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Dorsomorphin (Compound C) Sale

(Synonyms: 6-[4-[2-(1-哌啶基)乙氧基]苯基]-3-(4-吡啶基)吡唑并[1,5-A]嘧啶,Compound C) 目录号 : GC17243

Dorsomorphin(Compound C)是一种细胞渗透的AMPK抑制剂。

Dorsomorphin (Compound C) Chemical Structure

Cas No.:866405-64-3

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10mM (in 1mL DMSO)
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5mg
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50mg
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Description

Dorsomorphin (Compound C) is an agent that used as a cell-permeable AMPK inhibitor. It could rescue the antiproliferative actions of AICAR and metformin. Moreover, dorsomorphin (Compound C) is also used as a selective inhibitor of the BMP pathway. Compound C could inhibit a number of kinases other than AMPK.[1]

In vitro experiments indicate that Compound C inhibits AMPK activity and proliferation of human glioma cells. Dorsomorphin (Compound C) also reduces the apoptosis of cells induced by cisplatin, and decreases the expression of c-caspase3 and c-PARP in cisplatin treatment.

In vivo study demonstrate compound C attenuates cisplatin-induced nephrotoxicity in mice, and alleviates c-caspase 3 and c-PARP induced by cisplatin in kidney tissues.[1][2]

References:
[1].Liu X, et al. The AMPK inhibitor compound C is a potent AMPK-independent antiglioma agent. Mol Cancer Ther. 2014 Mar;13(3):596-605.
[2].Li F, et al. Compound C Protects Against Cisplatin-Induced Nephrotoxicity Through Pleiotropic Effects. Front Physiol. 2020 Dec 23;11:614244.

Dorsomorphin(Compound C)是一种细胞渗透的AMPK抑制剂。它可以挽救AICAR和二甲双胍的抗增殖作用。此外,dorsomorphin(Compound C)还被用作BMP通路的选择性抑制剂。 Compound C除了能够抑制AMPK之外,还能够抑制其他多种激酶。 [1]

体外实验表明,复合物C抑制AMPK活性和人脑胶质瘤细胞的增殖。Dorsomorphin(复合物C)还减少了顺铂诱导的细胞凋亡,并降低了顺铂治疗中c-caspase3和c-PARP的表达。

动物实验表明,化合物C可以减轻小鼠因顺铂引起的肾毒性,并且缓解了顺铂在肾脏组织中引起的c-caspase 3和c-PARP。[1][2]

实验参考方法

Cell experiment [1]:

Cell lines

BUMPT-306

Preparation Method

Cells were cultured in DMEM/F12 medium containing 10% fetal bovine serum and 10% streptomycin. Then, 20 μM cisplatin was used to induce obvious apoptosis as previously indicated

Reaction Conditions

Cells were cultured in 20 μM of cisplatin in the presence or absence of 20 mM compound C for 24 h. To evaluate the renal tubular cells apoptosis, morphologic assay and immunoblot were used to analyze the cleaved caspase3 and PARP.

Applications

Dorsomorphin (Compound C) could reduce the apoptosis of cells induced by cisplatin. Moreover, compound C also decreases the expression of c-caspase3 and c-PARP in cisplatin treatment, and the protective effect of compound C was dose-dependent.

Animal experiment [1]:

Animal models

Male C57BL/6 mice (8–10 weeks)

Preparation Method

Mice were injected intraperitoneally with cisplatin (30 mg/kg) oncely. The control group of mice were injected with the same dose of saline. Dorsomorphin (Compound C) was dissolved in DMSO and injected intraperitoneally at 10 mg/kg 1 h before the injection of cisplatin. The no-compound C animals were administered with a comparable volume of DMSO. All the mice were euthanized at 72 h.

Dosage form

10 mg/kg

Applications

Dorsomorphin (Compound C) could reduce the severe renal tubular damage caused by cisplatin in mice. Compound C also reduces the apoptosis of renal tubular cells in mice.

References:

[1]. Li F, et al. Compound C Protects Against Cisplatin-Induced Nephrotoxicity Through Pleiotropic Effects. Front Physiol. 2020 Dec 23;11:614244.

化学性质

Cas No. 866405-64-3 SDF
别名 6-[4-[2-(1-哌啶基)乙氧基]苯基]-3-(4-吡啶基)吡唑并[1,5-A]嘧啶,Compound C
化学名 6-[4-(2-piperidin-1-ylethoxy)phenyl]-3-pyridin-4-ylpyrazolo[1,5-a]pyrimidine
Canonical SMILES C1CCN(CC1)CCOC2=CC=C(C=C2)C3=CN4C(=C(C=N4)C5=CC=NC=C5)N=C3
分子式 C24H25N5O 分子量 399.49
溶解度 ≥ 8.49 mg/mL in DMSO with ultrasonic and warming 储存条件 4°C, protect from light
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1 mM 2.5032 mL 12.516 mL 25.0319 mL
5 mM 0.5006 mL 2.5032 mL 5.0064 mL
10 mM 0.2503 mL 1.2516 mL 2.5032 mL
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