Caldaret
Based on 1 Customer Validation
Caldaret is an intracellular Ca2+ handling modulator that acts through reverse mode Na+/Ca2+ exchanger inhibition.
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- Pureté: 98.35%
- CAS No.: 133804-44-1
- Formule: C11H16N2O3S
- Masse moléculaire:256.32
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Stockage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Na+/Ca2+ exchanger[1]
Caldaret (MCC-135) is demonstrated to restore Ca2+-ATPase activity of the sarcoplasmic reticulum (SR) isolated from the myocardium acutely exposed to ischemia and reperfusion in vitro[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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 |
Chemical Information
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CAS No. 133804-44-1
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Appearance Solid
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Masse moléculaire 256.32
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Formule C11H16N2O3S
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Color White to light yellow
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SMILES
O=S(C1=CC(C)=CC=C1N2CCNCC2)(O)=O
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Synonyms
MCC-135
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvant et solubilité
1 M HCl : 33.33 mg/mL (130.03 mM; Need ultrasonic)
DMSO : 4.81 mg/mL (18.77 mM; ultrasonic and warming and adjust pH to 3 with HCl and heat to 60°C; 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 (protect from light). 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocole
Dogs[1]
Experiments are performed on 69 male healthy dogs (derived from the hybrid dogs of Labrador retriever, beagle, and hound strain; 6-13 month old; weighing from 10-16 kg). The animals are assigned randomly to four treatment groups: a control group (CONT, n=10) intravenously infused with saline, a low dose of Caldaret-treated group (CAL(L), n=10) infused with Caldaret (3 μg/kg per hour), a high dose of Caldaret-treated group (CAL(H), n=10) infused with Caldaret (30 μg/ kg per hour), and a Diltiazem-treated group (DIL, n=10) infused with Diltiazem (2000 μg/ kg per hour). Saline vehicle or drugs are intravenously administered from 75 min of occlusion to 15 min of reperfusion at a constant rate of 2 mL/kg per hour. Caldaret treatment is designed to evaluate the efficacy against reperfusion injury, thereby the infusion is started 15 min before reperfusion in order to obtain sufficient plasma concentrations at the onset of reperfusion. Caldaret or Diltiazem saline solution is freshly prepared just before the administration in each experimental day. After completion of the successful four hours of reperfusion, ventricular fibrillation (VF) is induced by an intravenous injection of potassium chloride, and the heart is isolated, and processed for postmortem measurement of infarct size and RMBF determinations.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Kawasumi H, et al. Caldaret, an intracellular Ca2+ handling modulator, limits infarct size of reperfused canine heart. J Pharmacol Sci. 2007 Feb;103(2):222-33. [Content Brief]
[2]. Satoh N, et al. Lusitropic effect of MCC-135 is associated with improvement of sarcoplasmic reticulum function in ventricular muscles of rats with diabetic cardiomyopathy. J Pharmacol Exp Ther. 2001 Sep;298(3):1161-6. [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 (protect from 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 |
|---|---|---|---|---|---|
| DMSO / 1 M HCl | 1 mM | 3.9014 mL | 19.5069 mL | 39.0137 mL | 97.5343 mL |
| 5 mM | 0.7803 mL | 3.9014 mL | 7.8027 mL | 19.5069 mL | |
| 10 mM | 0.3901 mL | 1.9507 mL | 3.9014 mL | 9.7534 mL | |
| 15 mM | 0.2601 mL | 1.3005 mL | 2.6009 mL | 6.5023 mL | |
| 1 M HCl | 20 mM | 0.1951 mL | 0.9753 mL | 1.9507 mL | 4.8767 mL |
| 25 mM | 0.1561 mL | 0.7803 mL | 1.5605 mL | 3.9014 mL | |
| 30 mM | 0.1300 mL | 0.6502 mL | 1.3005 mL | 3.2511 mL | |
| 40 mM | 0.0975 mL | 0.4877 mL | 0.9753 mL | 2.4384 mL | |
| 50 mM | 0.0780 mL | 0.3901 mL | 0.7803 mL | 1.9507 mL | |
| 60 mM | 0.0650 mL | 0.3251 mL | 0.6502 mL | 1.6256 mL | |
| 80 mM | 0.0488 mL | 0.2438 mL | 0.4877 mL | 1.2192 mL | |
| 100 mM | 0.0390 mL | 0.1951 mL | 0.3901 mL | 0.9753 mL |
Caldaret Related Classifications
HY-100298 Related Classifications
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