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PCSK9-IN-11 (compound 5r) is a potent PCSK9 inhibitor with oral activity, exhibiting inhibitory activity on PCSK9 transcription in HepG2 cells (IC50 = 5.7 μM) and capable of increasing LDL receptor (LDLR) protein levels. PCSK9-IN-11 is applicable for atherosclerosis research.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $47 | In Stock | |
10 mg | $80 | In Stock | |
25 mg | $163 | In Stock | |
50 mg | $263 | In Stock | |
100 mg | $411 | In Stock |
Description | PCSK9-IN-11 (compound 5r) is a potent PCSK9 inhibitor with oral activity, exhibiting inhibitory activity on PCSK9 transcription in HepG2 cells (IC50 = 5.7 μM) and capable of increasing LDL receptor (LDLR) protein levels. PCSK9-IN-11 is applicable for atherosclerosis research. |
In vitro | PCSK9-IN-11 (compound 5r) (0-25 μM, 24 h) significantly reduces PCSK9 protein levels and increases LDLR expression in a dose-dependent manner[1]. |
In vivo | PCSK9-IN-11 (compound 5r) (0-1000 mg/kg, gavage, once) demonstrates superior safety in vivo, with an LD50 value exceeding 1000 mg/kg. Administered at 30 mg/kg via gavage once daily for 8 weeks, PCSK9-IN-11 significantly inhibits liver PCSK9 expression and slightly reduces serum PCSK9 levels [1]. |
Molecular Weight | 381.79 |
Formula | C16H17ClFN5O3 |
Smiles | CN1C(=O)C2=C(N=C(NCCO)N2CC2=C(F)C(Cl)=CC=C2)N(C)C1=O |
Relative Density. | no data available |
Storage | Shipping with blue ice. | ||||||||||||||||||||
Solubility Information | DMSO: 3.82 mg/mL (10 mM) | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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