| Identification | Back Directory | [Name]
1-[(1-Acetylpiperidin-4-yl)-3-adamantan-1-yl]urea | [CAS]
913548-29-5 | [Synonyms]
APAU
AR-9281
Apau (enzyme inhibitor)
1-(1-acetylpiperidin-4-yl)-3-(1-adamantyl)urea
1-[(1-Acetylpiperidin-4-yl)-3-adamantan-1-yl]urea
AR-9281; AR 9281; AR9281; APAU (ENZYME INHIBITOR);
Urea, N-(1-acetyl-4-piperidinyl)-N'-tricyclo[3.3.1.13,7]dec-1-yl-
inflammation,AR-9281,AR9281,hypertension,MsEH,HsEH,Epoxide Hydrolase,soluble epoxide hydrolase (s-EH),oral,inhibit,Inhibitor,AR 9281,type 2 diabetes | [Molecular Formula]
C18H29N3O2 | [MDL Number]
MFCD22373766 | [MOL File]
913548-29-5.mol | [Molecular Weight]
319.44 |
| Chemical Properties | Back Directory | [Boiling point ]
554.1±39.0 °C(Predicted) | [density ]
1.19±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO:25.0(Max Conc. mg/mL);78.26(Max Conc. mM) | [form ]
Solid | [pka]
13.66±0.20(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
AR9281 (APAU) is a potent, selective and orally active soluble epoxide hydrolase (s-EH) inhibitor. AR-9281 can inhibits human sEH (HsEH) and murine sEH (MsEH) with IC50 values of 13.8 nM and 1.7 nM, respectively. AR9281 can be used for the research of inflammation, hypertension and type 2 diabetes[1][2]. | [in vivo]
AR-9281 (APAU) (oral, 150-200 mg/dL, for 6 weeks) enhances the therapeutic effects of EETs, slows progression of hyperglycemia, protects the myocyte structure, and reduces Ca2+ dysregulation and SERCA remodeling in hyperglycemic rats[2]. | Animal Model: | T2DM rat model[2] | | Dosage: | 150-200 mg/dL | | Administration: | oral(drinking), for 6 weeks | | Result: | Attenuated the progressive increase of blood glucose concentration and preserved mitochondrial structure and myofibril morphology in cardiac myocytes.
Protected the intracellular Ca2+ effector system.
Had less downregulation of sarco(endo)plasmic reticulum Ca2+ ATPase (SERCA) and lowed expression of hypertrophic markers.
|
| [References]
[1] Fangyu Du, et al. Discovery of memantyl urea derivatives as potent soluble epoxide hydrolase inhibitors against lipopolysaccharide-induced sepsis. Eur J Med Chem. 2021 Nov 5;223:113678. DOI:10.1016/j.ejmech.2021.113678
[2] Kathleen Guglielmino, et al. Pharmacological inhibition of soluble epoxide hydrolase provides cardioprotection in hyperglycemic rats. Am J Physiol Heart Circ Physiol. 2012 Oct 1;303(7):H853-62. DOI:10.1152/ajpheart.00154.2012 |
|
| Company Name: |
InvivoChem
|
| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
|