环(组氨酰-脯氨酰)

生物活性靶点体外研究体内研究环(组氨酰-脯氨酰) 试剂级价格

环(组氨酰-脯氨酰)

CAS号:53109-32-3
英文名:CYCLO(-HIS-PRO)
中文名:环(组氨酰-脯氨酰)
CBNumber:CB8279260
分子式:C11H14N4O2
分子量:234.25
MOL File:53109-32-3.mol

环(组氨酰-脯氨酰)化学性质

熔点 :162-164 °C
沸点 :659.3±48.0 °C(Predicted)
密度 :1.41±0.1 g/cm3(Predicted)
储存条件 :2-8°C
溶解度 :DMF: 1 mg/ml; DMSO: 1 mg/ml; Ethanol: 1 mg/ml; PBS (pH 7.2): 1 mg/ml
形态 :A neat oil
酸度系数(pKa) :12.73±0.40(Predicted)
颜色 :Light yellow to yellow

安全信息

WGK Germany :3

环(组氨酰-脯氨酰)性质、用途与生产工艺

生物活性 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。
靶点

NF-κB

Human Endogenous Metabolite

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.