P-[(2R)-3-氨基-2-氟丙基]磷酸
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- CAS号:
- 344413-67-8
- 英文名:
- P-[(2R)-3-amino-2-fluoropropyl]Phosphinic acid
- 英文别名:
- AZD-3355;AR-H04966;AR-H061746;AR-H061719;AZ-11941831;Lesogaberan;Lesogaberan(AZD3355);LJNUIEQATDYXJH-GSVOUGTGSA-N;(R)-3-amino-2-fluoropropylphosphinic acid;P-[(2R)-3-amino-2-fluoropropyl]Phosphinic acid
- 中文名:
- P-[(2R)-3-氨基-2-氟丙基]磷酸
- 中文别名:
- 化合物 T15737;P-[(2R)-3-氨基-2-氟丙基]磷酸;AR-H04966;AR-H061719;AR-H061746;AZ-11941831;AZD-3355
- CBNumber:
- CB92473728
- 分子式:
- C3H9FNO2P
- 分子量:
- 141.08
- MOL File:
- 344413-67-8.mol
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P-[(2R)-3-氨基-2-氟丙基]磷酸化学性质
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沸点:
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306.1±52.0 °C(Predicted)
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储存条件:
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Store at -20°C
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酸度系数(pKa):
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2.52±0.10(Predicted)
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P-[(2R)-3-氨基-2-氟丙基]磷酸性质、用途与生产工艺
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。
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
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Cell Line:
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Human islet cells
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Concentration:
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3, 10, and 30 nM
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Incubation Time:
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4 days
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Result:
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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.
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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.
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Animal Model:
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Diabetic NOD/scid mice were implanted with human islets
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Dosage:
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0.08 mg/mL
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Administration:
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Oral feeding; 48 hours
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Result:
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Significantly reduced the percentages of apoptotic islet cells and increased the frequency of insulin
+
β-cells in human islet grafts.
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Animal Model:
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Female Sprague Dawley rats
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Dosage:
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7 μmol/kg (Pharmacokinetic Analysis)
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Administration:
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Oral
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Result:
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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.
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P-[(2R)-3-氨基-2-氟丙基]磷酸
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 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 |
P-[(2R)-3-氨基-2-氟丙基]磷酸
生产厂家
344413-67-8, P-[(2R)-3-氨基-2-氟丙基]磷酸 相关搜索:
- C3H9FNO2P
- AR-H04966;AR-H061719;AR-H061746;AZ-11941831;AZD-3355
- 化合物 T15737
- P-[(2R)-3-氨基-2-氟丙基]磷酸
- 344413-67-8
- AZ-11941831
- AR-H061746
- AR-H061719
- AR-H04966
- Phosphinic acid, P-[(2R)-3-amino-2-fluoropropyl]-
- AZD-3355
- (R)-3-amino-2-fluoropropylphosphinic acid
- LJNUIEQATDYXJH-GSVOUGTGSA-N
- Lesogaberan(AZD3355)
- Lesogaberan
- P-[(2R)-3-amino-2-fluoropropyl]Phosphinic acid