R-impp (PF-00932239) is an anti-secreting inhibitor of PCSK9 (IC50=4.8 μM), which can inhibit PCSK9 protein translation by targeting the ribosomes at the time of 80S.
| Cell Experiment | |
|---|---|
| Cell lines | Huh7 cells |
| Preparation method | Huh7 cells are plated at 150,000 cells per well and transfected with the full-length and truncation mutants. After 24 hr, cells are treated with vehicle, 30 μMR-IMPP, or 30 μM S-IMPP. At 48 hr post-transfection, cells are washed three times with TBS +2 mg/mL BSA and lysed with 100 mL of RIPA buffer per well. Protein lysates are subjected to SDS-PAGE and western blot analysis for PCSK9 (V5) and b-actin. |
| Concentrations | 10, 30 μM |
| Incubation time | 24 h |
| Animal Experiment | |
|---|---|
| Animal models | |
| Formulation | |
| Dosages | |
| Administration | |
| Molecular Weight | 389.49 |
| Formula | C24H27N3O2 |
| CAS Number | 2133832-83-2 |
| Solubility (25°C) | DMSO ≥ 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related PCSK9 Products |
|---|
| AZD0780
AZD0780 (PCSK9-IN-12, EX-A6975) is a heteroaryl compound. AZD0780 (PCSK9-IN-12, EX-A6975) has bind affinity for PCSK9 with a Kd value of ＜200 nM. AZD0780 (PCSK9-IN-12, EX-A6975) can be used for the research of cholesterol metabolism. |
| NNC0385-0434
NNC0385-0434 is an orally active peptide small molecule PCSK9 inhibitor for atherosclerosis-related studies. |
| CiVi-008
CiVi-008 is an orally active PCSK9 antisense oligonucleotide (ASO) inhibitor for studies related to disorders of lipid metabolism. |
| CiVi-007
CiVi-007 is an antisense oligonucleotide (ASO) polymerized with N-acetylglucosamine that targets PCSK9 and can be used in studies related to hypercholesterolemia. |
| AZD-8233
AZD-8233 is an orally active, antisense oligonucleotide (ASO) targeting PCSK9 that targets and inhibits the translation and protein synthesis of PCSK9 mRNA in hepatocytes and reduces circulating LDL-C levels. It can be used in studies related to hypercholesterolemia. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
