1. Caldaret

Caldaret is an intracellular Ca2+ handling modulator that acts through reverse mode Na+/Ca2+ exchanger inhibition.

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Caldaret Chemical Structure

Caldaret Chemical Structure

CAS No. : 133804-44-1

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1 mg USD 266 In-stock
5 mg USD 614 In-stock
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Description

Caldaret is an intracellular Ca2+ handling modulator that acts through reverse mode Na+/Ca2+ exchanger inhibition.

IC50 & Target

Na+/Ca2+ exchanger[1]

In Vitro

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.

In Vivo

Caldaret, an intracellular Ca2+ handling modulator, limits infarct size of reperfused canine heart. The cardioprotective effect of Caldaret, a novel intracellular Ca2+ handling modulator that acts through reverse-mode Na+/Ca2+ exchanger inhibition and potential sarcoplasmic reticulum (SR) Ca2+ uptake enhancement, against reperfusion injury is investigated. Intravenously infused Caldaret (3 or 30 microg/kg per hour) for 30 min at left circumflex (LCX)-reperfusion markedly reduces infarct size (by 51.3% or 71.9%, respectively). The amelioration of intracellular Ca2+ handling dysfunction achieved by Caldaret leads to cardioprotective effects against reperfusion injury following prolonged ischemia[1]. Caldaret (MCC-135) is a new potent compound with beneficial effects in heart failure. In diabetic rats, Caldaret decreases TR80 significantly without significant effect on developed tension (DT). Caldaret has minimal effects on SR Ca2+ uptake in normal rats, that is observed as increased SR Ca2+ uptake at uptake time of 20 and 30 s at the highest concentration of 10 μM. In diabetic rats, Caldaret increases SR Ca2+ uptake all over the range of uptake time. Both initial rate of SR Ca2+ uptake and the amount of Ca2+ accumulated in the SR with longer uptake time are increased by Caldaret[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

256.32

Formula

C11H16N2O3S

CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O=S(C1=CC(C)=CC=C1N2CCNCC2)(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.9014 mL 19.5069 mL 39.0137 mL
5 mM 0.7803 mL 3.9014 mL 7.8027 mL
View the 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.

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Working solution concentration: mg/mL
Purity & Documentation
Animal Administration
[1]

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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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 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
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Product Name:
Caldaret
Cat. No.:
HY-100298
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