resulting in measurable antidepressant and analgesic effects.
| ln Vitro |
At an IC50 value of approximately 0.50 nM, URB-597 (KDS-4103) inhibits the hydrolysis of [3H]anandamide by primary cultures of rat cortical neurons, which is catalyzed by FAAH[1].
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| ln Vivo |
In rodents that are either FAAH-null (-/-) or wild-type (+/+), URB-597 (KDS-4103) suppresses rat brain FAAH activity following intraperitoneal (ip) treatment at a median inhibitory dosage (ID50) of 0.15 mg/kg[1]. Treatment with CB1 receptor antagonists prevents the strong anxiolytic, antidepressant, and analgesic effects that KDS-4103 (0.1-0.3 mg/kg, ip) elicits in rats and mice[1]. Rats and cynomolgus monkeys may consume KDS-4103 orally[1]. After taking 10 mg/kg orally, URB-597 inhibits FAAH in the brain quickly (about an hour), maintaining >90% through 12 hours, and >60% through 24 hours.
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| Animal Protocol |
Animal/Disease Models: Wistar rats[1]
Doses: 250, 500, 750, 1000, 1250 mg/kg (pharmacokinetic/PK Analysis) Route of Administration: Oral administration Experimental Results: Absorbed at a moderate rate with peak plasma concentrations (Cmax) achieved at 1.2 h after treatment. The oral elimination half-life was approximately 2 h. |
| References |
[1]. Daniele Piomelli, et al. Pharmacological profile of the selective FAAH inhibitor KDS-4103 (URB597). CNS Drug Rev. Spring 2006;12(1):21-38.
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| Molecular Formula |
C20H22N2O3
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| Molecular Weight |
338.4
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| CAS # |
546141-08-6
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| SMILES |
O(C1=C([H])C([H])=C([H])C(C2C([H])=C([H])C([H])=C(C(N([H])[H])=O)C=2[H])=C1[H])C(N([H])C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C1([H])[H])=O
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 10 mg/mL (29.55 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 100.0 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 (7.39 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 (7.39 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 30% propylene glycol, 5% Tween 80, 65% D5W: 30mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9551 mL | 14.7754 mL | 29.5508 mL | |
| 5 mM | 0.5910 mL | 2.9551 mL | 5.9102 mL | |
| 10 mM | 0.2955 mL | 1.4775 mL | 2.9551 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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