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ODQ

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Chemical Structure| 41443-28-1 同义名 : 1H-ODQ
CAS号 : 41443-28-1
货号 : A222246
分子式 : C9H5N3O2
纯度 : 99%+
分子量 : 187.155
MDL号 : MFCD00792620
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(561.03 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Soluble guanylyl cyclase (sGC) is the principal enzyme in mediating the biological actions of nitric oxide. On activation, sGC converts guanosine triphosphate to guanosine 3',5'-cyclic monophosphate (cGMP), which mediates diverse physiological processes including vasodilation, platelet aggregation, and myocardial functions predominantly by acting on cGMP-dependent protein kinases[1].Impaired NO-sGC-cGMP signaling could lead to osteoblast apoptosis by mechanisms involving the oxidative-stress-induced shift of the redox state of the reduced heme to oxidized sGC, leading to diminished heme binding to the enzyme and rendering the sGC unresponsive to NO. Targeting oxidized sGC to enhance cGMP production could restore proliferation and differentiation of osteoblasts into osteocytes[2]. ODQ is a potent and selective sGC inhibitor. ODQ enhances the pro-apoptotic effects of Cisplatin in human mesothelioma cells. At 30 and 50 μM, ODQ causes significant induction of apoptosis in the NCI-H2452 cells, elevating apoptotic levels by 12 fold and 15 fold, respectively. At 10μM, a concentration below the threshold for induction of apoptosis by ODQ, ODQ in combination with Cisplatin enhanced (in fact, doubled) the pro-apoptotic effects of Cisplatin at 1 μM[3]. ODQ (2 mg/kg; i.p.) reduces the multiple organ injury and dysfunction caused by wall fragments of Gram-positive or Gram-negative bacteria in the anesthetized rat[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

5.34mL

1.07mL

0.53mL

26.72mL

5.34mL

2.67mL

53.43mL

10.69mL

5.34mL
参考文献

[1]Yuansheng Gao. Conventional and Unconventional Mechanisms for Soluble Guanylyl Cyclase Signaling. J Cardiovasc Pharmacol. 2016 May;67(5):367-72.

[2] Belay Tesfamariam,et al. Targeting heme-oxidized soluble guanylate cyclase to promote osteoblast function. Drug Discov Today. 2020 Feb;25(2):422-429.

[3] Ronald Fiscus, et al. ODQ, an inhibitor of soluble guanylyl cyclase (nitric oxide-activated enzyme), enhances the pro-apoptotic effects of cisplatin in human mesothelioma cells. Cancer Res May 1 2007 (67) (9 Supplement) LB-43.

[4] Zacharowski K, et al. The selective guanylate cyclase inhibitor ODQ reduces multiple organ injury in rodent models of Gram-positive and Gram-negative shock. Crit Care Med. 2001;29(8):1599-1608.