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SBC-115076

Cat. No. M7542
SBC-115076 Structure
Size Price Availability Quantity
5mg USD 88  USD88 In stock
10mg USD 115  USD115 In stock
50mg USD 400  USD400 In stock
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Quality Control & Documentation
Biological Activity

Sbc-115076 is an effective inhibitor of the preprotein invertase Bacillus subtilis proteinase/Kexin 9 (PCSK9). PCSK9 is a preprotein invertase that plays an important role in LDL receptor metabolism.

Chemical Information
Molecular Weight 527.61
Formula C31H33N3O5
CAS Number 489415-96-5
Solubility (25°C) 32 mg/mL in DMSO
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] Ping Jin, et al. Role of PCSK9 in Homocysteine-Accelerated Lipid Accumulation in Macrophages and Atherosclerosis in ApoE -/- Mice

[2] Chanisa Thonusin, et al. A proprotein convertase subtilisin/kexin type 9 inhibitor provides comparable efficacy with lower detriment than statins on mitochondria of oxidative muscle of obese estrogen-deprived rats

[3] Chanisa Thonusin, et al. The comparative effects of high dose atorvastatin and proprotein convertase subtilisin/kexin type 9 inhibitor on the mitochondria of oxidative muscle fibers in obese-insulin resistant female rats

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