| CAS NO: | 1515856-92-4 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| Molecular Weight (MW) | 366.33 |
|---|---|
| Formula | C18H17F3N2O3 |
| CAS No. | 1515856-92-4 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 80 mg/mL (218.4 mM) |
| Water: <1 mg/mL | |
| Ethanol: 34 mg/mL (92.8 mM) | |
| Other info | Chemical Name: (S)-2-(3-(pyridin-2-ylmethoxy)pyrrolidin-1-yl)-5-(trifluoromethyl)benzoic acid InChi Key: NBGRERFNOKZQLO-AWEZNQCLSA-N InChi Code: InChI=1S/C18H17F3N2O3/c19-18(20,21)12-4-5-16(15(9-12)17(24)25)23-8-6-14(10-23)26-11-13-3-1-2-7-22-13/h1-5,7,9,14H,6,8,10-11H2,(H,24,25)/t14-/m0/s1 SMILES Code: O=C(O)C1=CC(C(F)(F)F)=CC=C1N2C[C@@H](OCC3=NC=CC=C3)CC2 |
| Synonyms | XEN445; XEN 445; XEN-445 |
| In Vitro | In vitro activity: XEN445 shows good in vitro inhibitory potency against EL, and high selectivity over LPL and HL. Cell Assay: In vitro, XEN445 has been reported to selectively inhibit EL with IC50 values of 0.237μM, 20μM and 9.5μM for hEL, hLPL and hHL, respectively. In addition, XEN445 has been revealed to suppress EL in EL-transfected HEK cells with an IC50 value of 0.25μM which is very similar to that tested in cell-free assay. Besides, XEN445 has shown significantly high oral bioavailability and low clearance rates in C57BL6 mice. |
|---|---|
| In Vivo | In vivo, XEN445 displays good ADME and PK properties. In mice, XEN445 (30 mg/kg, p.o.) raises plasma HDL-cholesterol concentration. |
| Animal model | Male EL knockout mice and age-matched wild-type male C57BL6 mice |
| Formulation & Dosage | Formulated in 0.2% Tween-20/1% carboxymethyl-cellulose; 30 mg/kg bid; p.o. |
| References | Bioorg Med Chem. 2013 Dec 15;21(24):7724-34. |
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