1. Membrane Transporter/Ion Channel
  2. ATP Synthase
  3. Cyclocreatine

Cyclocreatine 是通过提供高水平的 ATP 用作一种脑渗透和有效的生物能量保护剂,是一种 Creatine 类似物。Cyclocreatine 可以被肌酸激酶磷酸化和去磷酸化。Cyclocreatine 抑制肌酸代谢,从而改善了肌酸转运蛋白缺乏小鼠模型的认知、自闭症和癫痫表型。Cyclocreatine 对狗和大鼠缺血损伤有保护作用,并在早期再灌注时促进心脏恢复。Cyclocreatine 减少淀粉样蛋白-β 病变 TREM2 缺陷小鼠斑块邻近神经元营养不良。Cyclocreatine 有望用于缺血性心脏病、心血管疾病、阿尔茨海默病,其他与小胶质细胞功能障碍相关的神经退行性疾病和前列腺癌的研究。

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Cyclocreatine Chemical Structure

Cyclocreatine Chemical Structure

CAS No. : 35404-50-3

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10 mM * 1 mL in Water ¥550
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MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Cyclocreatine, a creatine analogue, acts as a brain-penetrant and potent bioenergetic protective agent by providing high levels of ATP. Cyclocreatine can be phosphorylated and dephosphorylated by creatine kinases. Cyclocreatine suppresses creatine metabolism ameliorating the cognitive, autistic and epileptic phenotype in a mouse model of creatine transporter defciency. Cyclocreatine protects against ischemic injury and enhances cardiac recovery during early reperfusion in dogs and rats. Cyclocreatine decreases plaque-adjacent neuronal dystrophy in TREM2-deficient mice with amyloid-β pathology. Cyclocreatine is proming for research of ischemic heart disease, cardiovascular diseases, Alzheimer’s disease and other neurodegenerative diseases associated with microglial dysfunction, prostate cancer[1][2][3][4][5].

体外研究
(In Vitro)

Cyclocreatine (5 或 10 mM, 24 或 40 小时) 改善骨髓源性巨噬细胞外酸化率 (ECAR),同时减少自噬 (Autophagy),增加 mTOR 信号传导和细胞活力[2]
Cyclocreatine (0-50 mM, 24 小时) 抑制前列腺癌细胞的肌酸代谢,增殖,肌酸摄取[3]

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

Western Blot Analysis[2]

Cell Line: Bone marrow-derived macrophages
Concentration: 5 or 10 mM
Incubation Time: incubation for 24 or 40 h
Result: Increased mTOR signaling and cell viability in bone marrow-derived macrophages.

Cell Proliferation Assay[3]

Cell Line: Murine and human prostate cancer cells
Concentration: 0-50 mmol/L
Incubation Time: 24 h
Result: Impaired in vitro proliferation of both human and murine prostate cancer cells
体内研究
(In Vivo)

Cyclocreatine (500 mg/kg, 静脉注射, 单次注射, 持续 60 分钟) 在急性心肌梗死 (AMI) 完整犬模型中,比对照组 (生理盐水) 更恢复心脏收缩功能,心肌细胞损伤明显减轻[1]
Cyclocreatine (0.28 mg/g, 喝, 每天提供,持续 1 个月) 缓解 TREM2-/- 5XFAD 小鼠的小胶质细胞增生和聚集,并减轻神经营养不良[2]
Cyclocreatine (40 mg, 管饲, 每天强饲,持续 1 个月) 在小鼠肝转移模型中显著减少肝转移负担并影响前列腺癌进展[3]

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

Animal Model: AMI-intact dog model[1]
Dosage: 500 mg/kg
Administration: i.v., a single dose for 60 min
Result: Preserved 85% of pre-ischemic ATP level (loss of only 15%) and 97% of the CrP (loss of 3%) during ischemia, as well as immediately restored over 80% of contractile function during the 2 h of reperfusion in AMI-intact dog model.
Animal Model: 5XFAD and TREM2−/− 5XFAD mice
Dosage: 0.28 mg/g
Administration: Drinking water supplementation with cyclocreatine daily from 10-week to 8 months
Result: Improved microglial metabolism and the protective response to Aβ plaques in TREM2-deficient 5XFAD mice.
分子量

143.15

Formula

C5H9N3O2

CAS 号
性状

固体

颜色

White to 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
细胞实验: 

1M HCl 中的溶解度 : 100 mg/mL (698.57 mM; 超声助溶; 酸性条件溶解 (HCL 调节,pH≈2))

H2O 中的溶解度 : 5 mg/mL (34.93 mM; 超声助溶 (<60°C))

DMSO 中的溶解度 : < 1 mg/mL (insoluble or slightly soluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 6.9857 mL 34.9284 mL 69.8568 mL
5 mM 1.3971 mL 6.9857 mL 13.9714 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。

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

  • 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

动物实验:

以下溶解方案,请直接配制工作液。建议现用现配,在短期内尽快用完。 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。

  • 方案 一

    请依序添加每种溶剂: PBS

    Solubility: 10 mg/mL (69.86 mM); 澄清溶液; 超声加热助溶

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
您所需的储备液浓度超过该产品的实测溶解度,如有需要,请与 MCE 中国技术支持联系。
纯度 & 产品资料

纯度: 99.65%

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
H2O / 1M HCl 1 mM 6.9857 mL 34.9284 mL 69.8568 mL 174.6420 mL
5 mM 1.3971 mL 6.9857 mL 13.9714 mL 34.9284 mL
10 mM 0.6986 mL 3.4928 mL 6.9857 mL 17.4642 mL
15 mM 0.4657 mL 2.3286 mL 4.6571 mL 11.6428 mL
20 mM 0.3493 mL 1.7464 mL 3.4928 mL 8.7321 mL
25 mM 0.2794 mL 1.3971 mL 2.7943 mL 6.9857 mL
30 mM 0.2329 mL 1.1643 mL 2.3286 mL 5.8214 mL
1M HCl 40 mM 0.1746 mL 0.8732 mL 1.7464 mL 4.3660 mL
50 mM 0.1397 mL 0.6986 mL 1.3971 mL 3.4928 mL
60 mM 0.1164 mL 0.5821 mL 1.1643 mL 2.9107 mL
80 mM 0.0873 mL 0.4366 mL 0.8732 mL 2.1830 mL
100 mM 0.0699 mL 0.3493 mL 0.6986 mL 1.7464 mL

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
Cyclocreatine
目录号:
HY-W017540
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