Art. -Nr.: HY-B1153

Glafenine

(Synonyms: Glafenin)

5 Cited Publications

Kundenbewertung

Based on 5 publication(s) in Google Scholar

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

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Reinheit: 98.77%
CAS. Nr.: 3820-67-5
Formel: C₁₉H₁₇ClN₂O₄
Molecular Weight:372.80

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Glafenine Chemical Structure

CAS. Nr.: 3820-67-5

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (5)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

COX-1

COX-2

Alle COX Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
Sf21	IC₅₀	22.3 μM Compound: Glafenine	Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake	[PMID: 21965623]
Sf21	IC₅₀	32.2 μM Compound: Glafenine	Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake	[PMID: 21965623]

In Vitro

Glafenine (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 (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.

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 (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.

Chemical Information

CAS. Nr. 3820-67-5
Appearance Solid
Molecular Weight 372.80
Formel C₁₉H₁₇ClN₂O₄
Color Light yellow to yellow
SMILES

O=C(OCC(O)CO)C1=CC=CC=C1NC2=CC=NC3=CC(Cl)=CC=C23
Synonyms

Glafenin
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (5)

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Journal Impact Factor

Acta Pharm Sin B

DeepICER: A deep learning framework for predicting compound-induced gene expression profiles. [Abstract]

2026 May;16(5):2947-2963. PMID: 42180546
Acta Pharm Sin B

2026 Feb.
Int J Biol Macromol

Reticuline isomerase AKR1B1 with aldo-keto reductase activity and detoxification function from the insect Blaps rhynchopetera. [Abstract]

2026 Mar:352:151224. PMID: 41791543
Bioorg Chem

Identification of FTY720 and COH29 as novel topoisomerase I catalytic inhibitors by experimental and computational studies. [Abstract]

2024 Jun:147:107412. PMID: 38696845
Indian J Ophthalmol

Ranitidine protects Müller cells against ferroptosis in diabetic retinopathy by regulating the AKT1/GSK3β pathway. [Abstract]

2026 Feb 1;74(2):250-258. PMID: 41581041

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (268.24 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.6824 mL

13.4120 mL

26.8240 mL

5 mM

0.5365 mL

2.6824 mL

5.3648 mL

10 mM

0.2682 mL

1.3412 mL

2.6824 mL

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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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 (5.58 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.

Protocol 2

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

Solubility: 2.08 mg/mL (5.58 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (5.58 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (285 KB)
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Schöber W, et al. Impact of glafenine hydrochloride on human endothelial cells and human vascular smooth muscle cells: a substance reducing proliferation, migration and extracellular matrix synthesis. Cell Biol Int. 2003;27(12):987-96 [Content Brief]

[2]. Carlile GW, et al. The NSAID glafenine rescues class 2 CFTR mutants via cyclooxygenase 2 inhibition of the arachidonic acid pathway. Sci Rep. 2022 Mar 17;12(1):4595 [Content Brief]

[3]. Goldsmith JR, et al. Glafenine-induced intestinal injury in zebrafish is ameliorated by μ-opioid signaling via enhancement of Atf6-dependent cellular stress responses. Dis Model Mech. 2013 Jan;6(1):146-59. [Content Brief]

[4]. Chiu AM, et al. High Throughput Assay Identifies Glafenine as a Corrector for the Folding Defect in Corneal Dystrophy-Causing Mutants of SLC4A11. Invest Ophthalmol Vis Sci. 2015 Dec;56(13):7739-53. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. 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	2.6824 mL	13.4120 mL	26.8240 mL	67.0601 mL
	5 mM	0.5365 mL	2.6824 mL	5.3648 mL	13.4120 mL
	10 mM	0.2682 mL	1.3412 mL	2.6824 mL	6.7060 mL
	15 mM	0.1788 mL	0.8941 mL	1.7883 mL	4.4707 mL
	20 mM	0.1341 mL	0.6706 mL	1.3412 mL	3.3530 mL
	25 mM	0.1073 mL	0.5365 mL	1.0730 mL	2.6824 mL
	30 mM	0.0894 mL	0.4471 mL	0.8941 mL	2.2353 mL
	40 mM	0.0671 mL	0.3353 mL	0.6706 mL	1.6765 mL
	50 mM	0.0536 mL	0.2682 mL	0.5365 mL	1.3412 mL
	60 mM	0.0447 mL	0.2235 mL	0.4471 mL	1.1177 mL
	80 mM	0.0335 mL	0.1677 mL	0.3353 mL	0.8383 mL
	100 mM	0.0268 mL	0.1341 mL	0.2682 mL	0.6706 mL

Keywords

Glafenine

5 Cited Publications

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Glafenine

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Publications Citing Use of MedChemExpress (MCE) Glafenine

Alle COX Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (5)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Glafenine Related Classifications

HY-B1153 Related Classifications