Chol-CTPP

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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

Chol-CTPP Chemical Structure

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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].

IC50 & Target

Apoptosis, ROS[1]

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]

Shanghai Jinpan Biotech Co Ltd 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.

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].

Shanghai Jinpan Biotech Co Ltd 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

分子量

2884.62

Formula

C144H263N3O53

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.

参考文献
  • [1]. Jiaqi Lu, et al. Multiple targeted doxorubicin-lonidamine liposomes modified with p-hydroxybenzoic acid and triphenylphosphonium to synergistically treat glioma. Eur J Med Chem. 2022 Feb 15;230:114093.

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