344413-67-8

中文名称 P-[(2R)-3-氨基-2-氟丙基]磷酸

英文名称 P-[(2R)-3-amino-2-fluoropropyl]Phosphinic acid

CAS 344413-67-8

分子式 C3H9FNO2P

分子量 141.08

MOL 文件 344413-67-8.mol

更新日期 2023/03/20 15:41:23

344413-67-8 结构式

基本信息物理化学性质安全数据 P-[(2R)-3-氨基-2-氟丙基]磷酸价格(试剂级) 常见问题列表

基本信息

中文别名

P-[(2R)-3-氨基-2-氟丙基]磷酸

英文别名

AZD-3355
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

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.