P-[(2R)-3-氨基-2-氟丙基]磷酸 CAS#: 344413-67-8

P-[(2R)-3-氨基-2-氟丙基]磷酸

生物活性靶点体外研究体内研究用途与合成方法 MSDS P-[(2R)-3-氨基-2-氟丙基]磷酸价格(试剂级) 上下游产品信息

中文名称	P-[(2R)-3-氨基-2-氟丙基]磷酸
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)
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

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。

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)

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.

安全信息

MSDS信息

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 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