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。
生物活性 | Cyclo(his-pro) (Cyclo(histidyl-proline)) is an orally active cyclic dipeptide structurally related to tyreotropin-releasing hormone[1]. Cyclo(his-pro) could inhibitNF-κBnuclear accumulation. Cyclo(his-pro) can cross the brain-blood-barrier and affect diverse inflammatory and stress responses[2]. |
IC50& Target | NF-κB | Human Endogenous Metabolite |
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体外研究 (In Vitro) | 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[2]. 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[2]. Cyclo(his-pro) inhibits NF-κB nuclear accumulation induced by paraquat in rat pheochromocytoma PC12 cells via the Nrf2/heme oxygenase-1 pathway[2].
Western Blot Analysis[1] 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. |
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体内研究 (In Vivo) | 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[2]. 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[3].
Animal Model: | Sixty two/three month-old male C57BL/6 mice (25-30 g)[2] | 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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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Sealed storage, away from moisture Powder | -80°C | 2 years | | -20°C | 1 year |
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
溶解性数据 | In Vitro: H2O : ≥ 30 mg/mL(128.07 mM) *"≥" means soluble, but saturation unknown. 配制储备液 1 mM | 4.2689 mL | 21.3447 mL | 42.6894 mL | 5 mM | 0.8538 mL | 4.2689 mL | 8.5379 mL | 10 mM | 0.4269 mL | 2.1345 mL | 4.2689 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 |