344413-67-8
基本信息
Lesogaberan
Lesogaberan(AZD3355)
LJNUIEQATDYXJH-GSVOUGTGSA-N
(R)-3-amino-2-fluoropropylphosphinic acid
P-[(2R)-3-amino-2-fluoropropyl]Phosphinic acid
Phosphinic acid, P-[(2R)-3-amino-2-fluoropropyl]-
物理化学性质
| 储存条件 | -20°C储存 |
安全数据
| 危险性符号(GHS) |  GHS07 |
| 警示词 | 警告 |
| 危险性描述 | H302-H412 |
| 防范说明 | P273-P501-P264-P270-P301+P312-P330-P501 |
P-[(2R)-3-氨基-2-氟丙基]磷酸价格(试剂级)
| 报价日期 | 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 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 |
| 2023/03/20 | HY-10061 | P-[(2R)-3-氨基-2-氟丙基]磷酸 Lesogaberan | 344413-67-8 | 25mg | 13500元 |
常见问题列表
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. |