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Chemical Structure| 489415-96-5 Chemical Structure| 489415-96-5

Structure of SBC-115076
CAS No.: 489415-96-5

Chemical Structure| 489415-96-5

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SBC-115076 is an anti-proprotein convertase subtilisin kexin type 9 (anti-PCSK9) compounds, for the treatment and/or prevention of cardiovascular diseases.

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Product Details of SBC-115076

CAS No. :489415-96-5
Formula : C31H33N3O5
M.W : 527.61
SMILES Code : O=C1N(CCCN2CCOCC2)C(C3=CC=NC=C3)C(C(C4=CC=C(OCC5=CC=CC=C5)C(C)=C4)=O)=C1O
MDL No. :MFCD03296540

Safety of SBC-115076

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

Description
SBC-115076 is a powerful inhibitor of proprotein convertase subtilisin/kexin type 9 (PCSK9). PCSK9, a proprotein convertase, is pivotal in the metabolism of LDL receptors[1][2].

In Vitro:

Cell Line
Concentration Treated Time Description References
PK-15 cells 0–300 nM 6–48 hours To evaluate the effect of SBC-115076 on PRV proliferation in PK-15 cells. The results showed that SBC-115076 significantly increased PRV gE expression in a dose-dependent manner. PMC10804996
THP-1 macrophages 5, 10, 20 µmol/L 24 hours SBC-115076 dose-dependently suppressed the protein expression of PCSK9 in THP-1 macrophages, but had little effect on LDLR protein level. PMC8517151
THP-1 macrophages 20 µmol/L 24 hours On co-incubation with Hcy and SBC-115076, SBC-115076 decreased the protein level of PCSK9 about 38% as compared with Hcy treatment. PMC8517151

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c mice 4T1 tumor model Intravenous injection 8 mg/kg Daily for 5 days PRS significantly inhibited tumor growth and regulated LDLR protein expression levels in the liver of 4T1 tumor-bearing mice. PMC10610039
Mice PRV infection model Intraperitoneal injection 50 mg/kg T0901317, 30 mg/kg LG268 daily for 10 days To evaluate the effect of SBC-115076 on PRV infection in mice. The results showed that SBC-115076 treatment significantly increased PRV proliferation in the lungs, leading to more severe lung damage and higher mortality. PMC10804996
ApoE -/- mice High-fat diet-induced atherosclerosis model Subcutaneous injection 8 mg/kg Twice daily for 2 days To investigate the mechanism by which PCSK9i promotes the stabilization of atherosclerotic plaques by targeting the miR-186-5p/Wipf2 and miR-375-3p/Pdk1/Yap1 axes. The results showed that PCSK9i significantly reduced blood lipid levels, decreased plaque area, and promoted plaque stabilization by regulating the expression of related miRNAs. PMC11002805
ApoE−/−mice Hyperhomocysteinemia model Subcutaneous injection 5, 10, 15 mg/kg Every 4 days for a total of four injections SBC-115076 significantly reduced the lesion area and lipid accumulation, and increased the expressions of ABCA1 and ABCG1 in macrophages from atherosclerotic plaque. PMC8517151
Rats Type 2 diabetes model Subcutaneous injection 8 mg/kg Twice weekly for 8 weeks To evaluate the effect of PCSK9 inhibitors on cognitive dysfunction in T2DM rats, the results showed that PCSK9 inhibitors improved cognitive dysfunction. PMC11330219

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.90mL

0.38mL

0.19mL

9.48mL

1.90mL

0.95mL

18.95mL

3.79mL

1.90mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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