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| 5mg |
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| 25mg |
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Purity: ≥98%
JNJ-1661010 (JNJ 1661010; Takeda-25; JNJ1661010; Takeda25), a piperazinyl phenyl urea compound, is a selective and reversible inhibitor of Fatty acid amide hydrolase/FAAH with important biological activity. It inhibits FAAH with an IC50 of 10 nM (rat) and 12 nM (human),and exhibits >100-fold selectivity for FAAH-1 over FAAH-2. JNJ-1661010 is structurally distinct from alkylcarbamic acid esters and α–ketoheterocyclic compounds. JNJ-1661010 is a brain penetrant and active in vivo, and thus has been used to examine the contribution of endocannabinoid signaling in experimental fibrosis.
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In the inflammatory rat carrageenan paw model, JNJ-1661010 (Takeda-25; ip; 50 mg/kg) reduces thermal hyperalgesia[2]. T1/2 for JNJ-1661010 (ip; 10 mg/kg) in rats is 35 minutes, CL is 0.032 mL/min/kg, and Cmax is 1.58 μM[1].
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| Animal Protocol |
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| References |
[1]. Keith JM, et al. Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase. Bioorg Med Chem Lett. 2008 Sep 1;18(17):4838-43.
[2]. Karbarz MJ, et al. Biochemical and biological properties of 4-(3-phenyl-[1,2,4] thiadiazol-5-yl)-piperazine-1-carboxylicacid phenylamide, a mechanism-based inhibitor of fatty acid amide hydrolase. Anesth Analg. 2009 Jan;108(1):316-29. |
| Molecular Formula |
C19H19N5OS
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| Molecular Weight |
365.45
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| CAS # |
681136-29-8
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| Related CAS # |
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| SMILES |
S1C(=NC(C2C([H])=C([H])C([H])=C([H])C=2[H])=N1)N1C([H])([H])C([H])([H])N(C(N([H])C2C([H])=C([H])C([H])=C([H])C=2[H])=O)C([H])([H])C1([H])[H]
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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: ≥ 2.5 mg/mL (6.84 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.84 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. View More
Solubility in Formulation 3: 5% DMSO+95% Corn oil:5mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7364 mL | 13.6818 mL | 27.3635 mL | |
| 5 mM | 0.5473 mL | 2.7364 mL | 5.4727 mL | |
| 10 mM | 0.2736 mL | 1.3682 mL | 2.7364 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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