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Cat. No.: HY-130245A

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(R,R)-PCSK9 degrader 1

(R,R)-PCSK9 degrader 1 is an isomer of PCSK9 degrader 1 (HY-130245). (R,R)-PCSK9 degrader 1 is a HyT-like PCSK9 degrader (IC₅₀ of 655.4 nM) , and its PCSK9-binding site does not interfere with the binding of PCSK9 to LDL receptor. (R,R)-PCSK9 degrader 1 can be used in the research of atherosclerosis, hypercholesterolemia, coronary heart disease, metabolic syndrome, acute coronary syndrome, and related cardiovascular and cardiometabolic diseases.

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

CAS No.: 2216703-12-5
Formula: C₅₃H₆₉FN₈O₁₃S
Molecular Weight:1077.22

Storage:

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

Data Sheet (281 KB)

(R,R)-PCSK9 degrader 1 Chemical Structure

CAS No.: 2216703-12-5

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Use of MCE Products

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

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

Description

In Vitro

PCSK9 degrader 1 (Example 106) (24 h) induces concentration-dependent degradation of both precursor and mature PCSK9 in PCSK9-overexpressing HEK293 cells, with DC₅₀ values of 4.82 μM and 3.42 μM, respectively^[1].

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

Chemical Information

CAS No. 2216703-12-5
Molecular Weight 1077.22
Formula C₅₃H₆₉FN₈O₁₃S
SMILES

OC(C(C=C1)=CC=C1C(C(F)=C2)=CC=C2OC(C(OCCOCCNC([C@H](NC(OC(C)(C)C)=O)CCCN/C(NC(OC(C)(C)C)=O)=N/C(OC(C)(C)C)=O)=O)=C3)=CC4=C3CCN[C@]4(C)CC(NC5=NC=CS5)=O)=O
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 (281 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 (2659 KB)

References

[1]. Jason Eugene IMBRIGLO, et al. Substituted 1-methyl-1,2,3,4-tetrahydroisoquinoline molecules as pcsk9 allosteric binders. WO2018057409A1.

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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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