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CDN1163
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CDN1163图片
CAS NO:892711-75-0
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品介绍
CDN1163 是一种肌膜/内质网Ca2+-ATPase (SERCA)的变构激活剂,可改善 Ca2+稳态。CDN1163 可减轻糖尿病和代谢紊乱。
生物活性

CDN1163 is an allostericsarco/endoplasmic reticulum Ca2+-ATPase (SERCA)activator that improves Ca2+homeostasis. CDN1163 attenuates diabetes and metabolic disorders[1].

IC50& Target

SERCA[1]

体外研究
(In Vitro)

CDN1163 (10 μM; 24 hours; rat cardiac myocyte cells) treatment reduces high glucose-induced resistin and nuclear NFATc expression and increases the phosphorylation of AMPKα in a time-dependent manner[2].

Western Blot Analysis[2]

Cell Line:Rat cardiac myocyte cells (H9c2)
Concentration:10 μM
Incubation Time:24 hours
Result:High glucose-induced resistin and nuclear NFATc expression are significantly reduced. The phosphorylation of AMPKα is increased in a time-dependent manner.
体内研究
(In Vivo)

CDN1163 (50 mg/kg; intraperitoneal injection; for 5 days; maleob/obmice and leanob/+mice) increases SERCA2 Ca2+-ATPase activity, decreases endoplasmic reticulum (ER) stress-induced cell death in vitro and improves liver Ca2+transport activity. CDN1163 reduces blood glucose levels and improves metabolic parameters and gluconeogenic gene expression, reverses hepatic steatosis, inhibits ER stress and ER stress-induced apoptosis, and improves mitochondrial efficiency inob/obmice in vivo[1].

Animal Model:Male 8-10-week oldob/obmice and leanob/+mice[1]
Dosage:50 mg/kg
Administration:Intraperitoneal injection; for 5 days
Result:Markedly lowered fasting blood glucose, improved glucose tolerance, and ameliorated hepatosteatosis but did not alter glucose levels or body weight. Increased expression of uncoupling protein 1 (UCP1) and UCP3 in brown adipose tissue and reduced the hepatic expression of genes involved in gluconeogenesis and lipogenesis, attenuated ER stress response and ER stress-induced apoptosis, and improved mitochondrial biogenesis, possibly through SERCA2-mediated activation of AMP-activated protein kinase pathway.
分子量

320.39

性状

Solid

Formula

C20H20N2O2

CAS 号

892711-75-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL(312.12 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM3.1212 mL15.6060 mL31.2120 mL
5 mM0.6242 mL3.1212 mL6.2424 mL
10 mM0.3121 mL1.5606 mL3.1212 mL
*

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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40%PEG300   5%Tween-80   45% saline

    Solubility: ≥ 2.5 mg/mL (7.80 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.80 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin saline)

    Solubility: 2.5 mg/mL (7.80 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (7.80 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 2.5 mg/mL (7.80 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.80 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在本网站选购。