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Inclisiran

Cat. No. M11345
Inclisiran Structure
Synonym:

ALN-PCSsc

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Biological Activity

Inclisiran (ALN-PCSsc) is a first-in-class double-stranded small interfering RNA (siRNA) molecule and a PCSK9 inhibitor that inhibits the transcription of PCSK-9. Inclisiran is used in hyperlipidemia and cardiovascular disease (CVD) research.

Chemical Information
Molecular Weight 16339.00
CAS Number 1639324-58-5
Form Solid
Solubility (25°C) Water 5 mg/mL
Storage -20°C
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] Bruce A Warden, et al. J Cardiovasc Pharmacol. Inclisiran: A Novel Agent for Lowering Apolipoprotein B-containing Lipoproteins

[2] Yvette N Lamb. Drugs. Inclisiran: First Approval

[3] Frederick J Raal, et al. N Engl J Med. Inclisiran for the Treatment of Heterozygous Familial Hypercholesterolemia

[4] Kausik K Ray, et al. N Engl J Med. Two Phase 3 Trials of Inclisiran in Patients with Elevated LDL Cholesterol

[5] Toshiyuki Nishikido, et al. Expert Opin Investig Drugs. Inclisiran for the treatment of dyslipidemia

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