GW4869 (GW69A, GW554869A) is a noncompetitive inhibitor of neutral Smase (spspingolipase) with IC50 of 1 μM. GW4869 is selective for N-smase and has no inhibitory effect on acidic SMase at concentrations up to 150 μm. GW4869 is also an inhibitor of exosome synthesis/release. LPS-triggered exosome generation was remarkably attenuated in macrophages upon pre-treatment of macrophages with 10 μM GW4869, as evidenced by a 22% reduction in the activity of AChE. Such attenuation was further enhanced by treatment with 20 μM GW4869. GW4869 prevented CLP-induced diaphragm calpain activation and diaphragm weakness in mice.
Int J Biol Sci. 2023 Sep 4;19(15):4744-4762.
Hypoxia-induced exosomes facilitate lung pre-metastatic niche formation in hepatocellular carcinoma through the miR-4508-RFX1-IL17A-p38 MAPK-NF-κB pathway
GW4869 2HCl purchased from AbMole
Int Immunopharmacol. 2023 Nov 27;126:111301.
Inhibition of circulating exosomes release with GW4869 mitigates severe acute pancreatitis-stimulated intestinal barrier damage through suppressing NLRP3 inflammasome-mediated pyroptosis
GW4869 2HCl purchased from AbMole
Cell Death Dis. 2021 Aug 27;12(9):815.
Extracellular vesicles package dsDNA to aggravate Crohn’s disease by activating the STING pathway
GW4869 2HCl purchased from AbMole
| Molecular Weight | 577.50 |
| Formula | C30H30Cl2N6O2 |
| CAS Number | 6823-69-4 |
| Solubility (25°C) | DMSO 1 mg/mL (Need ultrasonic) |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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