Cyclo(his-pro) (Synonyms:Cyclo(histidyl-proline; Histidylproline diketopiperazine))
目录号 : KM5781 CAS No. : 53109-32-3 纯度 : 98%

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。

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生物活性

Cyclo(his-pro) (Cyclo(histidyl-proline)) is an orally active cyclic dipeptide structurally related to tyreotropin-releasing hormone. Cyclo(his-pro) could inhibit NF-κB nuclear accumulation. Cyclo(his-pro) can cross the brain-blood-barrier and affect diverse inflammatory and stress responses.

体外研究

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.
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.
Cyclo(his-pro) inhibits NF-κB nuclear accumulation induced by paraquat in rat pheochromocytoma PC12 cells via the Nrf2/heme oxygenase-1 pathway.

Western Blot Analysis

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

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.
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.

Animal Model: Sixty two/three month-old male C57BL/6 mice (25-30 g)
Dosage: 1.8 mg/ear
Administration: Topical application on the right ear; 30 min prior to TPA
Result: Reduced TPA-induced ear oedema.
分子式
C11H14N4O2
分子量
234.25
CAS号
53109-32-3
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -80°C 2 years
-20°C 1 year
In solvent -80°C 6 months
-20°C 1 month
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 mg 5 mg 10 mg
1 mM 4.2689 mL 21.3447 mL 42.6894 mL
5 mM 0.8538 mL 4.2689 mL 8.5379 mL
10 mM 0.4269 mL 2.1345 mL 4.2689 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°C, 6 months; -20°C, 1 month。-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。

The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2