| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| ln Vitro |
Ataciguat (1-100 μM) causes the coronary or aortic artery rings to relax [2]. In HUVEC cells, ataciguat (0.1–10 μM; 30 minutes) boosts NO production [2]. High-concentration biliary contractions are induced in the carbachine-precontracted circular sphincter of Oddi (SO) by ataciguat (1 nM-100 μM). [3].
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| Animal Protocol |
The study is an ex vivo pharmacological investigation. Tissue samples were obtained from ten adult male Anatolian Akkaraman sheep, weighing 38-45 kg. The sheep were sacrificed, and the sphincter of Oddi was quickly removed. The SO was placed in a pre-aerated (95% O2 and 5% CO2) Krebs' bicarbonate solution for transport to the laboratory. [3]
Tissue Bath Protocol:** The SO was dissected into rings and mounted in 10 mL tissue baths containing the aerated Krebs' solution maintained at 37°C. Each ring was tied to an isometric transducer (Grass FT 03) under a resting tension of 1.5 g. The tissues were allowed to equilibrate for 60-90 minutes, during which the bath solution was changed every 15 minutes. After equilibration, the rings were contracted with a submaximal concentration of carbachol (10⁻⁶ mol/L). Once a stable contraction was achieved, cumulative concentration-response curves to ataciguat (10⁻⁹ to 10⁻⁴ mol/L) were obtained. To investigate the mechanism, the effect of ataciguat was also tested in the presence of the sGC inhibitor ODQ (10⁻⁵ mol/L), which was added to the bath prior to ataciguat administration. Between each drug application, the tissues were washed at least twice and allowed to re-equilibrate for at least 30 minutes. [3] |
| References |
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| Additional Infomation |
Ataciguat has been used in basic scientific research on aortic stenosis.
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| Exact Mass |
574.981
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|---|---|
| CAS # |
254877-67-3
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| Related CAS # |
254877-67-3;254976-06-2 (Sodium);
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| PubChem CID |
213037
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| Appearance |
White to off-white solid powder
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| Density |
1.6±0.1 g/cm3
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| Index of Refraction |
1.685
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| LogP |
6.08
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
35
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| Complexity |
944
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| Defined Atom Stereocenter Count |
0
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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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| InChi Key |
PQHLRGARXNPFCF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H19Cl2N3O6S3/c22-14-1-6-18(25-34(28,29)20-8-7-19(23)33-20)17(13-14)21(27)24-15-2-4-16(5-3-15)35(30,31)26-9-11-32-12-10-26/h1-8,13,25H,9-12H2,(H,24,27)
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| Chemical Name |
5-chloro-2-[(5-chlorothiophen-2-yl)sulfonylamino]-N-(4-morpholin-4-ylsulfonylphenyl)benzamide
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| Synonyms |
HMR-1766 HMR1766 HMR 1766
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~173.46 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.34 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.34 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02049203 | COMPLETED | Drug: Ataciguat Drug: Placebo |
Aortic Valve Stenosis | Jordan D. Miller, Ph.D. | 2014-01 | Phase 1 |
| NCT00799656 | COMPLETED | Drug: ataciguat (HMR1766) Drug: placebo |
Pain | Sanofi | 2008-11 | Phase 2 |
| NCT02481258 | COMPLETEDWITH RESULTS | Drug: Ataciguat (HMR1766) Other: Placebo Comparator: Matching Placebo |
Aortic Valve Stenosis | Mayo Clinic | 2015-06 | Phase 2 |
| NCT00443287 | COMPLETED | Drug: ataciguat (HMR1766) Drug: placebo Drug: cilostazol |
Intermittent Claudication | Sanofi | 2007-02 | Phase 2 |
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