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名称

Firibastat, 氨基肽酶 A 抑制剂

分子类型

小分子

别名

非利巴司他

英文别名

英文名称

Firibastat

货号

F651723-5mg

包装规格

5mg

浓度

≥98%

储存温度

-20°C储存

运输条件

超低温冰袋运输

产品介绍

Firibastat (QGC001), an orally active brain penetrating proagent of EC33, is a first-in-class brain aminopeptidase A (APA) inhibitor ( K i =200 nM). Firibastat selectively and specifically inhibits conversion of brain angiotensin-II into angiotensin-III and decreases blood pressure in hypertensive rats. In Vivo When given orally, Firibastat (0.1-30 mg/kg; p.o.) crosses the gastrointestinal and blood-brain barriers, enters the brain, and generates two active molecules of EC33 which inhibit brain APA activity, blocking brain angiotensin III formation, and decrease blood pressure for several hours in hypertensive rats. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Normotensive and hypertensive DOCA-salt rats Dosage: 0.1-30 mg/kg Administration: P.o. Result: Resulting in a dose-dependent decrease in mean arterial blood pressure (MABP). Form:Solid

生化机理

菲瑞巴司他（QGC001）是一种口服活性脑穿透原药 EC33，是第一类脑氨肽酶 A（APA）抑制剂（K i =200 nM）。非利巴司他能选择性地特异抑制脑血管紧张素-II 向血管紧张素-III a 的转化。

CAS号

648927-86-0

分子式

C8H20N2O6S4

分子量

368.51 g/mol

EC号

817-496-7

PubChem编号

24851355

Isomeric SMILES

C(CS(=O)(=O)O)[C@@H](CSSC[C@H](CCS(=O)(=O)O)N)N

IIUPAC Name

(3S)-3-amino-4-[[(2S)-2-amino-4-sulfobutyl]disulfanyl]butane-1-sulfonic acid

INCHI

1S/C8H20N2O6S4/c9-7(1-3-19(11,12)13)5-17-18-6-8(10)2-4-20(14,15)16/h7-8H,1-6,9-10H2,(H,11,12,13)(H,14,15,16)/t7-,8-/m0/s1

InChi Key

HJPXZXVKLGEMGP-YUMQZZPRSA-N

Smiles

C(CS(=O)(=O)O)C(CSSCC(CCS(=O)(=O)O)N)N

PubChem CID

24851355

关联CAS

648927-86-0

MeSH Entry Terms

4,4'-dithio(bis(3-aminobutyl sulfonic acid));firibastat;RB 150;RB-150;RB150;RB150 cpd

溶解性

H2O : 33.33 mg/mL (90.45 mM; Need ultrasonic)

氢键供体数Hydrogen Bond Donor Count

氢键受体数Hydrogen Bond Acceptor Count

可旋转键计数Rotatable Bond Count

精确质量Exact Mass

368.02 Da

单同位素质量Monoisotopic Mass

368.02 Da

拓扑极表面积Topological Polar Surface Area

228.000 Å²

重原子数Heavy Atom Count

形式电荷Formal Charge

复杂度Complexity

410.000

同位素原子数Isotope Atom Count

共价键合单元计数Covalently-Bonded Unit Count

XLogP3

-6.900

ALogP

-6.9

作用类型

抑制剂

作用机制

氨基肽酶 A 抑制剂

Safety

「No Dangerous Attributes」

「No upstream and downstream information yet」

Technical Documents

「No technical documents」

Articles

「No related articles yet」

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