Inclisiran
Based on 8 publication(s) in Google Scholar
Inclisiran is a double-stranded small interfering RNA (siRNA) molecule. Inclisiran inhibits the transcription of PCSK9. Inclisiran inhibits Pyroptosis, activates PPARγ, and reduces NLRP3, cleaved caspase-1, IL-1β, and IL-18. Inclisiran has anti-inflammatory, lipid-regulating and anti-atherosclerotic activities. Inclisiran can be used in researches of hyperlipidemia and cardiovascular disease (CVD).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.96%
- No. CAS: 1639324-58-5
- Peso molecular:16339.00
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Almacenamiento:
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Inclisiran
More- Nat Cardiovasc Res. 2026 Jun 22. [Abstract]
- Free Radic Biol Med. 2026 Mar 16:246:547-561. [Abstract]
- J Med Chem. 2025 Apr 24;68(8):8190-8207. [Abstract]
- Biochem Pharmacol. 2025 Jul 27;242(Pt 2):117192. [Abstract]
- Drug Metab Dispos. 2025 Jun;53(6):100089. [Abstract]
- Biol Methods Protoc. 2024 May 6;9(1):bpae029. [Abstract]
- medRxiv. 2025 Feb 12.
- Ann Transl Med. 2022 Nov;10(22):1205. [Abstract]
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Cell Proliferation/Viability Assay
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Actividad biológica
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PPARγ |
IL-1β |
Caspase-1 |
NLRP3 |
Inclisiran (50-200 nM; 48 h) significantly inhibits cell death, cytotoxicity, and downregulates mRNA and protein expressions of pyroptosis-related factors in ox-LDL-induced HUVECs[2].
Inclisiran (50-200 nM; 48 h) inhibits ox-LDL-induced foam cell formation in Raw264.7 macrophages by activating the PPARγ pathway[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human umbilical vein endothelial cells (HUVECs) treated with 25 μg/mL ox-LDL
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Concentration:50 nM, 100 nM, 200 nM
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Incubation Time:48 h
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Result:Decreased the protein expression of NLRP3, ASC, cleaved caspase-1, GSDMD-N, IL-1β, and IL-18.
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Cell Line:Raw264.7 macrophages treated with ox-LDL
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Concentration:50 nM, 100 nM, 200 nM
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Incubation Time:48 h
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Result:Increased PPARγ, SR-B1, ApoE, ABCA1.
Decreased SR-A, LOX-1, CD36.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male ApoE-/- mice (8 weeks old, 17-20 g); high-fat diet (HFD)-induced atherosclerosis model[2]
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Dosage:1, 5, 10 mg/kg (dissolved in PBS)
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Administration:Intraperitoneal injection; 20 weeks
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Result:Significantly reduced LDL-C, TC, TG, and increased HDL-C in plasma.
Decreased aortic plaque area and lipid deposition.
Decreased pyroptosis-related factors (NLRP3, ASC, GSDMD, IL-1β, IL-18).
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1639324-58-5
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Appearance Solid
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Peso molecular 16339.00
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Color White to off-white
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SMILES
[Inclisiran]
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Synonyms
ALN-PCSsc
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Sequence
RNA, (Am-sp-(2'-deoxy-2'-fluoro)C-sp-Am-(2'-deoxy-2'-fluoro)A-(2'-deoxy-2'- fluoro)A-(2'-deoxy-2'-fluoro)A-Gm-(2'-deoxy-2'-fluoro)C-Am-(2'-deoxy-2'-fluoro)AAm-(2'-deoxy-2'-fluoro)A-Cm-(2'-deoxy-2'-fluoro)A-Gm-(2'-deoxy-2'-fluoro)G-Um-(2'-deoxy-2'-fluoro)C-Um-Am-Gm-sp-Am-sp-Am), complex with RNA (Cm-sp-Umsp -Am-Gm-Am-Cm-(2'-deoxy-2'-fluoro)C-Um-(2'-deoxy-2'-fluoro)G-Um-dT-UmUm-Gm-Cm-Um-Um-Um-Um-Gm-Um) 3'-[[(2S,4R)-1-[29-[[2-(acetylamino)-2- deoxy-β-D-galactopyranosyl]oxy]-14,14-bis[[3-[[3-[[5-[[2-(acetylamino)-2-deoxy-βD-galactopyranosyl]oxy]-1-oxopentyl]amino]propyl]amino]-3-oxopropoxy]methyl]- 1,12,19,25-tetraoxo-16-oxa-13,20,24-triazanonacos-1-yl]-4-hydroxy-2- pyrrolidinyl]methyl hydrogen phosphate] (1:1)
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications (8)
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Journal Impact Factor
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Most Recent
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Nat Cardiovasc Res
Proteomics reveals spatial and molecular heterogeneities in advanced atherosclerotic carotid artery plaques. [Abstract]2026 Jun 22. PMID: 42332205 -
Free Radic Biol Med
Inclisiran attenuates Alzheimer's disease-like changes by suppressing microvascular endothelial ferroptosis to preserve blood-brain barrier integrity. [Abstract]2026 Mar 16:246:547-561. PMID: 41605321
Inclisiran purchased from MedChemExpress. Usage Cited in: Free Radic Biol Med. 2026 Mar 16:246:547-561. [Abstract]
Inclisiran sodium (5 mg/kg). Western blot and quantitative analysis of Aβ expression in the cortex of ApoE-/− mice.
Inclisiran purchased from MedChemExpress. Usage Cited in: Free Radic Biol Med. 2026 Mar 16:246:547-561. [Abstract]
Inclisiran sodium (5 mg/kg). Colocalization of Aβ in microvascular endothelial cells of ApoE −/− mouse brain (scale bar: 75 μm; DAPI (blue fluorescence) indicates cell nuclei, Aβ (green) and CD31 (red)).
Inclisiran purchased from MedChemExpress. Usage Cited in: Free Radic Biol Med. 2026 Mar 16:246:547-561. [Abstract]
Inclisiran sodium (5 mg/kg). Western blot and quantitative analysis of ACSL4 and GPX4 expression in the cortex of ApoE-/− mice.
Inclisiran purchased from MedChemExpress. Usage Cited in: Free Radic Biol Med. 2026 Mar 16:246:547-561. [Abstract]
Western blot and quantitative analyses of PCSK9 expression after ox-LDL (50 μg/mL) and Inclisiran (100 nmol/L) treatment in HCMEC/D3 cells.
Inclisiran purchased from MedChemExpress. Usage Cited in: Free Radic Biol Med. 2026 Mar 16:246:547-561. [Abstract]
Cell viability of HCMEC/D3 cells after treatment with ox-LDL (50 μg/mL) and Inclisiran (100 nmol/L) measured by CCK-8 assay.
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J Med Chem
PCSK9 Targeted Autophagosome-Tethering Compounds: Design, Synthesis, and Antiatherosclerosis Evaluation. [Abstract]2025 Apr 24;68(8):8190-8207. PMID: 40226893 -
Biochem Pharmacol
Intracellular fatty acid levels differentially impact target silencing by FDA-approved siRNA drugs. [Abstract]2025 Jul 27;242(Pt 2):117192. PMID: 40730278 -
Drug Metab Dispos
Comparative metabolism of an N-acetylgalactosamine-conjugated small interfering RNA, inclisiran, among various in vitro systems and correlations with in vivo metabolism in rats. [Abstract]2025 Jun;53(6):100089. PMID: 40505270 -
Biol Methods Protoc
A highly sensitive stem-loop RT-qPCR method to study siRNA intracellular pharmacokinetics and pharmacodynamics. [Abstract]2024 May 6;9(1):bpae029. PMID: 38783988 -
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Ann Transl Med
PCSK9 inhibitor inclisiran for treating atherosclerosis via regulation of endothelial cell pyroptosis. [Abstract]2022 Nov;10(22):1205. PMID: 36544639
Solvente y solubilidad
H2O : 5 mg/mL (0.31 mM; Need ultrasonic)
Pureza y Documentación
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Ficha de datos (280 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Instrucciones de manejo (2242 KB)
Referencias
[1]. Constantine E Kosmas, et al. Inclisiran for the Treatment of Cardiovascular Disease: A Short Review on the Emerging Data and Therapeutic Potential. Ther Clin Risk Manag. 2020 Oct 28;16:1031-1037. [Content Brief]
[2]. Kong N, Xu Q, Cui W, Feng X, Gao H. PCSK9 inhibitor inclisiran for treating atherosclerosis via regulation of endothelial cell pyroptosis. Ann Transl Med. 2022;10(22):1205. [Content Brief]
[3]. Wang Z, et al. Inclisiran inhibits oxidized low-density lipoprotein-induced foam cell formation in Raw264.7 macrophages via activating the PPARγ pathway. Autoimmunity. 2022 Jun;55(4):223-232. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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