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Cyclo(his-pro)
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。
Cyclo(his-pro)图片
CAS NO:53109-32-3
包装与价格:
包装价格(元)
10 mM * 1 mL in Water电议
1mg电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品名称
Cyclo(histidyl-proline)
Histidylproline diketopiperazine
产品介绍
Cyclo(his-pro) (Cyclo(histidyl-proline)) 是一种具有口服活性的,结构上与促甲状腺激素释放激素相关的环状二肽。Cyclo(his-pro) 可以抑制NF-κB核积累。Cyclo(his-pro) 可以穿越脑血屏障并影响多种炎症和应激反应。
生物活性

Cyclo(his-pro) (Cyclo(histidyl-proline)) is an orally active cyclic dipeptide structurally related to tyreotropin-releasing hormone[1]. Cyclo(his-pro) could inhibitNF-κBnuclear accumulation. Cyclo(his-pro) can cross the brain-blood-barrier and affect diverse inflammatory and stress responses[2].

IC50& Target

NF-κB

 

Human Endogenous Metabolite

 

体外研究
(In Vitro)

cyclo(his-pro) (Cyclo(histidyl-proline); 50 μM; 1-48 hours) increases the nuclear level of Nrf2 and inhibits NF-κB nuclear translocation. Cyclo(His-Pro) alone has no effect on nuclear translocation of these transcription factors[2].
cyclo(his-pro) (50 μM; prior to PQ exposure for 48 hours) abolishes protein nitration that followed paraquat (PQ) exposure and lessenes its functional consequences, as shown by decrease in cell apoptosis, detected by caspase 3 activity and by cytochrome c release[2].
Cyclo(his-pro) inhibits NF-κB nuclear accumulation induced by paraquat in rat pheochromocytoma PC12 cells via the Nrf2/heme oxygenase-1 pathway[2].

Western Blot Analysis[1]

Cell Line:PC12 cells
Concentration:50 μM
Incubation Time:1, 2, 4, 8, 24, 48 hours
Result:Increased the nuclear level of Nrf2 and inhibited NF-κB nuclear translocation.
体内研究
(In Vivo)

Cyclo(his-pro) (Cyclo(histidyl-proline); 1.8 mg/ear; topical application on the right ear; 30 min prior to TPA) reduces TPA-induced ear oedema confirming that it can exert anti-inflammatory effect[2].
Cyclo(his-pro) exerts in vivo anti-inflammatory effects in the central nervous system by down-regulating hepatic and cerebral TNFα expression thereby counteracting LPS-induced gliosis. Moreover, by up-regulating Bip, Cyclo(his-pro) increases the ER stress sensitivity andtriggers the unfolded protein response to alleviate the ER stress[3].

Animal Model:Sixty two/three month-old male C57BL/6 mice (25-30 g)[2]
Dosage:1.8 mg/ear
Administration:Topical application on the right ear; 30 min prior to TPA
Result:Reduced TPA-induced ear oedema.
分子量

234.25

性状

Solid

Formula

C11H14N4O2

CAS 号

53109-32-3

Sequence Shortening

Cyclo(HP)

结构分类
  • Others
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Sealed storage, away from moisture

Powder-80°C2 years
-20°C1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

H2O : ≥ 30 mg/mL(128.07 mM)

*"≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM4.2689 mL21.3447 mL42.6894 mL
5 mM0.8538 mL4.2689 mL8.5379 mL
10 mM0.4269 mL2.1345 mL4.2689 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 (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。