Art. -Nr.: HY-14952

Giripladib

Name: Giripladib
Brand: MedChemExpress
SKU: HY-14952
Price: 235.00 USD
Availability: InStock
Rating: 5 (1 reviews)

(Synonyms: PLA-695)

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

Giripladib (PLA-695) is a selective cPLA_2α inhibitor. Giripladib attenuates CKD serum-induced PUFA accumulation, MDA and ROS levels, restores the GSH/GSSG ratio, and alleviates mitochondria-Ferroptosis-related morphological changes. Giripladib exhibits anti-inflammatory and disease-modifying effects in collagen-induced arthritis. Giripladib can be used in research on chronic kidney disease-associated plaque vulnerability, rheumatoid arthritis, and breast cancer.

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Reinheit : 99.68%
CAS. Nr.: 865200-20-0
Formel: C₄₁H₃₆ClF₃N₂O₄S
Molecular Weight:745.25

Speicherung:

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

Giripladib Chemical Structure

CAS. Nr.: 865200-20-0

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[3]

cPLA2α

Alle Phospholipase Isoform-spezifische Produkte anzeigen :

Alle Glutathione Peroxidase Isoform-spezifische Produkte anzeigen :

GPX1
GPX4

In Vitro

Lipid MetabolismOxidative StressFerroptosisInnate ImmunityLipid Inflammatory MediatorsAnti-cancer

Lipid Metabolism

Giripladib (10 μM) attenuates CKD serum-induced PUFA accumulation in hVSMCs^[1].

Lipid Metabolism

Oxidative Stress

Ferroptosis

Giripladib (10 μM) attenuates CKD serum-induced ferroptosis in hVSMCs by reducing oxidative stress markers and restoring the GSH/GSSG ratio^[1].

Innate Immunity

Lipid Inflammatory Mediators

Giripladib (1 μM) inhibits cPLA₂α in RAW264.7 cells, reduces AA release and PG biosynthesis, and simultaneously increases PG-G levels^[2].

Lipid Inflammatory Mediators

Lipid Metabolism

Giripladib (300 nM) reduces arachidonic acid levels in MCF-7 BCSCs by inhibiting PLA2G16 enzyme activity^[4].

Anti-cancer

Giripladib acts synergistically with Tamoxifen (HY-13757A) and Doxorubicin (HY-15142) to effectively eliminate MCF7 and Hs578T BCSC^[4].

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

Cell Viability Assay^[4]

Cell Line:

BCSCs and non-BCSCs derived from breast cancer cells
Concentration:

Various concentrations
Incubation Time:

48 h
Result:

Increased sensitivity of BCSCs to chemotherapeutic agents.
Combination with chemotherapeutic agents was more effective in reducing BCSCs numbers than single agent treatment alone.

In Vivo

Lipid MetabolismFerroptosisAnti-cancer

Lipid Metabolism

Ferroptosis

Giripladib (7.5 mg/kg; i.p.; daily; 12 weeks), a specific cPLA₂ inhibitor, attenuates VSMC ferroptosis and CKD-related atherosclerotic plaque vulnerability in CKD/ApoE^−/− mice by blocking PUFA accumulation^[1].

Anti-cancer

Giripladib (7.5 mg/kg; i.p.; once daily) in combination with Doxorubicin (HY-15142) effectively eliminates BCSCs and inhibits tumor growth in mice by reducing KLF4 expression^[4].

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

Animal Model:

ApoE−/− (C57BL/6J background) (male, 8 weeks old, 20-25 g)^[1]
Dosage:

7.5 mg/kg
Administration:

i.p.; daily; 12 weeks
Result:

Ameliorated PUFA accumulation, reduced arterial MDA production, and diminished 4-HNE expression in fibrous cap VSMCs.
Mitigated mitochondrial-ferroptosis-associated morphological alterations including mitochondrial shrinkage.
Significantly mitigated atherosclerotic plaque vulnerability and reduced lesion area.

Animal Model:

BALB/c nude (female, 5-week-old)^[4]
Dosage:

7.5 mg/kg (Giripladib); 4 mg/kg (Doxorubicin)
Administration:

i.p.; once daily (Giripladib); every 5 days (Doxorubicin)
Result:

Notably decreased tumorigenesis of BCSCs and suppressed tumor growth compared with monotherapy.
Significantly reduced stemness-related transcription factor KLF4 in tumors.

Related Protocols :

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991			2011-05	PHASE1

Chemical Information

CAS. Nr. 865200-20-0
Appearance Solid
Molecular Weight 745.25
Formel C₄₁H₃₆ClF₃N₂O₄S
Color White to light yellow
SMILES

O=C(C1=CC=C(CCCC2=C(CCNS(=O)(CC3=C(C(F)(F)F)C=CC=C3)=O)N(C(C4=CC=CC=C4)C5=CC=CC=C5)C6=C2C=C(C=C6)Cl)C=C1)O
Synonyms

PLA-695
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Publications (1)

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Journal Impact Factor

Research (Wash D C)

2026 Sep 2:9:1411. PMID: 42688573

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 125 mg/mL (167.73 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

1.3418 mL

6.7092 mL

13.4183 mL

5 mM

0.2684 mL

1.3418 mL

2.6837 mL

10 mM

0.1342 mL

0.6709 mL

1.3418 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)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (305 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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]. Bi X, et al. -Deficiency-Mediated Polyunsaturated Fatty Acid Accumulation Promotes Vascular Smooth Muscle Cell Ferroptosis and Chronic-Kidney-Disease-Associated Plaque Vulnerability. Research (Washington, D.C.). 2026;9:1411.

[2]. Mitchener MM, et al. Competition and allostery govern substrate selectivity of cyclooxygenase-2. Proceedings of the National Academy of Sciences of the United States of America. 2015 Oct 06;112(40):12366-71.

[3]. Kokotos G, et al. Inhibition of group IVA cytosolic phospholipase A2 by thiazolyl ketones in vitro, ex vivo, and in vivo. Journal of medicinal chemistry. 2014 Sep 25;57(18):7523-35. [Content Brief]

[4]. Liu S, et al. A novel lncRNA ROPM-mediated lipid metabolism governs breast cancer stem cell properties. Journal of hematology & oncology. 2021 Oct 29;14(1):178. [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	1.3418 mL	6.7092 mL	13.4183 mL	33.5458 mL
	5 mM	0.2684 mL	1.3418 mL	2.6837 mL	6.7092 mL
	10 mM	0.1342 mL	0.6709 mL	1.3418 mL	3.3546 mL
	15 mM	0.0895 mL	0.4473 mL	0.8946 mL	2.2364 mL
	20 mM	0.0671 mL	0.3355 mL	0.6709 mL	1.6773 mL
	25 mM	0.0537 mL	0.2684 mL	0.5367 mL	1.3418 mL
	30 mM	0.0447 mL	0.2236 mL	0.4473 mL	1.1182 mL
	40 mM	0.0335 mL	0.1677 mL	0.3355 mL	0.8386 mL
	50 mM	0.0268 mL	0.1342 mL	0.2684 mL	0.6709 mL
	60 mM	0.0224 mL	0.1118 mL	0.2236 mL	0.5591 mL
	80 mM	0.0168 mL	0.0839 mL	0.1677 mL	0.4193 mL
	100 mM	0.0134 mL	0.0671 mL	0.1342 mL	0.3355 mL

Bioz

Giripladib

1 Cited Publications

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Giripladib

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