| CAS NO: | 101155-02-6 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 询价 |
| 10mg | 询价 |
| 25mg | 询价 |
| 50mg | 询价 |
| 100mg | 询价 |
| 250mg | 询价 |
| 500mg | 询价 |
| Molecular Weight (MW) | 257.27 |
|---|---|
| Formula | C13H12FN5 |
| CAS No. | 101155-02-6 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: ≥ 120 mg/mL |
| Water: N/A | |
| Ethanol: N/A | |
| Chemical Name | 9-((2-Fluorophenyl)methyl)-N-methyl-9H-purin-6-amine |
| Synonyms | BW A78U; BW-A 78U; BW-A78U |
| In Vitro | In vitro activity: BW-A 78U is a novel and potent PDE4 inhibitor with an IC50 of 3 μM. BW-A 78U fails to significantly inhibit arachidonate release. BW-A 78U is ineffective to inhibit the lipopolysaccharide (LPS)-induced TNF-α release. Kinase Assay: BW-A 78U is a novel and potent PDE4 inhibitor with an IC50 of 3 μM. Cell Assay: Mononuclear cells are incubated for 30 min with BW-A 78U at the concentration of 10 nM to 10 μM. The cells are then stimulated with lipopolysaccharide (10 μg/mL) overnight at 37°C in an atmosphere of 5% CO2 at 100% humidity. Cell-free supernatants are collected, centrifuged (2000 g), and stored frozen at -20°C before TNF-α determination. TNF-α concentrations in cell culture supernatants are determined by specific ELISA using a commercial kit. Sensitivity of the assay is 1 pg/mL. The absorbance at 450 nm is assessed with an ELISA reader. |
|---|---|
| In Vivo | The most effective compounds in vitro (RP 73401 and NCS 613) were further investigated in vivo. Both PDE inhibitors dose dependently (1, 10, and 30 mg/kg per os) inhibited the recruitment of neutrophils in the bronchoalveolar lavage fluid of mice exposed to endotoxin via aerosol. Significant differences were observed with 10 and 30 mg/kg RP 73401 and 30 mg/kg NCS 613. In rats, RP 73401, but not NCS 613, significantly increased basal acid secretion at 30 mg/kg i.v. and pentagastrin-stimulated acid secretion at 0.3, 1, and 10 mg/kg. These results demonstrate that the compounds derived from 9-benzyladenine, namely NCS 613, elicit anti-inflammatory activities. It is also suggested that their activities have been mediated through the inhibition of PDE4 isoenzyme. The fact that NCS 613 did not stimulate the gastric acid secretion suggests that this compound may produce fewer gastrointestinal side effects than second-generation PDE4 inhibitors, such as RP 73401. |
| Animal model | Rats |
| Formulation & Dosage | 0.3, 1, and 10 mg/kg; i.v |
| References | J Pharmacol Exp Ther. 2000 Feb;292(2):647-53. |
| 维奥蛋白资源库 - 中文蛋白资源 CopyRight © 2010-2024 |