PSB-0739

立即咨询

PSB-0739

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1052087-90-7

包装与价格：

包装	价格(元)
5mg	电议
10mg	电议
25mg	电议
50mg	电议
100mg	电议
200mg	电议
500mg	电议

产品介绍

PSB-0739 是一种高亲和力、竞争性、非选择性的血小板P2Y₁₂受体拮抗剂，K_i值为 24.9 nM。P2Y₁₂受体在血小板聚集中起着至关重要的作用。PSB-0739 具有抗血栓作用。

生物活性

PSB-0739 is a high-affinity potent, competitive, nonselective plateletP2Y₁₂receptorantagonist with a K_ivalues of 24.9 nM. The P2Y₁₂receptor plays a crucial role in platelet aggregation. Antithrombotic effect^[1].

IC₅₀& Target

P2Y12 Receptor

体外研究
(In Vitro)

PSB-0739 is a potent competitive non-nucleotide antagonist at the human P2Y₁₂receptor with a pA₂value of 9.8^[2].
PSB-0739 inhibits ADP-evoked Ca²⁺responses with an EC₅₀of 5.4±1.8 μM and causes a rightward parallel shift in the ADP concentration–response curve in THP-1 cells^[3].

Cell Viability Assay^[3]

Cell Line:	THP-1 monocytic cell line
Concentration:	10 nM, 100 nM, 1 μM, 10 μM
Incubation Time:
Result:	Attenuated ADP-evoked responses (IC₅₀=5.4±1.8 μM).

体内研究
(In Vivo)

PSB-0739 (0.01-0.3 mg/kg, intrathecally) has dose-dependent and significant antihyperalgesic effect in low doses. The minimal effective dose (mED) is 0.1 mg/kg^[4].

Animal Model:	Male Wistar rats, 150-250 g, 6-8/group^[4]
Dosage:	0.01, 0.03, 0.1, 0.3 mg/kg
Administration:	Intrathecal injection ( i.t.)
Result:	Displayed a dose-dependent inhibitory effect on mechanical hyperalgesia in the range of 0.01–0.1 mg/kg.

分子量

609.54

性状

Solid

Formula

C₂₆H₁₇N₃Na₂O₈S₂

CAS 号

1052087-90-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)