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Cat. No.: HY-158827

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AZD8233

AZD8233 is an orally active antisense oligonucleotide targeting PCSK9 mRNA. AZD8233 highly specifically reduces PCSK9 mRNA. AZD8233 lowers LDL cholesterol. AZD8233 can be used in research on dyslipidemia.

For research use only. We do not sell to patients.

CAS No.: 2604215-74-7
Molecular Weight:6920.84

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (283 KB)

AZD8233 Chemical Structure

CAS No.: 2604215-74-7

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

In Vitro

AZD8233 is highly specific to reducing PCSK9 mRNA in human cells, showing ≥10-fold IC₅₀ selectivity over all other transcripts^[1].
AZD8233 (5-134 nM; 8 h; 12 h post-transfection) silenced PCSK9 comparably to P-12c in human HepG2 cells at 5 nM, while P-12c exhibited markedly superior efficiency at higher doses^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Real Time qPCR^[4]

Cell Line:

human HepG2 cells
Concentration:

5, 15, 44, and 134 nM
Incubation Time:

8 h (incubation); 12 h post-transfection (RNA analysis)
Result:

No numerical PCSK9 silencing value for AZD8233 alone was reported.
P-12c displayed comparable PCSK9 silencing efficacy to AZD8233 at 5 nM, while P-12c exhibited markedly superior efficiency at 15, 44, and 134 nM.

In Vivo

AZD8233 (0.25-5 mg/kg; s.c.; days 1, 5, 8, 15, and 23) produces dose-dependent reductions in human plasma PCSK9 and LDL cholesterol in human PCSK9 transgenic mice, with 80% PCSK9 reduction at 0.5 mg/kg^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

heterozygous human PCSK9 transgenic (huPCSK9 Tg) (male, 5 months old)^[1]
Dosage:

0.25, 0.5, 1, 2.5, and 5 mg/kg
Administration:

s.c.; days 1, 5, 8, 15, and 23
Result:

Liver exposure increased dose-dependently.
Liver exposure of 4 µg/g (3 and 5 µg/g; 5th and 95th percentiles) was predicted to result in 80% reduction in plasma PCSK9.
A dose of AZD8233 0.5 mg/kg was required to reduce PCSK9 by 80%.
The liver exposure-PCSK9 model estimated IC₅₀ = 2.0 µg/g (1.4 and 2.9 µg/g; 5th and 95th percentiles) and Hill coefficient h = 2.2 (1.6 and 3.8).
Concomitant dose-dependent reductions of human plasma PCSK9 and LDL cholesterol were observed.

Related Protocols :

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 2604215-74-7
Molecular Weight 6920.84
SMILES

[AZD8233]
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (283 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2242 KB)

References

[1]. Gennemark P, et al. An oral antisense oligonucleotide for PCSK9 inhibition. Science translational medicine. 2021 May 12;13(593):eabe9117.

[2]. Totary-Jain H, et al. Novel anti-atherosclerotic mRNA-based therapy. Atherosclerosis. 2022 Aug 1;355:27.

[3]. Wada F, et al. Drug discovery and development scheme for liver-targeting bridged nucleic acid antisense oligonucleotides. Molecular therapy. Nucleic acids. 2021 Dec 03;26:957-969.

[4]. Chen S, et al. ClinASO: An open-source platform for rapid drug discovery of gapmer antisense oligonucleotides. Molecular therapy. Nucleic acids. 2026 Jun 16;37(2):102933.

[5]. Kingwell K. Pushing the envelope with PCSK9. Nat. Rev. Drug Discov. 2021 Jul 1;20:506.

[6]. Burnett JR, et al. MK-0616: an oral PCSK9 inhibitor for hypercholesterolemia treatment. Expert Opin Investig Drugs. 2023 Jul-Dec;32(10):873-878.

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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