Chloramphenicol [56-75-7]

Referencia HY-B0239-1g

embalaje : 1g

Marca : MedChemExpress

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Descripciòn

Chloramphenicol is an orally active, potent and broad-spectrum antibiotic. Chloramphenicol shows antibacterial activity. Chloramphenicol represses the oxygen-labile transcription factor and hypoxia inducible factor-1 alpha (HIF-1α) in hypoxic A549 and H1299 cells. Chloramphenicol suppresses the mRNA levels of vascular endothelial growth factor (VEGF) and glucose transporter 1, eventually decreasing VEGF release. Chloramphenicol can be used for anaerobic infections and lung cancer research[1][2][3].

IC50 & Target

JNK

 

MMP13

 

In Vitro

Chloramphenicol (1-100 μg/mL, 18-24 h) inhibits the HIF-1α pathway in NSCLC cells in a concentration-dependent manner[1].
Chloramphenicol (100 μg/mL, 0-24 h) induces autophagy in NSCLC cells, substantially increases the levels of autophagic biomarkers (beclin-1, Atg12-Atg5 conjugates, and LC3-II)[1].
Chloramphenicol induces abnormal differentiation and inhibits apoptosis in activated T cells[2].
Chloramphenicol can inhibit both bacterial and mitochondrial protein synthesis, causing mitochondrial stress and decreased ATP biosynthesis[3].
chloramphenicol (1-100 μg/mL) can induce matrix metalloproteinase (MMP)-13 expression and increase MMP-13 protein[3].
chloramphenicol (1-100 μg/mL) can activate c-Jun N-terminal kinases (JNK) and phosphatidylinositol 3-kinase (PI-3K)/Akt signaling, leading to c-Jun protein phosphorylation[3].
Chloramphenicol acts primarily on the 50S subunit of bacterial 70S rihosomes and inhibits peptide bond formation by suppressing peptidyl transferase activity[5].

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

Cell Viability Assay[1]

Cell Line: A549 and H1299 cells
Concentration: 0, 1, 10, 100 μg/mL
Incubation Time: 3 h and 24 h
Result: In the 3-h-treated group, the viability of A549 and H1299 cells at 100 μg/mL concentration was 97.0 ± 3.9% and 98.1 ± 5.0%, respectively. The viability of A549 cells was 102.9 ± 1.3% and 99.2 ± 0.9%, whereas the viability of H1299 cells was 103.3 ± 1.9% and 93.8 ± 4.5%, under hypoxia and treatment with CoCl2, respectively.

Western Blot Analysis[1]

Cell Line: A549 and H1299 cells
Concentration: 0, 1, 10, 50, 100 μg/mL
Incubation Time: 18-24 h
Result: Inhibited HIF-1α protein accumulation in NSCLC cells in a concentration-dependent manner, while the expression levels of ARNT remained unaltered. Had no effect on CoCl2 (250 μM, 3 h treatment)-mediated HIF-1α protein accumulation and SENP-1 protein reduction.

Western Blot Analysis[1]

Cell Line: A549 and H1299 cells
Concentration: 100 μg/mL
Incubation Time: 0, 6, 12, 24 h
Result: Induced autophagy in NSCLC cells in a time-dependent manner. Upregulats the expression of beclin-1 and increased the levels of Atg12-Atg5 conjugates in both NSCLC cell lines, both in a time dependent and concentration-dependent manner. Augmented LC3-II and downregulated p62/STSQM1 in A549 cells. Induced an augmentation of p62/STSQM1, and a decrease in LC3-II levels in H1299 cells.
In Vivo

Chloramphenicol (0-3500 mg/kg, Gavage, daily, for 5 days) decreases erythrocytes and erythrocyte precursors and reduces marrow erythroid cells were at day 1 post-dosing, and returns to normal by 14 days post-dosing[4].

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

Animal Model: Female B6C3F1 mice (12-14 weeks old)[4]
Dosage: 0, 2500 and 3500 mg/kg
Administration: Gavage, daily, for 5 days
Result: Cessation of erythropoiesis was evident at day 1 post-dosing. A recovery was seen at day 7 post-dosing at the 2500 mg/kg dose level and at between 7 and 14 days at the 3500 mg/kg dose level. Myelotoxicity was most pronounced in the erythroid series at each dose level. Depressed femoral marrow BFU-E and CFU-E at day 1 post-dosing. All the blood and marrow parameters in the present study returned to normal by 14 days post-dosing.
Peso molecular

323.13

Fòrmula

C11H12Cl2N2O5

No. CAS
Appearance

Solid

Color

White to off-white

SMILES

O=C(N[C@H](CO)[C@H](O)C1=CC=C([N+]([O-])=O)C=C1)C(Cl)Cl

Structure Classification
Initial Source
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento
Powder -20°C 3 years
4°C 2 years

*The compound is unstable in solutions, freshly prepared is recommended.

Solvente y solubilidad
In Vitro: 

DMSO : ≥ 150 mg/mL (464.21 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : 100 mg/mL (309.47 mM; Need ultrasonic)

H2O : 3.06 mg/mL (9.47 mM; Need ultrasonic)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0947 mL 15.4736 mL 30.9471 mL
5 mM 0.6189 mL 3.0947 mL 6.1894 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (7.74 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (7.74 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 2.5 mg/mL (7.74 mM); Clear solution; Need ultrasonic

Pureza y Documentación
Referencias

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