计算溶液所需的质量、体积或浓度。
提供 ≥99% 纯度,适用于对基线干扰要求严格的色谱和分析工作流程。
避光,-20°C储存,充氩。超低温运输 。请查阅批次 COA 获取详细规格。
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在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
Cyclo(his-pro) TFA (Cyclo(histidyl-proline) TFA) is an orally active cyclic dipeptide structurally related to tyreotropin-releasing hormone Cyclo(his-pro) TFA could inhibit NF-κB nuclear accumulation. Cyclo(his-pro) TFA can cross the brain-blood-barrier and affect diverse inflammatory and stress responses .
In Vitro
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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell 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.
In Vivo
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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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.
Form:Solid
IC50& Target:NF-κB Human Endogenous Metabolite
分类树(Taxonomy Tree)
| 界(kingdom) | 有机化合物 |
|---|---|
| 超类(Superclass) | 有机酸及其衍生物 |
| 类(Class) | 羧酸及其衍生物 |
| 亚类(Subclass) | 氨基酸、肽和类似物 |
| 中间层级节点(Intermediate Tree Nodes) | 氨基酸及其衍生物 |
| 直接上位类(Direct Parent) | α氨基酸及其衍生物 |
| 其他上位类(Alternative Parents) | 2,5-二氧代哌嗪 N-烷基哌嗪 叔羧酸酰胺 吡咯烷 咪唑类 杂芳族化合物 α-卤代羧酸 仲羧酸酰胺 内酰胺类 一元羧酸及其衍生物 羧酸 氮杂环化合物 有机光子化合物 有机氮化合物 有机氟化物 有机氧化物 碳氢化合物衍生物 羰基化合物 烷基氟化物 |
| 分子骨架(Molecular Framework) | 暂无 |
| 取代基(Substituents) | 1,4-二氮杂环丁烷 - 2,5-二氧代哌嗪 - 氟化烷基 - 烷基溴化物 - α-氨基酸或其衍生物 - α-卤代羧酸 - α-卤代羧酸或其衍生物 - 芳香族杂多环化合物 - 氮杂环 - 吡唑 - 羰基 - 羧酰胺基 - 羧酰胺基 - 二氧杂哌嗪 - 杂芳香族化合物 - 烃衍生物 - 咪唑 - 肟 - 单羧酸或其衍生物 - N-烷基哌嗪 - 有机硝基化合物 - 有机氧化物 - 有机氧化合物 - 有机氟化物 - 有机卤化物 - 有机杂环化合物 - 有机氮化合物 - 有机氧化合物 - 有机氮化合物 - 哌嗪 - 吡咯烷 - 醛基 - 叔羧酸酰胺 |
| 描述(Description) | 该化合物属于α-氨基酸及其衍生物类有机化合物。这类氨基酸的氨基连接在羧基团直接相邻的碳原子(α碳)上,或其衍生物。 |
| 外部描述符(External Descriptors) | 暂无 |