Senazodan hydrochloride
Based on 1 Customer Validation
Senazodan (MCI 154) (hydrochloride), as a Ca2+ sensitiser, shows inhibition effect on PDE III.
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- Reinheit : 99.84%
- CAS. Nr.: 98326-33-1
- Formel: C15H15ClN4O
- Molecular Weight:302.76
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Speicherung:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Beschreibung
IC50 & Target
PDE III[1]
In Vitro
Senazodan (hydrochloride) seems to affect directly the actin-myosin crossbridge kinetics, and increases myosin ATPase activity[1]. Senazodan (hydrochloride) produces a concentration-dependent increase in tension development. Senazodan (hydrochloride) enhances Ca2+ binding to myofilaments and to purified cardiac troponin C. Senazodan (hydrochloride) also enhances contractility in guinea-pig papillary muscles by inhibiting PDE III[2].Senazodan (0.1 nM~0.1 mM) (hydrochloride) shows that the contractile response of superior mesenteric arterie (SMA) to norepinephrine (NE) after hemorrhagic shock is significantly decreased as compared with the normal control group. Senazodan (0.01 mM) (hydrochloride) pretreatment prevents the effects of Ang II, and the concentration-response curve of Ca2+ is shifted to the right as compared with Ang II-alone group[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Senazodan (0.1 mg/kg; i.v.) (hydrochloride) makes LVSP, IP, MC, and Lo all increased significantly, while heart rate is not obviously changed and left ventricular end-diastolic pressure (LVEDP) is reduced remarkably[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar rats (200~250 g)[3]
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Dosage:0.1~2.0 mg/kg
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Administration:Left femoral vein catheterization infusion
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Result:Decreased the pressor effect of norepinephrine (NE).
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Animal Model:Rabbits[4]
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Dosage:0.1 mg/kg
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Administration:I.v.
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Result:LVSP, IP, MC, and Lo all were increased significantly while heart rate was not obviously changed and left ventricular end-diastolic pressure (LVEDP) was reduced remarkably.
Chemical Information
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CAS. Nr. 98326-33-1
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Appearance Solid
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Molecular Weight 302.76
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Formel C15H15ClN4O
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Color Light yellow to yellow
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SMILES
[H]Cl.O=C1CCC(C2=CC=C(NC3=CC=NC=C3)C=C2)=NN1
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Synonyms
MCI 154 hydrochloride
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 67.5 mg/mL (222.95 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 25 mg/mL (82.57 mM; Need ultrasonic)
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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
In Vivo:
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 (8.26 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (8.26 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
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.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Reinheit & Dokumentation
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Data Sheet (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Lehtonen LA, et al. Pharmacokinetics and pharmacodynamics of intravenous inotropic agents. Clin Pharmacokinet. 2004;43(3):187-203. [Content Brief]
[2]. Erhardt L. An emerging role for calcium sensitisation in the treatment of heart failure. Expert Opin Investig Drugs. 2005 Jun;14(6):659-70. [Content Brief]
[3]. Yang G, et al. Effects of MCI-154 on vascular reactivity and its mechanisms after hemorrhagic shock in rats. J Cardiovasc Pharmacol. 2006;47(6):751-757. [Content Brief]
[4]. Ming MJ, et al. Effects of MCI-154, a calcium sensitizer, on cardiac dysfunction in endotoxic shock in rabbits. Shock. 2000;13(6):459-463. [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 (sealed storage, away from moisture and light). 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 |
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| H2O / DMSO | 1 mM | 3.3029 mL | 16.5147 mL | 33.0295 mL | 82.5737 mL |
| 5 mM | 0.6606 mL | 3.3029 mL | 6.6059 mL | 16.5147 mL | |
| 10 mM | 0.3303 mL | 1.6515 mL | 3.3029 mL | 8.2574 mL | |
| 15 mM | 0.2202 mL | 1.1010 mL | 2.2020 mL | 5.5049 mL | |
| 20 mM | 0.1651 mL | 0.8257 mL | 1.6515 mL | 4.1287 mL | |
| 25 mM | 0.1321 mL | 0.6606 mL | 1.3212 mL | 3.3029 mL | |
| 30 mM | 0.1101 mL | 0.5505 mL | 1.1010 mL | 2.7525 mL | |
| 40 mM | 0.0826 mL | 0.4129 mL | 0.8257 mL | 2.0643 mL | |
| 50 mM | 0.0661 mL | 0.3303 mL | 0.6606 mL | 1.6515 mL | |
| 60 mM | 0.0550 mL | 0.2752 mL | 0.5505 mL | 1.3762 mL | |
| 80 mM | 0.0413 mL | 0.2064 mL | 0.4129 mL | 1.0322 mL | |
| DMSO | 100 mM | 0.0330 mL | 0.1651 mL | 0.3303 mL | 0.8257 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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