| Identification | Back Directory | [Name]
CAY10640 | [CAS]
1208549-68-1 | [Synonyms]
CAY10640
1-[1-(cyclopropanecarbonyl)piperidin-4-yl]-3-[4-(trifluoromethoxy)phenyl]urea | [Molecular Formula]
C17H20F3N3O3 | [MDL Number]
MFCD13413342 | [MOL File]
1208549-68-1.mol | [Molecular Weight]
371.35 |
| Chemical Properties | Back Directory | [Melting point ]
195-196 °C(Solv: ethyl acetate (141-78-6); hexane (110-54-3)) | [Boiling point ]
470.8±45.0 °C(Predicted) | [density ]
1.37±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMF: 5 mg/ml; DMSO: 5 mg/ml; DMSO:PBS(pH7.2) (1:1): 0.5 mg/ml; Ethanol: 2 mg/ml; PBS (pH 7.2): Isoluble | [form ]
A crystalline solid | [pka]
13.11±0.20(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
Soluble epoxide hydrolase (sEH) inhibitors have important therapeutic use by increasing the in vivo concentration of EETs and other fatty acid epoxides, resulting in anti-inflammatory, antihypertensive, neuroprotective, and cardioprotective effects. CAY10640 is a 1-aryl-3-(1-acylpiperidin-4-yl)urea analog that inhibits recombinant human and mouse sEH with IC50 values both equal to 0.4 nM.1 CAY10640 demonstrates a 1,000-fold increase in potency compared to morphine in reducing hyperalgesia in an in vivo carrageenan-induced inflammatory pain model.1 | [Uses]
sEH inhibitor-1 (compound TCPU ) is a potent and oral active inhibitor of sEH (soluble epoxide hydrolase) with IC50s of 0.4 and 5.3 nM in human and murine, respectively[1]. | [in vivo]
Pharmacokinetic parameters of sEH inhibitor-1 (TCPU) after oral gavage with a non-compartmental analysis[1].
| Doses (mg/kg) | Cmaxa (nmol/L) | Tmax (h)a | AUCt (uM h)a | MRT (h)a | | 0.1 (0.27d) | 270±120 | 5.3±1.2 | 2.2±1.1 | 18.9±6.6 | | 0.3 (0.81d) | 1680±1170 | 4.7±1.2 | 16.6±8.8 | 16.9±5.4 | | 1.0 (2.69d) | 2560±95 | 3.2±2.2 | 43.8±5.1 | 24.0±1.8 | | 3.0 (8.08d) | 5160±265 | 3.9±2.5 | 94.3±8.0 | 32.1±5.6 |
a: T max, the time of maximum concentration; C max, the maximum blood concentration; MRT, the mean residence time; and AUC t, area under the concentration-time curve to terminal time. Additional PK parameters with non-compartmental model are presented in Table S3.
d: The dose with the unit of μmol/kg.
| [storage]
Store at -20°C | [References]
1. Rose, T.E., Morisseau, C., Liu, J.Y., et al. 1-aryl-3-(1-acylpiperidin-4-yl)urea inhibitors of human and murine soluble epoxide hydrolase: Structure-activity relationships, pharmacokinetics, and reduction of inflammatory pain J. Med. Chem. 53(19),7067-7075(2010). |
|
| Company Name: |
BOC Sciences
|
| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
| Company Name: |
amyjet
|
| Tel: |
4006800868;027-59626688 18371453821;18771149750 |
| Website: |
http://www.amyjet.com/ |
|