2. Metabolic Enzyme/Protease
  3. PCSK9
  4. PCSK9-IN-11

PCSK9-IN-11 (compound 5r) is a potent and orally active PCSK9 inhibitor. PCSK9-IN-11 exhibits PCSK9 transcriptional inhibitory activity in HepG2 cells, with an IC50 of 5.7 μM. PCSK9-IN-11 increases LDL receptor (LDLR) protein level. PCSK9-IN-11 can be used for atherosclerosis research.

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

PCSK9-IN-11 Chemical Structure

PCSK9-IN-11 Chemical Structure

CAS No. : 2882035-56-3

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Based on 1 publication(s) in Google Scholar

PCSK9-IN-11 Related Antibodies

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Description

PCSK9-IN-11 (compound 5r) is a potent and orally active PCSK9 inhibitor. PCSK9-IN-11 exhibits PCSK9 transcriptional inhibitory activity in HepG2 cells, with an IC50 of 5.7 μM. PCSK9-IN-11 increases LDL receptor (LDLR) protein level. PCSK9-IN-11 can be used for atherosclerosis research[1].

IC50 & Target

IC50: 5.7 μM (PCSK9)[1]
In Vitro

PCSK9-IN-11 (compound 5r) (0-25 μM, 24 h) significantly decreases PCSK9 protein level and increases LDLR expression in a dose dependent manner[1].

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

PCSK9-IN-11 Related Antibodies

Western Blot Analysis[1]

Cell Line: HepG2 cells
Concentration: 0, 2.5, 5, 12.5, 25 μM
Incubation Time: 24 h
Result: Significantly decreased PCSK9 protein level in a dose dependent manner. Markedly increased LDLR expression in a dose dependent manner. Significantly and dose-dependently increased DiI-LDL uptake by around 1.7 folds.
In Vivo

PCSK9-IN-11 (compound 5r) (0-1000 mg/kg, IG, once) exhibits a good in vivo safety feature with the halflethal dose (LD50) value of over 1000 mg/kg[1].
PCSK9-IN-11 (30 mg/kg, IG, once a day for 8 weeks) significantly suppresses hepatic PCSK9 expression and slightly reduces serum PCSK9 level[1].

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

Animal Model: C57BL/6J mice[1]
Dosage: 0, 250, 500 or 1000 mg/kg
Administration: Intragastrically administrated, single dose
Result: Exhibited a good in vivo safety feature with the halflethal dose (LD50) value of over 1000 mg/kg. Did not affected the body weight, behavioral and survival characteristics of mice.
Animal Model: ApoE KO mice (under high-fat diet (HFD))[1]
Dosage: 30 mg/kg
Administration: Intragastric administration, once a day for 8 weeks
Result: Significantly suppressed hepatic PCSK9 expression and slightly reduced serum PCSK9 level.
Molecular Weight

381.79

Formula

C16H17ClFN5O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N1C)N(C)C2=C(N(CC3=CC=CC(Cl)=C3F)C(NCCO)=N2)C1=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (327.41 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6192 mL 13.0962 mL 26.1924 mL
5 mM 0.5238 mL 2.6192 mL 5.2385 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6192 mL 13.0962 mL 26.1924 mL 65.4810 mL
5 mM 0.5238 mL 2.6192 mL 5.2385 mL 13.0962 mL
10 mM 0.2619 mL 1.3096 mL 2.6192 mL 6.5481 mL
15 mM 0.1746 mL 0.8731 mL 1.7462 mL 4.3654 mL
20 mM 0.1310 mL 0.6548 mL 1.3096 mL 3.2741 mL
25 mM 0.1048 mL 0.5238 mL 1.0477 mL 2.6192 mL
30 mM 0.0873 mL 0.4365 mL 0.8731 mL 2.1827 mL
40 mM 0.0655 mL 0.3274 mL 0.6548 mL 1.6370 mL
50 mM 0.0524 mL 0.2619 mL 0.5238 mL 1.3096 mL
60 mM 0.0437 mL 0.2183 mL 0.4365 mL 1.0914 mL
80 mM 0.0327 mL 0.1637 mL 0.3274 mL 0.8185 mL
100 mM 0.0262 mL 0.1310 mL 0.2619 mL 0.6548 mL
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PCSK9-IN-11 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PCSK9-IN-112882035-56-3PCSK9Proprotein convertase subtilisin/kexin type 9CSK9Transcriptional inhibitionCholesterolAtherosclerosisHepG2 cellsInhibitorinhibitorinhibit

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