Benzamide, N-[3-[[(3S)-3-amino-1-piperidinyl]methyl]-5-(4-methyl-1H-imidazol-1-yl)phenyl]-4-methyl-3-phenoxy-
- CAS No.
- 2244129-23-3
- Chemical Name:
- Benzamide, N-[3-[[(3S)-3-amino-1-piperidinyl]methyl]-5-(4-methyl-1H-imidazol-1-yl)phenyl]-4-methyl-3-phenoxy-
- Synonyms
- PCSK9-IN-13;(S)-N-(3-((3-Aminopiperidin-1-yl)methyl)-5-(4-methyl-1H-imidazol-1-yl)phenyl)-4-methyl-3-phenoxybenzamide;Benzamide, N-[3-[[(3S)-3-amino-1-piperidinyl]methyl]-5-(4-methyl-1H-imidazol-1-yl)phenyl]-4-methyl-3-phenoxy-
- CBNumber:
- CB612150067
- Molecular Formula:
- C30H33N5O2
- Molecular Weight:
- 495.62
- MDL Number:
- MOL File:
- 2244129-23-3.mol
Benzamide, N-[3-[[(3S)-3-amino-1-piperidinyl]methyl]-5-(4-methyl-1H-imidazol-1-yl)phenyl]-4-methyl-3-phenoxy- Chemical Properties,Uses,Production
Uses
PCSK9-IN-13(compound 3f) is a potent PCSK9 inhibitor, which can antagonize low-density lipoprotein (LDL) receptor binding by binding to PCSK9, with an IC50 of 537 nM[1].
in vivo
PCSK9-IN-13(compound 3f) (3.28 or 16.4 mg/kg/day, s.c., 14 days) in male C57BL/6 mice dose not show a reduction in total cholesterol at a dose of 3.28 mg/kg, however, a dose of 16.4 mg/kg shows a significant reduction of total cholesterol plasma levels by approximately 10%, and exhibits excellent bioavailability[1].
The pharmacokinetic parameters of PCSK9-IN-13(compound 3f) in C57BL/6 mice
Parameter | SC | PO | IV(single) | IV(cassette) |
Dose(mg/kg) | 20 | 20 | 5 | 0.4 |
Tmax(h) | 1 | 2 | - | - |
Cmax(ng/mL) | 2207 | 52.6 | - | - |
CL(L/h/kg) | - | - | 1.09 | 0.3 |
Vss(L/kg) | - | - | 3.87 | 9.13 |
T1/2(h) | 5.47 | - | 9.86 | 25.7 |
AUC∞(h*ng/mL) | 16811 | - | 4605 | 1472 |
MRT∞(h) | - | - | 3.56 | 34.9 |
F(%) | 91.3 | 0.527 | - | - |
References
[1] Benny J.?Evison, et al. A small molecule inhibitor of PCSK9 that antagonizes LDL receptor binding via interaction with a cryptic PCSK9 binding groove.Bioorganic & Medicinal Chemistry
Benzamide, N-[3-[[(3S)-3-amino-1-piperidinyl]methyl]-5-(4-methyl-1H-imidazol-1-yl)phenyl]-4-methyl-3-phenoxy- Preparation Products And Raw materials
Raw materials
Preparation Products
Benzamide, N-[3-[[(3S)-3-amino-1-piperidinyl]methyl]-5-(4-methyl-1H-imidazol-1-yl)phenyl]-4-methyl-3-phenoxy- Suppliers
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
TargetMol Chemicals Inc. | +17819995354 | marketing@targetmol.com | United States | 19939 | 58 |
Shanghai Beckham Medical Technology Co., Ltd | 021-13816613772 13816613772 | huahero21@sina.com | China | 1666 | 55 |
Tianjin Kailiqi Biotechnology Co., Ltd. | 15076683720 | klq@cw-bio.com | China | 6708 | 55 |
Angel Pharmatech, Ltd. | 17317130613 | 3358272972@qq.com | China | 3267 | 58 |
Bide Pharmatech Ltd. | 400-1647117 13681763483 | product02@bidepharm.com | China | 62320 | 58 |
TargetMol Chemicals Inc. | 4008200310 | marketing@tsbiochem.com | China | 24982 | 58 |
Shanghai Tachizaki Biomedical Research Center | 18014399201 | sales@chemlab-tachizaki.com | China | 2678 | 58 |
View Lastest Price from Benzamide, N-[3-[[(3S)-3-amino-1-piperidinyl]methyl]-5-(4-methyl-1H-imidazol-1-yl)phenyl]-4-methyl-3-phenoxy- manufacturers
Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
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2025-07-16 | PCSK9-IN-13
2244129-23-3
|
US $2180.00-1670.00 / mg | 10g | TargetMol Chemicals Inc. |
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- PCSK9-IN-13
2244129-23-3
- US $2180.00-1670.00 / mg
- TargetMol Chemicals Inc.