性能参数

产品名称

Tiplaxtinin

规格

10mM (in 1mL DMSO) 5mg 10mg 50mg

货号

GOY-Y3254

 含量

>98.00%

CAS

393105-53-8

别名

化学名

2-(1-benzyl-5-(4-(trifluoromethoxy)phenyl)-1H-indol-3-yl)-2-oxoacetic acid

分子式

C24H16F3NO4

分子量

分子量 439.38

溶解度

≥ 17.6mg/mL in DMSO

储存条件

Store at -20°C

General tips

用途

仅供科研

价格

电询

详细内容

Description:

IC50: 2.7 μM

Plasminogen activator inhibitor-1 (PAI-1) is the most important physiologic regulator of the plasminogen activation system through its inhibition of its target serine proteases, tissue plasminogen activator, and urokinase plasminogen activator. Significant elevations of PAI-1 lead to stabilization of arterial and venous thrombi, which contribute respectively to coronary arterial occlusion in postmyocardial infarction and venous thrombosis following postoperative recovery from orthopedic surgery. Tiplaxtinin (PAI-039) is a novel, orally efficacious inhibitor of PAI-1.

In vitro: Tiplaxtinin inhibited PAI-1 as determined by the antibody method. By use of fluorescent spectroscopy, tiplaxtinin bound to the PAI-1 mutant selectively with a Kd of 480 nM. This binding event was saturable and associated with inhibition of the protein [1].

In vivo: In the rat model of carotid thrombosis, oral administration of tiplaxtinin at 1 mg/kg increased time to occlusion and prevented the carotid blood flow reduction when compared to the vehicle group. All of the vehicle control rats exhibited thrombosis with an average time to occlusion of 11 min and a complete reduction of 100% carotid flow. Conversely, those rats receiving tiplaxtinin at 1 mg/kg po exhibited an average time to occlusion of >50 min and a carotid blood flow reduction of approximately 50% [1].

Clinical trial: Up to now, tiplaxtinin is still in the preclinical development stage.

2-三氟甲基吡啶  368-48-9  4-羟基-6-(三氟甲基)嘧啶-2-硫醇  368-54-7

2-硝基咪唑  36877-68-6  3-三氟甲基苯肼  368-78-5

4-(三氟甲基)苯肼  368-90-1  3',4'-二氟苯乙酮  369-33-5

2-氟-5-硝基苯胺  369-36-8  4-溴-2-羟基吡啶  36953-37-4

3-溴-4-羟基吡啶  36953-41-0  三苯甲硫醇  3695-77-0

1-Boc-2-氨甲基哌370069-31-1  2-巯基-5-?

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