ODQ |
カタログ番号GC10279
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ODQは、競争力のあるが不可逆的な方法でSGCを結合する可溶性グアニリルシクラーゼ（SGC）阻害剤である。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 41443-28-1
Sample solution is provided at 25 µL, 10mM.
ODQは、競争力のあるが不可逆的な方法でSGCを結合する可溶性グアニリルシクラーゼ（SGC）阻害剤である[1-2]。
ODQ（10μm）は可溶性グアニリルシクラーゼ（SGC）を阻害することでCOPPの抗ウイルス効果を部分に逆転させる[3]。ODQ（20μM）はナリングニン（NAR）が人の歯周靭帯幹細胞（HPDLSCS）の他の骨形成の分化を促進する能力を低下させる[4] ODQ（30μm）はNCI-H2452細胞のアポトーシスを誘発できる[5]。
ODQ（I.P; 6mg/kg; 8日間）の治療だけで腫瘍の成長の速度が遅くなる可能性があり、ODQとFruquintinibの組み合わせにより腫瘍サイズがさらに減少する[6]。 ODQ（25-100μg/mL）はゼブラフィッシュのSGC-CGMP-PKGシグナル伝達経路を阻害することにより、心筋肥大に対するZhenwu Decoction (ZWD)の保護効果を排除できる[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.
| 細胞実験[1]: | |
細胞株 | NBL-6細胞 |
準備方法 | 細胞に0.1のMOIで1時間EQHV-8を感染させた後にODQ（10µm）の存在下または非存在下でCOPP（100µm）の有無にかかわらず細胞の治療を行う。 |
反応条件 | 10µM |
アプリケーション | ODQは、EQHV-8子孫ウイルスによるコバルトプロトポルフィリン（COPP）の抗ウイルス効果を部分的に逆転させました世代である。 |
| 動物実験 [2]: | |
動物モデル | C57BL/6J鼠（LLC腫瘍モデル） |
準備方法 | 鼠は2.5mg/kgのフルキンティニブの経口投与と6mg/kg ODQの腹腔内注射を受け、両方とも6日目の腫瘍注射後から、腫瘍後14日目の腫瘍分析を受ける。 |
投与形態 | i.p; 6mg/kg; 8日 |
アプリケーション | ODQの治療だけで腫瘍の成長が減少し、ODQとフルキンティニブの組み合わせにより、腫瘍サイズがさらに減少する。 |
References: | |
| Cas No. | 41443-28-1 | SDF | |
| Chemical Name | 1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one | ||
| Canonical SMILES | O=C1ON=C2N1C3=CC=CC=C3N=C2 | ||
| Formula | C9H5N3O2 | M.Wt | 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 | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 | 534.3 μL | 2.6715 mL | 5.343 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 18 reference(s) in Google Scholar.)