中文名称: Caldaret
英文名称: Caldaret
CAS No: 133804-44-1
分子式: C11H16N2O3S
分子量: 256.32
C11179 Caldaret ≥98% (psaitong)
包装规格:
100mg in glass bottle
产品描述:

基本信息

产品编号:

C11179

产品名称:

Caldaret

CAS:

133804-44-1

 

储存条件

粉末

-20℃

四年

分子式:

C11H16N2O3S

溶于液体

-80℃

四年

分子量:

256.32

 

 

化学名: 

5-Methyl-2-(1-piperazinyl)-benzenesulfonic acid

Solubility (25°C):

 

体外:

 

DMSO

 

Ethanol

 

Water

 

体内(现配现用):

 

1mg/ml表示微溶或不溶。

普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。

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。

 

生物活性

产品描述

一种细胞内Ca2+调节剂,通过反向模式抑制Na+/Ca2+交换作用。

靶点

Na+/Ca2+ exchanger

 

体外研究

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.

体内研究

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.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 10μM.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.

 

推荐实验方法(仅供参考)

动物实验:

 

Dogs

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 10-16kg).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 (3μg/kg per hour),a high dose of Caldaret-treated group (CAL(H),n=10) infused with Caldaret (30μg/ kg per hour),and a Diltiazem-treated group (DIL,n=10) infused with Diltiazem (2000μg/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 2mL/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.

保存条件:
-20℃
UN码:
HazardClass:
危害声明:
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参考文献 & 客户发表文献

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

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开始浓度 x 开始体积 = 最终浓度 x 最终体积

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  • 计算结果

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    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):