MBCQ

MBCQ用途

MBCQ 是一种有效的选择性 cGMP 特异性磷酸二酯酶 (PDE V; PDE5) 抑制剂,IC50 为 19 nM。MBCQ 对其他 PDE 同工酶没有抑制活性,IC50 均大于 100 µM。MBCQ 通过特异性抑制 cGMP-PDE 来扩张冠状动脉。

MBCQ名称

[ CAS 号 ]:
150450-53-6

[ 英文名 ]:
MBCQ

[英文别名 ]:

UPCMLD-DP008
MBCQ

MBCQ生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 心血管疾病

信号通路 >> 代谢酶/蛋白酶 >> 磷酸二酯酶(PDE)

[ 靶点 ]

PDE V:19 nM (IC50)

PDE Ⅰ:>100 μM (IC50)

PDE Ⅱ:>100 μM (IC50)

PDE Ⅲ:>100 μM (IC50)

PDE Ⅳ:>100 μM (IC50)

[体外研究]

MBCQ(化合物3d)对前列腺素F2预收缩猪离体冠状动脉的舒张作用α (PGF2型α; EC50=190纳米)[1]。MBCQ(0.01-10)μ米；10分钟)抑制卡巴胆碱(10分钟μM) -在大鼠回肠平滑肌中以浓度依赖性方式诱导收缩[3]。

[参考文献]

[1]. Y Takase, et al. Cyclic GMP phosphodiesterase inhibitors. 2. Requirement of 6-substitution of quinazoline derivatives for potent and selective inhibitory activity. J Med Chem. 1994 Jun 24;37(13):2106-11.

[2]. Jeffery D MacPherson, et al. Inhibition of phosphodiesterase 5 selectively reverses nitrate tolerance in the venous circulation J Pharmacol Exp Ther. 2006 Apr;317(1):188-95.

[3]. Takeharu Kaneda, et al. Lack of cyclic nucleotide regulation of MBCQ-induced relaxation of rat ileal smooth muscle. J Smooth Muscle Res. 2003 Jun;39(3):47-54.

MBCQ物理化学性质

[ 分子式 ]:
C₁₆H₁₂ClN₃O₂

[ 分子量 ]:
313.73800

[ 精确质量 ]:
313.06200

[ PSA ]:
56.27000

[ LogP ]:
3.69700

MBCQMSDS

MBCQ安全信息

[ 危险品运输编码 ]:
NONH for all modes of transport

MBCQ合成路线

MBCQ上下游产品

MBCQ上游产品

MBCQ下游产品

MBCQ文献

BH3 domain-independent apolipoprotein L1 toxicity rescued by BCL2 prosurvival proteins.

Am. J. Physiol. Cell Physiol. 309 , C332-47, (2015)

The potent trypanolytic properties of human apolipoprotein L1 (APOL1) can be neutralized by the trypanosome variant surface antigen gene product known as serum resistance-associated protein. However, ...

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