Ataciguat
Based on 1 publication(s) in Google Scholar
Ataciguat (HMR-1766) is a nitric oxide-independent soluble guanylate cyclase (sGC) activator. Ataciguat is able to activate the ferric heme-iron redox form of sGC that stimulate the production of cyclic GMP (cGMP). Ataciguat exhibits vasodilator effects.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.70%
- CAS 番号: 254877-67-3
- 分子式: C21H19Cl2N3O6S3
- 分子量:576.49
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
MedChemExpress(MCE)の使用を引用している文献 Ataciguat
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生物活性
soluble guanylate cyclase[1]
Ataciguat (1-100 μM) induces the relaxation in aortic rings or coronary rings[2].
Ataciguat (0.1-10 μM; 30 min) increases NO production in HUVEC cells[2].
Ataciguat (1 nM-100 μM) induces concentration-dependent relaxations in sphincter of Oddi (SO) rings pre-contracted by Carbachol[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 254877-67-3
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性状 Solid
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分子量 576.49
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分子式 C21H19Cl2N3O6S3
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Color White to off-white
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SMILES
O=C(NC1=CC=C(S(=O)(N2CCOCC2)=O)C=C1)C3=CC(Cl)=CC=C3NS(=O)(C4=CC=C(Cl)S4)=O
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別名
HMR-1766
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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bioRxiv
Circulating biomarkers in serum from aortic valve stenosis patients predict sex-specific drug responses in valve myofibroblasts. [Abstract]2026 Jan 20:2026.01.16.700010. PMID: 41648356
溶剤 & 溶解度
DMSO : 100 mg/mL (173.46 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.34 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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データシート (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
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- Deutsch - DE (393 KB)
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- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Schindler U, et, al. Biochemistry and pharmacology of novel anthranilic acid derivatives activating heme-oxidized soluble guanylyl cyclase. Mol Pharmacol. 2006 Apr;69(4):1260-8. [Content Brief]
[2]. Martinelli AM, et, al. In Endothelial Cells, the Activation or Stimulation of Soluble Guanylyl Cyclase Induces the Nitric Oxide Production by a Mechanism Dependent of Nitric Oxide Synthase Activation. J Pharm Pharm Sci. 2018;21(1):38-45. [Content Brief]
[3]. Çakmak E, et, al. Comparative Relaxant Effects of Ataciguat and Zaprinast on Sheep Sphincter of Oddi. Balkan Med J. 2016 Jul;33(4):453-7. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7346 mL | 8.6731 mL | 17.3463 mL | 43.3657 mL |
| 5 mM | 0.3469 mL | 1.7346 mL | 3.4693 mL | 8.6731 mL | |
| 10 mM | 0.1735 mL | 0.8673 mL | 1.7346 mL | 4.3366 mL | |
| 15 mM | 0.1156 mL | 0.5782 mL | 1.1564 mL | 2.8910 mL | |
| 20 mM | 0.0867 mL | 0.4337 mL | 0.8673 mL | 2.1683 mL | |
| 25 mM | 0.0694 mL | 0.3469 mL | 0.6939 mL | 1.7346 mL | |
| 30 mM | 0.0578 mL | 0.2891 mL | 0.5782 mL | 1.4455 mL | |
| 40 mM | 0.0434 mL | 0.2168 mL | 0.4337 mL | 1.0841 mL | |
| 50 mM | 0.0347 mL | 0.1735 mL | 0.3469 mL | 0.8673 mL | |
| 60 mM | 0.0289 mL | 0.1446 mL | 0.2891 mL | 0.7228 mL | |
| 80 mM | 0.0217 mL | 0.1084 mL | 0.2168 mL | 0.5421 mL | |
| 100 mM | 0.0173 mL | 0.0867 mL | 0.1735 mL | 0.4337 mL |