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Cyclo(his-pro) (TFA)

Cyclo(his-pro) (TFA), 936749-56-3, 結(jié)構(gòu)式
Cyclo(his-pro) (TFA)
CAS號(hào):
936749-56-3
英文名:
Cyclo(his-pro) (TFA)
英文別名:
Cyclo(his-pro) (TFA);(3S,8aS)-3-((1H-Imidazol-5-yl)methyl)hexahydropyrrolo[1,2-a]pyrazine-1,4-dione 2,2,2-trifluoroacetate
中文名:
Cyclo(his-pro) (TFA)
中文別名:
化合物 CYCLO(HIS-PRO) TFA;(3S,8AS)-3-((1H-咪唑-5-基)甲基)六氫吡咯并[1,2-A]吡嗪-1,4-二酮 三氟乙酸鹽
CBNumber:
CB45848740
分子式:
C13H15F3N4O4
分子量:
348.28
MOL File:
936749-56-3.mol

Cyclo(his-pro) (TFA)化學(xué)性質(zhì)

儲(chǔ)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
安全信息

Cyclo(his-pro) (TFA)性質(zhì)、用途與生產(chǎn)工藝

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(yīng)激反應(yīng)。

靶點(diǎn)

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.

Cyclo(his-pro) (TFA) 上下游產(chǎn)品信息

上游原料

下游產(chǎn)品

Cyclo(his-pro) (TFA) 試劑級(jí)價(jià)格

更新日期產(chǎn)品編號(hào)產(chǎn)品名稱CAS編號(hào)包裝價(jià)格
2025/02/05HY-101402ACyclo(his-pro) (TFA)
Cyclo(his-pro) TFA
936749-56-31 mg500元
2025/02/05HY-101402ACyclo(his-pro) (TFA)
Cyclo(his-pro) TFA
936749-56-310mM * 1mLin DMSO690元

Cyclo(his-pro) (TFA) 生產(chǎn)廠家

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936749-56-3, Cyclo(his-pro) (TFA) 相關(guān)搜索:

  • 抑制劑
  • (3S,8AS)-3-((1H-咪唑-5-基)甲基)六氫吡咯并[1,2-A]吡嗪-1,4-二酮 三氟乙酸鹽
  • 化合物 CYCLO(HIS-PRO) TFA
  • 936749-56-3
  • (3S,8aS)-3-((1H-Imidazol-5-yl)methyl)hexahydropyrrolo[1,2-a]pyrazine-1,4-dione 2,2,2-trifluoroacetate
  • Cyclo(his-pro) (TFA)
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