P-[(2R)-3-氨基-2-氟丙基]磷酸
- CAS号:344413-67-8
- 英文名:P-[(2R)-3-amino-2-fluoropropyl]Phosphinic acid
- 中文名:P-[(2R)-3-氨基-2-氟丙基]磷酸
- CBNumber:CB92473728
- 分子式:C3H9FNO2P
- 分子量:141.08
- MOL File:344413-67-8.mol
- 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]磷酸性质、用途与生产工艺
- 生物活性 Lesogaberan (AZD-3355) 是一种有效的选择性 GABAB 受体激动剂,对人重组 GABAB 受体的 EC50 为 8.6 nM。对大鼠脑 GABAB 和 GABAA 受体的结合亲和力 (Ki) 分别为 5.1 nM 和 1.4 μM。
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靶点
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)
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体外研究
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. -
体内研究
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.
- 更新日期:2023/03/20
- 产品编号:HY-10061
- 产品名称:P-[(2R)-3-氨基-2-氟丙基]磷酸 Lesogaberan
- CAS编号:344413-67-8
- 包装:5mg
- 价格:4000元
- 更新日期:2023/03/20
- 产品编号:HY-10061
- 产品名称:P-[(2R)-3-氨基-2-氟丙基]磷酸 Lesogaberan
- CAS编号:344413-67-8
- 包装:10mg
- 价格:6800元
- 公司名称:TargetMol Chemicals Inc.
- 联系电话:+1-781-999-5354 +1-00000000000
- 电子邮件:marketing@targetmol.com
- 国家:美国
- 产品数:19892
- 优势度:58
- 公司名称:MedChemExpress
- 联系电话:--
- 电子邮件:sales@medchemexpress.com
- 国家:美国
- 产品数:6398
- 优势度:58