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936749-56-3

中文名稱 Cyclo(his-pro) (TFA)
英文名稱 Cyclo(his-pro) (TFA)
CAS 936749-56-3
分子式 C13H15F3N4O4
分子量 348.28
MOL 文件 936749-56-3.mol
更新日期 2023/03/20 15:41:21
936749-56-3 結(jié)構(gòu)式 936749-56-3 結(jié)構(gòu)式

基本信息

中文別名
化合物 CYCLO(HIS-PRO) TFA
英文別名
Cyclo(his-pro) (TFA)

物理化學性質(zhì)

儲存條件Store at -20°C, protect from light, stored under nitrogen
溶解度DMSO: 260 mg/mL (746.53 mM); Water: 125 mg/mL (358.91 mM; ultrasonic and adjust pH to 10 with NaOH)
形態(tài)Solid
顏色White to off-white
Cyclo(his-pro) (TFA)價格(試劑級)
報價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2024/08/19HY-101402ACyclo(his-pro) (TFA)
Cyclo(his-pro) TFA
936749-56-31 mg500元
2024/08/19HY-101402ACyclo(his-pro) (TFA)
Cyclo(his-pro) TFA
936749-56-310mM * 1mLin DMSO690元
2024/08/19HY-101402ACyclo(his-pro) (TFA)
Cyclo(his-pro) TFA
936749-56-35mg900元

常見問題列表

生物活性
Cyclo(his-pro) TFA (Cyclo(histidyl-proline) TFA) 是一種具有口服活性的,結(jié)構(gòu)上與促甲狀腺激素釋放激素相關(guān)的環(huán)狀二肽。Cyclo(his-pro) TFA 可以抑制 NF-κB 核積累。Cyclo(his-pro) TFA 可以穿越腦血屏障并影響多種炎癥和應激反應。
靶點

NF-κB

Human Endogenous Metabolite

體外研究

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.
體內(nèi)研究

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.
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