P-[(2R)-3-氨基-2-氟丙基]磷酸
![P-[(2R)-3-氨基-2-氟丙基]磷酸 结构式](https://img.chemicalbook.com/CAS/GIF/344413-67-8.gif)
P-[(2R)-3-氨基-2-氟丙基]磷酸 性质
| 沸点 | 306.1±52.0 °C(Predicted) |
|---|---|
| 储存条件 | Store at -20°C |
| 酸度系数(pKa) | 2.52±0.10(Predicted) |
P-[(2R)-3-氨基-2-氟丙基]磷酸 用途与合成方法
Ki: 5.1±1.2 nM (rat GABA B ), 1.4±0.3 μM (rat GABA A ) EC50: 8.6±0.77 nM (human GABA B receptor)
Lesogaberan (3-30 nM) enhances human islet cell proliferation in vitro.
Cell Proliferation Assay
| Cell Line: | Human islet cells |
| Concentration: | 3, 10, and 30 nM |
| Incubation Time: | 4 days |
| Result: | 3 nM had a small but nonsignificant promitotic effect, while treatment at higher dosages (10 and 30 nM) led to a 2-3-fold increase in proliferation relative to that of islets cultured in medium alone. |
Lesogaberan (AZD3355) potently stimulates recombinant human GABA
B
receptors and inhibits transient lower esophageal sphincter relaxation (TLESR) in dogs, with a biphasic dose-response curve.
Oral Lesogaberan (0.08 mg/mL; 48 hours) protects human islet β-cells from apoptosis in islet grafts in mice.
Lesogaberan (7 μmol/kg) shows high oral availability (88% in the dog and 100% in the rat) and relatively low systemic clearance in female SpragueDawley rats.
| Animal Model: | Diabetic NOD/scid mice were implanted with human islets |
| Dosage: | 0.08 mg/mL |
| Administration: | Oral feeding; 48 hours |
| Result: | Significantly reduced the percentages of apoptotic islet cells and increased the frequency of insulin + β-cells in human islet grafts. |
| Animal Model: | Female Sprague Dawley rats |
| Dosage: | 7 μmol/kg (Pharmacokinetic Analysis) |
| Administration: | Oral |
| Result: | High oral availability (88% in the dog and 100% in the rat) and relatively low systemic clearance. Plasma protein binding was 1% in rat and human plasma. |
P-[(2R)-3-氨基-2-氟丙基]磷酸 价格(试剂级)
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2023-03-20 | HY-10061 | P-[(2R)-3-氨基-2-氟丙基]磷酸 | 344413-67-8 | 5mg | 4000 |
| 2023-03-20 | HY-10061 | P-[(2R)-3-氨基-2-氟丙基]磷酸 | 344413-67-8 | 10mg | 6800 |
