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Lalistat 1

Cat. No. M21211
Lalistat 1  Structure
Size Price Availability Quantity
5mg USD 485  USD485 In stock
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Quality Control & Documentation
Biological Activity

Lalistat 1 is a lysosomal acid lipase inhibitor with IC50 value of 68 nM. It can block LAL-mediated lipid hydrolysis of acetylated LDL and reduce efflux of cholesterol from lipid-loaded cells.

Chemical Information
Molecular Weight 298.36
Formula C12H18N4O3S
CAS Number 501104-16-1
Form Solid
Solubility (25°C) DMSO : 20 mg/mL
Storage -20°C, dry, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Mari Ohira, et al. Mol Genet Metab Rep. LC-MS/MS-based enzyme assay for lysosomal acid lipase using dried blood spots

[2] Ivan Bradić, et al. Mol Metab. Off-target effects of the lysosomal acid lipase inhibitors Lalistat-1 and Lalistat-2 on neutral lipid hydrolases

[3] Ron C Helderman, et al. Bone. Loss of function of lysosomal acid lipase (LAL) profoundly impacts osteoblastogenesis and increases fracture risk in humans

[4] Nikolay Mayanskiy, et al. JIMD Rep. A kinetic assay of total lipase activity for detecting lysosomal acid lipase deficiency (LAL-D) and the molecular characterization of 18 LAL-D patients from Russia

[5] John Hamilton, et al. Clin Chim Acta. A new method for the measurement of lysosomal acid lipase in dried blood spots using the inhibitor Lalistat 2

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