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PCSK9-IN-10, a potent and orally active inhibitor of Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9), exhibits a half-maximal inhibitory concentration (IC50) of 6.4 µM. By enhancing the expression of Low-Density Lipoprotein Receptor (LDLR) protein and reducing PCSK9 expression, PCSK9-IN-10 effectively decreases atherosclerosis progression. This compound holds promise for hyperlipidemia research applications.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
2 mg | $35 | In Stock | |
5 mg | $58 | In Stock | |
10 mg | $93 | In Stock | |
25 mg | $188 | In Stock | |
50 mg | $296 | In Stock | |
100 mg | $435 | In Stock | |
200 mg | $616 | In Stock | |
1 mL x 10 mM (in DMSO) | $59 | In Stock |
Description | PCSK9-IN-10, a potent and orally active inhibitor of Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9), exhibits a half-maximal inhibitory concentration (IC50) of 6.4 µM. By enhancing the expression of Low-Density Lipoprotein Receptor (LDLR) protein and reducing PCSK9 expression, PCSK9-IN-10 effectively decreases atherosclerosis progression. This compound holds promise for hyperlipidemia research applications. |
Targets&IC50 | PCSK9:6.4 µM |
In vitro | PCSK9-IN-10 (0, 2.5, 5, 12.5, 25 µM ; 24 h) significantly reduces PCSK9 protein expression and increases the expression of LDL receptor (LDLR) in a dose-dependent manner.[1] |
In vivo | PCSK9-IN-10 (30 mg/kg; oral administration; once daily for 8 weeks) reduces total cholesterol (TC) levels and atherosclerotic plaque size in ApoE KO mice.[1] |
Molecular Weight | 373.41 |
Formula | C18H23N5O4 |
Cas No. | 368434-98-4 |
Smiles | COCCNc1nc2n(C)c(=O)n(C)c(=O)c2n1Cc1cccc(OC)c1 |
Relative Density. | 1.32 g/cm3 (Predicted) |
Storage | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 225.0 mg/mL (602.6 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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