P-[(2R)-3-氨基-2-氟丙基]磷酸
中文名称 | P-[(2R)-3-氨基-2-氟丙基]磷酸 |
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中文同义词 | P-[(2R)-3-氨基-2-氟丙基]磷酸;化合物 T15737 |
英文名称 | P-[(2R)-3-amino-2-fluoropropyl]Phosphinic acid |
英文同义词 | P-[(2R)-3-amino-2-fluoropropyl]Phosphinic acid;Lesogaberan;Lesogaberan(AZD3355);LJNUIEQATDYXJH-GSVOUGTGSA-N;(R)-3-amino-2-fluoropropylphosphinic acid;AZD-3355;Phosphinic acid, P-[(2R)-3-amino-2-fluoropropyl]- |
CAS号 | 344413-67-8 |
分子式 | C3H9FNO2P |
分子量 | 141.08 |
EINECS号 | |
相关类别 | |
Mol文件 | 344413-67-8.mol |
结构式 | ![]() |
P-[(2R)-3-氨基-2-氟丙基]磷酸 性质
沸点 | 306.1±52.0 °C(Predicted) |
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储存条件 | Store at -20°C |
酸度系数(pKa) | 2.52±0.10(Predicted) |
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. |
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2023/03/20 | HY-10061 | P-[(2R)-3-氨基-2-氟丙基]磷酸 Lesogaberan | 344413-67-8 | 5mg | 4000元 |
2023/03/20 | HY-10061 | P-[(2R)-3-氨基-2-氟丙基]磷酸 Lesogaberan | 344413-67-8 | 10mg | 6800元 |