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Ezetimibe

Cat. No. M3499
Ezetimibe Structure
Synonym:

SCH 58235

Size Price Availability Quantity
10mg USD 38  USD38 In stock
50mg USD 60  USD60 In stock
100mg USD 80  USD80 In stock
200mg USD 120  USD120 In stock
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Quality Control & Documentation
Biological Activity

Ezetimibe (Zetia) is a beta-lactam analog that targets NPC1L1, thereby lowering blood cholesterol levels. In addition, Ezetimibe can prevent spinal cord injury by inhibiting apoptosis through activation of autophagy and modulation of the PI3K/AKT/mTOR signaling pathway, which can be used in studies related to spinal cord injury.

Chemical Information
Molecular Weight 409.4
Formula C24H21F2NO3
CAS Number 163222-33-1
Solubility (25°C) DMSO 72 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
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] Yvette N Lamb. Rosuvastatin/Ezetimibe: A Review in Hypercholesterolemia

[2] Larysa Strilchuk, et al. An overview of rosuvastatin/ezetimibe association for the treatment of hypercholesterolemia and mixed dyslipidemia

[3] Yasuyoshi Ouchi, et al. Ezetimibe Lipid-Lowering Trial on Prevention of Atherosclerotic Cardiovascular Disease in 75 or Older (EWTOPIA 75): A Randomized, Controlled Trial

[4] Christie M Ballantyne, et al. Bempedoic acid plus ezetimibe fixed-dose combination in patients with hypercholesterolemia and high CVD risk treated with maximally tolerated statin therapy

[5] Soo Hyun Kim, et al. Ezetimibe ameliorates steatohepatitis via AMP activated protein kinase-TFEB-mediated activation of autophagy and NLRP3 inflammasome inhibition

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