ODQ

目录号: GC10279纯度: >98.00%同义词: 1H-[1,2,4]恶草灵并[4,3-A]喹喔啉-1-酮
ODQ是一种可溶性鸟苷酰环化酶 (sGC) 抑制剂,以竞争不可逆的方式结合sGC。

ODQ
Cas No.: 41443-28-1
规格价格库存数量操作
5mg¥381.00现货
1
10mg¥653.00现货
1
50mg¥2,285.00现货
1
100mg¥4,189.00现货
1

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产品描述 Description

ODQ is a soluble guanylyl cyclase (sGC) inhibitor that binds sGC in a competitive but irreversible manner [1-2].

ODQ(10μM) partially reversed the antiviral effect of CoPP by inhibiting Soluble guanylyl cyclase (sGC) [3]. ODQ(20μM) reduces the ability of Naringenin (NAR) to promote the osteogenic differentiation of human periodontal ligament stem cells (hPDLSCs) [4]. ODQ(30μM) significantly induced apoptosis of NCI-H2452 cells [5].

ODQ(i.p; 6mg/kg; 8 days) treatment alone can slow the growth rate of tumors, the combination of ODQ and Fruquintinib further decreased tumor size[6]. ODQ(25-100μg/mL) can eliminate the protective effect of Zhenwu Decoction (ZWD) on myocardial hypertrophy by inhibiting sGC-cGMP-PKG signaling pathway in zebrafish [7].

References:
[1]. Feelisch M, Kotsonis P, et,al. The soluble guanylyl cyclase inhibitor 1H-[1,2,4]oxadiazolo[4,3,-a] quinoxalin-1-one is a nonselective heme protein inhibitor of nitric oxide synthase and other cytochrome P-450 enzymes involved in nitric oxide donor bioactivation. Mol Pharmacol. 1999 Aug;56(2):243-53. doi: 10.1124/mol.56.2.243. PMID: 10419542.
[2]. Schrammel A, Behrends S, et,al. Characterization of 1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one as a heme-site inhibitor of nitric oxide-sensitive guanylyl cyclase. Mol Pharmacol. 1996 Jul;50(1):1-5. PMID: 8700100.
[3]. Wang T, Li S, et,al. Heme oxygenase-1 is an equid alphaherpesvirus 8 replication restriction host protein and suppresses viral replication via the PKCβ/ERK1/ERK2 and NO/cGMP/PKG pathway. Microbiol Spectr. 2024 Apr 2;12(4):e0322023. doi: 10.1128/spectrum.03220-23. Epub 2024 Mar 5. PMID: 38441979; PMCID: PMC10986571.
[4]. Li S, Xiong Z, et,al. Naringenin modulates the NO‑cGMP‑PKG signaling pathway by binding to AKT to enhance osteogenic differentiation in hPDLSCs. Int J Mol Med. 2024 Aug;54(2):67. doi: 10.3892/ijmm.2024.5391. Epub 2024 Jun 28. PMID: 38940332; PMCID: PMC11232664.
[5]. 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.
[6]. Zhu J, Yang W, et,al. Pericyte signaling via soluble guanylate cyclase shapes the vascular niche and microenvironment of tumors. EMBO J. 2024 Apr;43(8):1519-1544. doi: 10.1038/s44318-024-00078-5. Epub 2024 Mar 25. PMID: 38528180; PMCID: PMC11021551.
[7].Chen L, Zhou X, et,al. Zhenwu decoction ameliorates cardiac hypertrophy through activating sGC (soluble guanylate cyclase) - cGMP (cyclic guanosine monophosphate) - PKG (protein kinase G) pathway. J Ethnopharmacol. 2023 Jan 10;300:115705. doi: 10.1016/j.jep.2022.115705. Epub 2022 Sep 12. PMID: 36099983.

ODQ是一种可溶性鸟苷酰环化酶 (sGC) 抑制剂,以竞争不可逆的方式结合sGC[1-2]

ODQ(10µM)通过抑制可溶性鸟苷酸环化酶(sGC)部分逆转了CoPP的抗病毒效果[3]。ODQ(20μM)降低Naringenin(NAR)促进人牙周韧带干细胞(hPDLSCs)成骨分化的能力[4]。ODQ(30μM)显著诱导NCI-H2452细胞凋亡[5]

ODQ(i.p; 6mg/kg; 8 days)单独治疗可减缓肿瘤生长速度,ODQ和fruquininib联合治疗可进一步降低肿瘤大小[6]。ODQ(25-100μg/mL)可通过抑制斑马鱼sGC-cGMP-PKG信号通路,消除真五汤对心肌肥厚的保护作用[7]

实验参考方法 Experimental Reference Method

Cell experiment [1]:

Cell lines

NBL-6 cells

Preparation Method

Cells were infected with EqHV-8 at an MOI of 0.1 for 1 h, followed by the treatment of cells with or without CoPP (100µM) in the presence or absence of ODQ (10µM).

Reaction Conditions

10µM

Applications

ODQ partially reversed the anti-viral effect of cobalt-protoporphyrin (CoPP) by EqHV-8 progeny virus generation.
Animal experiment [2]:

Animal models

C57BL/6J mice(LLC tumor model)

Preparation Method

Mice received oral administration of 2.5mg/kg Fruquintinib and intraperitoneal injection of 6mg/kg ODQ, both starting from day 6 post-tumor injection, and tumor analysis at day 14 post-tumor injection.

Dosage form

i.p; 6mg/kg; 8 days

Applications

ODQ treatment alone reduced tumor growth, the combination of ODQ and Fruquintinib further decreased tumor size.

References:
[1]. Wang T, Li S, et,al. Heme oxygenase-1 is an equid alphaherpesvirus 8 replication restriction host protein and suppresses viral replication via the PKC?/ERK1/ERK2 and NO/cGMP/PKG pathway. Microbiol Spectr. 2024 Apr 2;12(4):e0322023. doi: 10.1128/spectrum.03220-23. Epub 2024 Mar 5. PMID: 38441979; PMCID: PMC10986571.
[2].Zhu J, Yang W, et,al. Pericyte signaling via soluble guanylate cyclase shapes the vascular niche and microenvironment of tumors. EMBO J. 2024 Apr;43(8):1519-1544. doi: 10.1038/s44318-024-00078-5. Epub 2024 Mar 25. PMID: 38528180; PMCID: PMC11021551.

产品文档 Product Documents

Purity:>98.00%

化学性质Chemical Properties

CAS 号
41443-28-1
同义词
1H-[1,2,4]恶草灵并[4,3-A]喹喔啉-1-酮
化学名
1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one
SMILES
O=C1ON=C2N1C3=CC=CC=C3N=C2
分子式
C9H5N3O2
分子量
187.16 g/mol
溶解性
DMF: 30 mg/ml,DMF:PBS (pH 7.2) (1:1): .1 mg/ml,DMSO: 15 mg/ml,Ethanol: .5 mg/ml
保存条件
Store at -20°C
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至 37°C,然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备 RT,或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol