Cyclo(his-pro) (TFA)

Cyclo(his-pro) (TFA)

中文名称Cyclo(his-pro) (TFA)
中文同义词化合物 CYCLO(HIS-PRO) TFA;(3S,8AS)-3-((1H-咪唑-5-基)甲基)六氢吡咯并[1,2-A]吡嗪-1,4-二酮 三氟乙酸盐
英文名称Cyclo(his-pro) (TFA)
英文同义词Cyclo(his-pro) (TFA);(3S,8aS)-3-((1H-Imidazol-5-yl)methyl)hexahydropyrrolo[1,2-a]pyrazine-1,4-dione 2,2,2-trifluoroacetate
CAS号936749-56-3
分子式C13H15F3N4O4
分子量348.28
EINECS号
相关类别
Mol文件936749-56-3.mol
结构式Cyclo(his-pro) (TFA) 结构式

Cyclo(his-pro) (TFA) 性质

储存条件Store at -20°C, protect from light, stored under nitrogen
溶解度DMSO:260mg/mL(746.53mM);水:125 mg/mL(358.91 mM;超声并用 NaOH 将 pH 调节至 10)
形态固体
颜色白色至米白色
序列Cyclo(His-Pro)

Cyclo(his-pro) (TFA) 用途与合成方法

Cyclo(his-pro) TFA (Cyclo(histidyl-proline) TFA) 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) TFA 可以抑制 NF-κB 核积累。Cyclo(his-pro) TFA 可以穿越脑血屏障并影响多种炎症和应激反应。

NF-κB

Human Endogenous Metabolite

Cyclo(his-pro) TFA (Cyclo(histidyl-proline) TFA; 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) TFA (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) TFA 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.

Cyclo(his-pro) TFA (Cyclo(histidyl-proline) TFA; 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) TFA 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.

安全信息

MSDS信息

更新日期产品编号产品名称CAS号包装价格
2025/12/22HY-101402ACyclo(his-pro) (TFA)
Cyclo(his-pro) TFA
936749-56-31 mg500元
2025/12/22HY-101402ACyclo(his-pro) (TFA)
Cyclo(his-pro) TFA
936749-56-310mM * 1mLin DMSO690元

Cyclo(his-pro) (TFA) 上下游产品信息

"Cyclo(his-pro) (TFA)"相关产品信息
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