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PiF 是一种对胰腺 β 细胞具有高度特异性的荧光探针 (Ex/Em = 535 nm/565 nm),其荧光信号在体外实验中随胰岛素浓度升高而显著增强。PiF 能够在小鼠肝脏中可视化经门静脉移植的大鼠和人胰岛,且肝脏背景信号低。PiF 的氟原子可被放射性 18F 替换,从而制备成 PET 示踪剂。PiF 可用于 1 型糖尿病的研究。

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PiF

PiF Chemical Structure

CAS No. : 2688758-23-6

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PiF is a fluorescent probe with high specificity for pancreatic β-cells (Ex/Em = 535 nm/565 nm), and its fluorescence signal increases significantly with elevated insulin concentrations in in vitro experiments. PiF enables visualization of rat and human islets transplanted via the portal vein in mouse livers with low liver background signals. The fluorine atom of PiF can be replaced by radioactive 18F to prepare a PET tracer. PiF can be used for research on type 1 diabetes[1].

体外研究
(In Vitro)

PiF (0.5 μM; 30 min) 在无细胞的 20 mM HEPES 缓冲体系 (pH 7.4) 中孵育 30 min 后,对牛胰岛素呈现剂量依赖性的荧光响应[1]
PiF (1 μM; 30 min) 在无细胞的 20 mM HEPES 缓冲体系 (pH 7.4) 中孵育 30 min 后,对胰岛素的选择性远高于胰高血糖素和人血清白蛋白[1]
PiF (1 μM; 1 h) 可在分离的小鼠胰岛中选择性染色胰腺 β 细胞 (而非 α 细胞),孵育 1 h 后,经细胞特异性标志物共染色及分选细胞群的基因表达分析证实这一结果[1]
PiF (0.25-2 μM; 1 h) 以浓度依赖、无毒性的方式选择性染色分离的大鼠胰岛,孵育 1 h 后荧光强度与探针浓度呈线性相关[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

PiF (300 μM/250 μL; 尾静脉注射; 单次给药) 可选择性染色胰腺 β 细胞,能够检测 Streptozotocin (HY-13753) 诱导的 1 型糖尿病小鼠中减少的 β 细胞量;与糖尿病小鼠胰腺相比,对照组胰腺的荧光强度高 5 倍以上,胰岛数量多 3.4 倍,单胰岛强度高 2 倍以上[1]
[18F]PiF (~7.4 MBq; 静脉注射;单次给药),作为 PiF 的 PET 示踪剂形式,可选择性在健康 ICR 小鼠的胰腺 β 细胞中聚集,注射后 30 分钟时摄取量达到峰值 16.1 %ID/g,且其特异性摄取已通过阻断实验得到证实[1]

指南 (以下是我们推荐的方案,本方案仅提供指南,应根据您的具体需要进行修改)。
快速可视化小鼠胰腺组织中的 β 细胞/胰岛
1. 配制试剂:PiF 储备液 (溶于 DMSO),临用前用含 2% BSA 的 PBS 稀释至 300 μM。
2. 操作程序:
2.1 活体注射:将 PiF 工作液 (300 μM, 250 μL) 通过小鼠尾静脉注射入体内。
2.2 孵育与取材:
孵育 1 小时,使探针循环并特异性富集于胰腺 β 细胞。
处死小鼠,迅速取出胰腺组织。
2.3 组织冷冻 (无需固定/脱水):
将新鲜取出的胰腺组织直接置于 Tissue-Freezing Media (TFM/OCT) 中,在干冰上冷冻。
此优化流程跳过了传统 4% 多聚甲醛固定和 30% 蔗糖脱水步骤。
2.4 切片:
使用冷冻切片机将组织切成 20 μm 厚 的冰冻切片,贴附于载玻片上。
2.5 直接染色与观察:
直接将 TFM/OCT 覆盖的切片置于荧光显微镜下,用 TRITC 滤光片 (Ex 535 nm / Em 565 nm) 观察。PiF 染色的胰岛 (β 细胞核心) 将呈现强红色荧光。
可选清洗:如需去除包埋剂背景,可在切片上滴加 PBS 孵育/冲洗,再观察 PiF 特异性信号。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6[1]
Dosage: 300 μM
Administration: i.v.; single 250 μL injection via tail vein
Result: Showed over 5 times higher average fluorescence intensity in pancreases of control nondiabetic mice than in streptozotocin-treated diabetic mice.
Detected 3.4 times more PiF-stained islets in control mice (3803 total) than in diabetic mice (1116 total).
Demonstrated over 2 times higher average fluorescence intensity per islet in control mice than in diabetic mice.
Animal Model: ICR[1]
Dosage: ~7.4 MBq
Administration: i.v.; single injection
Result: Showed an initial pancreatic uptake of 10.8 %ID/g.
Reached a maximum uptake of 16.1 %ID/g at 30 minutes post-injection.
Was gradually washed out from the pancreas over the subsequent 90 minutes.
Showed significantly reduced pancreatic radioactivity uptake in a blocking experiment with excess cold PiF, confirming target specificity.
Clinical Trial
分子量

554.55

Formula

C26H26F4N2O5S

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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