ODQ
(Synonyms: 1H-[1,2,4]恶草灵并[4,3-A]喹喔啉-1-酮) 目录号 : GC10279
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。
Cas No.:41443-28-1
Sample solution is provided at 25 µL, 10mM.
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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]。
| 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: | |
| Cas No. | 41443-28-1 | SDF | |
| 别名 | 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 | ||
| Canonical SMILES | O=C1ON=C2N1C3=CC=CC=C3N=C2 | ||
| 分子式 | C9H5N3O2 | 分子量 | 187.16 |
| 溶解度 | DMF: 30 mg/ml,DMF:PBS (pH 7.2) (1:1): .1 mg/ml,DMSO: 15 mg/ml,Ethanol: .5 mg/ml | 储存条件 | 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℃，然后在超声波浴中震荡一段时间。 |
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| 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。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 5.343 mL | 26.7151 mL | 53.4302 mL |
| 5 mM | 1.0686 mL | 5.343 mL | 10.686 mL |
| 10 mM | 0.5343 mL | 2.6715 mL | 5.343 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet