Synonym
PF-06815345 HCl; PF06815345 HCl; PF 06815345 HCl; PF-06815345 hydrochloride
IUPAC/Chemical Name
(S)-1-(5-(4-(4-((3-chloropyridin-2-yl)((R)-piperidin-3-yl)carbamoyl)-2-fluorophenyl)-1-methyl-1H-pyrazol-5-yl)-1H-tetrazol-1-yl)ethyl ethyl carbonate hydrochloride
InChi Key
RFEUFHPTEFEGDQ-KUGOCAJQSA-N
InChi Code
InChI=1S/C27H29ClFN9O4.ClH/c1-4-41-27(40)42-16(2)38-25(33-34-35-38)23-20(15-32-36(23)3)19-10-9-17(13-22(19)29)26(39)37(18-7-5-11-30-14-18)24-21(28)8-6-12-31-24;/h6,8-10,12-13,15-16,18,30H,4-5,7,11,14H2,1-3H3;1H/t16-,18+;/m0./s1
SMILES Code
O=C(O[C@H](N1N=NN=C1C2=C(C3=CC=C(C(N(C4=NC=CC=C4Cl)[C@H]5CNCCC5)=O)C=C3F)C=NN2C)C)OCC.[H]Cl
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Preparing Stock Solutions
The following data is based on the
product
molecular weight
634.49
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
Lavecchia, A., & Cerchia, C. (2019). Recent advances in developing PCSK9 inhibitors for lipid-lowering therapy. Future medicinal chemistry, 11(5), 423-441.
Aspnes, G. E., Coffey, S. B., Darout, E., Dechert-Schmitt, A. M., Dullea, R. G., Kamlet, A. S., ... & Xiao, J. (2023). Small molecule inhibitors of PCSK9. SAR investigations of head and amine groups. Bioorganic & Medicinal Chemistry Letters, 92, 129394.
Ahamad, S., & Bhat, S. A. (2022). Recent update on the development of PCSK9 inhibitors for hypercholesterolemia treatment. Journal of Medicinal Chemistry, 65(23), 15513-15539.
Piotrowski, D. W., & McInturff, E. L. (2019). Discovery and Early Development of Small Molecule Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9) Inhibitors. In Complete Accounts of Integrated Drug Discovery and Development: Recent Examples from the Pharmaceutical Industry Volume 2 (pp. 267-296). American Chemical Society.
