1. 多肽产品
  2. 多肽及其衍生物
  3. 多肽药物递送
  4. 响应肽
  5. pH-Low Insertion Peptide TFA

pH-Low Insertion Peptide TFA  (Synonyms: pHLIP TFA)

目录号: HY-P4116A 纯度: 96.37%
COA 产品使用指南

pH-Low Insertion Peptide TFA (pHLIP) 是一种短的,pH 响应肽,能够在酸性 pH 下插入细胞膜形成跨膜螺旋。pH-Low Insertion Peptide TFA 以高特异性靶向肿瘤早期和转移阶段的酸性肿瘤微环境,作为特异性配体使用。pH-Low Insertion Peptide TFA 成功修饰聚赖氨酸聚合物,使其具有 pH 响应能力。基于 pH-Low Insertion Peptide TFA 的癌症靶向为监测代谢变化提供了机会,并有选择地向肿瘤输送成像和治疗药物。

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Custom Peptide Synthesis

pH-Low Insertion Peptide TFA Chemical Structure

pH-Low Insertion Peptide TFA Chemical Structure

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5 mg ¥1500
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Customer Review

Other Forms of pH-Low Insertion Peptide TFA:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

pH-Low Insertion Peptide TFA (pHLIP TFA) is a short, pH-responsive peptide capable of inserting across a cell membrane to form a transmembrane helix at acidic pH. pH-Low Insertion Peptide TFA targets the acidic tumor microenvironment for tumors at early and metastatic stages with high specificity, used as a specific ligand. pH-Low Insertion Peptide TFA successfully modifys polylysine polymers to have the pH-responsive capability. pH-Low Insertion Peptide TFA -based targeting of cancer presents an opportunity to monitor metabolic changes and to selectively deliver imaging and therapeutic agents to tumors[1][2][3].

体外研究
(In Vitro)

pH-Low Insertion Peptide TFA (5 μM, 2 h) 与肽核酸 (peptide nucleic acid, PNA) 联合使用可显著增加 pH 值为 6.2 时 A549 细胞 PNA 的递送量[3]

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

Immunofluorescence[3]

Cell Line: A549 cells
Concentration: 5 μM
Incubation Time: 2 h
Result: Significantly increases PNA delivery combined with PNA at pH 6.2 in A549 cells.
体内研究
(In Vivo)

pH-Low Insertion Peptide TFA (50 μM, 单次尾静脉注射, 4, 24, 48 小时) 变体在小鼠 4T1 异种移植模型下显示 pH 依赖性肿瘤靶向和不同的血液清除率,总体肿瘤空间分布是相同的[2]
pH-Low Insertion Peptide TFA (10 μM, 静脉注射, 单次 24 小时 ) 在 MMTV-Py MT 小鼠中可以清楚地区分主要肿瘤细胞和非恶性间质组织的区域,还可以密切积累缺氧标志物 Pimonidazole (HY-105129A),并与酸性葡萄糖代谢物的产生有关[2]
pH-Low Insertion Peptide TFA (0.2 μmol/kg, 静脉注射, 单次 24 小时) 与 PNA 联用在接种黑色素瘤肿瘤的小鼠中表现出良好的肿瘤靶向性[3]

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

Animal Model: Murine 4T1 xenograft model[2]
Dosage: 50 μM
Administration: a single tail vein injection, tumors collected at 4, 24, and 48 h after administration
Result: The spatial distribution and the intensity profiles of all pHLIP TFAs in tumors were identical in murine 4T1 xenograft mode.
Animal Model: FVB/N-Tg(MMTV-PyVT)634Mul/J transgenic female mice developed palpable mammary tumors at 12-15 weeks of age[2]
Dosage: 10 μM
Administration: i.v., a single dose for 24 h
Result: Clearly differentiated between regions of primarily tumor cells and nonmalignant stromal tissues.
Animal Model: 6-week old C57BL/6 mice seeded melanoma tumors[3]
Dosage: 0.2 μmol/kg
Administration: intravenously injected via the retro-orbital sinus, a single dose for 24 h
Result: All the pH-Low Insertion Peptide TFA-PNAs demonstrated excellent tumor targeting.
分子量

4054.57 (free base)

Formula

C189H282N42O55S.xC2HF3O2

性状

固体

颜色

White to off-white

Sequence

Ala-Cys-Glu-Gln-Asn-Pro-Ile-Tyr-Trp-Ala-Arg-Tyr-Ala-Asp-Trp-Leu-Phe-Thr-Thr-Pro-Leu-Leu-Leu-Leu-Asp-Leu-Ala-Leu-Leu-Val-Asp-Ala-Asp-Glu-Thr

Sequence Shortening

ACEQNPIYWARYADWLFTTPLLLLDLALLVDADET

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Sealed storage, away from moisture and light

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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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产品名称:
pH-Low Insertion Peptide TFA
目录号:
HY-P4116A
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