1. Membrane Transporter/Ion Channel
  2. Na+/Ca2+ Exchanger
  3. Caldaret

Caldaret  (Synonyms: MCC-135)

目录号: HY-100298 纯度: 98.35%
COA 产品使用指南

Caldaret 是一种细胞内 Ca2+ 调节剂,通过反向模式抑制 Na+/Ca2+ 交换作用。

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Caldaret Chemical Structure

Caldaret Chemical Structure

CAS No. : 133804-44-1

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1 mg ¥2660
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5 mg ¥6140
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10 mg ¥8600
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Customer Review

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

IC50 & Target

Na+/Ca2+ exchanger[1]

体外研究
(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].

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

体内研究
(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].

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

Clinical Trial
分子量

256.32

Formula

C11H16N2O3S

CAS 号
性状

固体

颜色

White to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

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

溶解性数据
In Vitro: 

DMSO 中的溶解度 : 4.81 mg/mL (18.77 mM; 超声助溶 (<60 ℃);酸性条件溶解 (HCL 调节,pH=3) ; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 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
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献
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.

参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 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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  • Do most proteins show cross-species activity?

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Caldaret
目录号:
HY-100298
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