上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。
Chol-CTPP
Chol-CTPP 是一种对血脑屏障 (BBB) 和胶质瘤 （glioma） 细胞具有双重靶向作用的配体，能与 Chol-TPP 合成Lip-CTPP 。 Lip-CTPP 是发挥阿霉素 (DOX) 和氯胺达明 (LND) 联合抗胶质瘤 (anti-glioma) 作用的潜在载体。Lip-CTPP 可提高对肿瘤细胞增殖、迁移和侵袭的抑制率，促进细胞凋亡 (apoptosis) 和坏死 (necrosis)，干扰线粒体功能。
Chol-CTPP Chemical Structure
| 规格 |
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是否有货 |
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| 100 mg |
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询价 |
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| 250 mg |
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询价 |
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| 500 mg |
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询价 |
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* Please select Quantity before adding items.
| 生物活性 |
Chol-CTPP is a ligand with dual targeting effect on blood-brain barrier (BBB) and glioma cells. Lip-CTPP can be gained by Chol-CTPP and another mitochondria targeting ligand (Chol-TPP). Lip-CTPP is a promising potential carrier to exert the anti-glioma effect of doxorubicin (DOX) and lonidamine (LND) collaboratively. Lip-CTPP elevates the inhibition rate of tumor cell proliferation, migration and invasion, promote apoptosis and necrosis, and interfere with mitochondrial function[1].
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IC50 & Target |
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体外研究
(In Vitro) |
Lip-CTPP shows satisfying cellular uptake and mitochondrial uptake[1].
Lip-CTPP (0-20 µg/mL DOX and LND, 24 h) shows cytotoxicity and induces apoptosis in C6 cells[1].
Lip-CTPP inhibits intracellular ATP production and has the most severe damage on the membrane potential of mitochondria[1].
Lip-CTPP possesses excellent potential to induce ROS generation[1].
Lip-CTPP (0.5 µg/mL DOX, 48 h) exhibits strong inhibitory effect both on cell migration and invasion[1]
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Cytotoxicity Assay[1]
| Cell Line: |
C6 cells |
| Concentration: |
0.1, 0.5, 2.5, 5, 10, and 20 µg/mL of DOX and LND |
| Incubation Time: |
24 h |
| Result: |
Showed cytotoxicity on C6 cells in a concentration-dependent manner. |
Apoptosis Analysis[1]
| Cell Line: |
C6 cells |
| Concentration: |
0.5 µg/mL DOX and LND |
| Incubation Time: |
24 h |
| Result: |
Performed excellent lethality on C6 cells and the apoptosis and necrosis rate is 3.4 times that of Free DOX + LND. |
Cell Invasion Assay[1]
| Cell Line: |
C6 cells |
| Concentration: |
0.5 µg/mL DOX |
| Incubation Time: |
48 h |
| Result: |
Obviously restricted the invasion of C6 cells. |
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体内研究
(In Vivo) |
Lip-CTPP (3 mg/kg DOX and LND; i.v.; once on day 4, 7, 10 and 13) induces glioma cells apoptosis and inhibits tumor growth[1].
Lip-CTPP can slow down the clearance of free drugs and enhance tumor targeting properties[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: |
Kunming mice (male, 20-25 g), 5 µL of C6 cells (2 × 108 cells/mL) were injected into the striatum[1] |
| Dosage: |
3 mg/kg DOX and LND |
| Administration: |
Tail vein injection, once on day 4, 7, 10 and 13 |
| Result: |
Increased the survival time, decreased tumor area and the density of tumor cells. |
| Animal Model: |
Kunming mice (20-25 g)[1] |
| Dosage: |
10 mg/kg DOX and LND |
| Administration: |
Tail vein injection (Pharmacokinetics Analysis) |
| Result: |
Pharmacokinetic parameters of DOX in blood after administration (mean ± SD, n = 3)[1]
| parameters |
AUC(0-t)
(µg/mL*min) |
MRT (min) |
Tmax (min) |
Cmax (µg/mL) |
t1/2 (min) |
Clz (L/min/kg) |
| Lip-CTPP |
5901.90 ± 406.18 |
291.30 ± 1.18 |
30 |
23.31 ± 0.42 |
231.06 ± 43.35 |
1.68 ± 0.13 |
Pharmacokinetic parameters of DOX in brain after administration (mean ± SD, n = 3)[1]
| parameters |
AUC(0-t)
(µg/mL*min) |
MRT (min) |
Tmax (min) |
Cmax (µg/mL) |
t1/2 (min) |
Clz (L/min/kg) |
| Lip-CTPP |
1757.61 ± 19.35
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| 分子量 |
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| Formula |
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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| 参考文献 |
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