K6PC-5,一种神经酰胺衍生物,是一种鞘氨醇激酶 1 (SPHK1) 激活剂,可引起细胞内钙水平的短暂快速升高。K6PC-5 用于研究涉及异常角质形成细胞的皮肤疾病、神经退行性疾病和病毒感染。
生物活性 | K6PC-5, a ceramide derivative, is asphingosine kinase 1(SPHK1)activator and elicites a rapid transient increase in intracellular calcium levels. K6PC-5 has the potential for skin diseases involving abnormal keratinocyte, and neurodegeneration and virusinfectionresearch[1][2][3]. |
IC50& Target | |
体外研究 (In Vitro) | K6PC-5 (1-10 μM; 24 h) increases the involucrin and loricrin levels in a dose-dependent manner in normal human epidermal keratinocytes (NHEKs). K6PC-5 promotes differentiation and proliferation of keratinocytes via intracellular Ca2+signaling. In addition, K6PC-5 stimulates the phosphorylation of p42/44 extracellular signal-regulated kinase and c-Jun N-terminal kinase[1]. K6PC-5 (1-10 μM; 24 h) promotes fibroblasts proliferation and collagen synthesis in human fibroblasts. K6PC-5 induces intracellular Ca2+concentration ([Ca2+]i) oscillations in human fibroblasts[2]. K6PC-5 (10, 25, and 50 μM; 48 h) significantly attenuates EBOV-induced infection in EBOV-infected EA.hy926 cells. K6PC-5 significantly reduces the virus titers in supernatants of infected cells and strikingly decreased the amount of VP40 in a concentration-dependent manner[3].
Western Blot Analysis[1] Cell Line: | Normal human epidermal keratinocytes (NHEKs) | Concentration: | 1 μM, 5 μM, 10 μM | Incubation Time: | 24 h | Result: | Increased the involucrin and loricrin levels in a dose-dependent manner. |
Cell Proliferation Assay[2] Cell Line: | Human fibroblasts | Concentration: | 1 μM, 5 μM, 10 μM | Incubation Time: | 24 h | Result: | Promoted fibroblast proliferation and procollagen production in human fibroblasts significantly. |
|
体内研究 (In Vivo) | In intrinsically aged hairless mice (56 weeks old), 1% K6PC-5 is applied topically for 2 weeks. This K6PC-5 treatment significantly increases both the number of dermal fibroblasts and collagen production. As a consequence, dermal thickness also increased significantly[2].
Animal Model: | Intrinsically aged hairless mice (56 weeks old)[2] | Dosage: | 1% (vehicle (PEG:EtOH = 7:3)) | Administration: | Topical application; twice daily for 2 weeks | Result: | Enhanced fibroblast proliferation, collagen production, and eventually increased dermal thickness. |
|
分子量 | |
性状 | |
Formula | |
CAS 号 | |
运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -20°C | 3 years | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
|
溶解性数据 | In Vitro: DMSO : 100 mg/mL(291.12 mM;Need ultrasonic) 配制储备液 1 mM | 2.9112 mL | 14.5560 mL | 29.1121 mL | 5 mM | 0.5822 mL | 2.9112 mL | 5.8224 mL | 10 mM | 0.2911 mL | 1.4556 mL | 2.9112 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。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (7.28 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (7.28 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (7.28 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (7.28 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (7.28 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (7.28 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
|