2. Immunology/Inflammation Anti-infection Apoptosis Membrane Transporter/Ion Channel
  3. CFTR Endoplasmic Reticulum Oxidoreductase 1 (ERO1) Apoptosis COX
  4. Glafenine hydrochloride

Glafenine hydrochloride  (Synonyms: Glafenin hydrochloride)

Cat. No.: HY-B1153A Purity: 99.03%
COA
SDS
Handling Instructions Technical Support

Glafenine (Glafenin) hydrochloride is a non-selective, non-steroidal anti-inflammatory drug-based COX-1/COX-2 inhibitor. Glafenine hydrochloride exerts anti-inflammatory, anti-proliferative and anti-cell migration effects by inhibiting the arachidonic acid metabolic pathway and reducing prostaglandin synthesis. Glafenine hydrochloride can induce cell cycle arrest in vascular smooth muscle cells and endothelial cells and reduce the synthesis of the extracellular matrix protein Tenascin. Glafenine hydrochloride can be used in the research of inflammatory-related diseases, vascular restenosis and cystic fibrosis (CF).

For research use only. We do not sell to patients.

Glafenine hydrochloride Chemical Structure

Glafenine hydrochloride Chemical Structure

CAS No. : 65513-72-6

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Based on 1 publication(s) in Google Scholar

Other Forms of Glafenine hydrochloride:

Glafenine hydrochloride Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Glafenine hydrochloride

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COX COX-1 COX-2 COX-3

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  • Purity & Documentation

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Description

Glafenine (Glafenin) hydrochloride is a non-selective, non-steroidal anti-inflammatory drug-based COX-1/COX-2 inhibitor. Glafenine hydrochloride exerts anti-inflammatory, anti-proliferative and anti-cell migration effects by inhibiting the arachidonic acid metabolic pathway and reducing prostaglandin synthesis. Glafenine hydrochloride can induce cell cycle arrest in vascular smooth muscle cells and endothelial cells and reduce the synthesis of the extracellular matrix protein Tenascin. Glafenine hydrochloride can be used in the research of inflammatory-related diseases, vascular restenosis and cystic fibrosis (CF)[1][2][3][4].

IC50 & Target

COX-1

 

COX-2

 

In Vitro

Glafenine hydrochloride (10-100 μM; 4-20 days) inhibits cell proliferation and colony formation in human aortic smooth muscle cells (haSMCs) and endothelial cells (ECs) in a dose-dependent manner, induces cell cycle arrest at the G2/M phase, and reduces the synthesis of the extracellular matrix protein tenascin[1].
Glafenine hydrochloride (10 μM; 24 h) promotes the maturation and translocation of the F508del-CFTR mutant protein to the cell surface and enhances its chloride channel function in human bronchial epithelial cells (HBE) by inhibiting the COX-2-mediated arachidonic acid pathway[2].

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

Glafenine hydrochloride Related Antibodies

Cell Viability Assay[1]

Cell Line: Human aortic smooth muscle cells (haSMCs), human endothelial cells (ECs)
Concentration: 10 μM, 50 μM, 100 μM
Incubation Time: 4 days (short-term), 20 days (long-term)
Result: In haSMCs, short-term treatment (4 days) with 50 μM and 100 μM significantly reduced cell proliferation by 30-50% compared to control, while long-term treatment (20 days) with all concentrations caused dose-dependent inhibition, with 100 μM nearly halting proliferation.
Clonogenic activity was reduced by 40-70% in both short- and long-term treatments.
Flow cytometry revealed a G2/M phase block (25-35% increase) and reduced G1 phase (15-20% decrease) in haSMCs at 50-100 μM.

Immunofluorescence[1]

Cell Line: Human aortic smooth muscle cells (haSMCs), human endothelial cells (ECs)
Concentration: 10 μM, 50 μM, 100 μM
Incubation Time: 4 days (short-term), 20 days (long-term)
Result: Resulted a 60% reduction in tenascin expression in haSMCs treated with 100 μM for 4 days.
Significantly decreased proliferation by 25-40% after 4 days at 50 μM and 100 μM, in ECs, without significant cytotoxicity observed at ≤50 μM.
In Vivo

Glafenine hydrochloride (25 μM; immersion; single; 12 h) induces intestinal epithelial cell apoptosis, endoplasmic reticulum (ER) and mitochondrial stress, and damages intestinal structure in zebrafish larvae, while the μ-opioid receptor agonist DALDA (HY-P3870) alleviates the intestinal damage induced by glafenine by enhancing the atf6-dependent unfolded protein response (UPR)[3].

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

Animal Model: Zebrafish (Danio rerio) larvae (AB strain, 5 days post-fertilization)[3]
Dosage: 25 μM
Administration: Immersion in culture medium for 12 h
Result: Caused dose-dependent intestinal injury, characterized by apoptotic cell accumulation in the lumen, detected by acridine orange (AO) staining and activated caspase-3 immunohistochemistry.
Resulted ER pitting and mitochondrial vacuolization in intestinal epithelial cells (IECs) in transmission electron microscopy (TEM) assay, indicating ER and mitochondrial stress.
Disrupted intestinal architecture with pyknotic nuclei and cellular hypertrophy in segments 1 and 2 in histological analysis.
Molecular Weight

409.26

Formula

C19H18Cl2N2O4
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

[H]Cl.O=C(OCC(O)CO)C1=CC=CC=C1NC2=CC=NC3=CC(Cl)=CC=C23
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility
In Vitro: 

DMSO : 41.67 mg/mL (101.82 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4434 mL 12.2172 mL 24.4343 mL
5 mM 0.4887 mL 2.4434 mL 4.8869 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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: ≥ 2.08 mg/mL (5.08 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (5.08 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.03%

SDS (393 KB)

COA (255 KB) LCMS (264 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4434 mL 12.2172 mL 24.4343 mL 61.0859 mL
5 mM 0.4887 mL 2.4434 mL 4.8869 mL 12.2172 mL
10 mM 0.2443 mL 1.2217 mL 2.4434 mL 6.1086 mL
15 mM 0.1629 mL 0.8145 mL 1.6290 mL 4.0724 mL
20 mM 0.1222 mL 0.6109 mL 1.2217 mL 3.0543 mL
25 mM 0.0977 mL 0.4887 mL 0.9774 mL 2.4434 mL
30 mM 0.0814 mL 0.4072 mL 0.8145 mL 2.0362 mL
40 mM 0.0611 mL 0.3054 mL 0.6109 mL 1.5271 mL
50 mM 0.0489 mL 0.2443 mL 0.4887 mL 1.2217 mL
60 mM 0.0407 mL 0.2036 mL 0.4072 mL 1.0181 mL
80 mM 0.0305 mL 0.1527 mL 0.3054 mL 0.7636 mL
100 mM 0.0244 mL 0.1222 mL 0.2443 mL 0.6109 mL
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Glafenine hydrochloride Related Classifications

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  • 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.

Keywords:

Glafenine65513-72-6GlafeninCFTREndoplasmic Reticulum Oxidoreductase 1 (ERO1)ApoptosisCOXCystic fibrosis transmembrane conductance regulatorEndoplasmic Reticulum Oxidoreductase 1CyclooxygenaseInhibitorinhibitorinhibit

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