3-溴甲基-2-环丙基-4-(4′-氟苯基)喹啉三苯基膦

3-溴甲基-2-环丙基-4-(4′-氟苯基)喹啉三苯基膦 - Names and Identifiers

Name	[2-Cyclopropyl-4-(4-fluorophenyl)-quinolin-3-ylmethyl]-triphenyl-phosphonium bromido
Synonyms	N-8.2 Pitavastatin InterMediate Pitavastatin Calcium Intermediate pitavastatin fluorine isomer impurity 2-Cyclopropyl-4-(4-fluoropenyl)-quinolyl-3-Methyltriphenyl BroMide [2-cyclopropyl-4-(4-fluorophenyl)-quinoline-3-methyl]-3-phenylphosphonium [[2-Cyclopropyl-4-(4-fluorophenyl)-3-quinolinyl]methyl]triphenylphosphonium bromide [2-Cyclopropyl-4-(4-fluorophenyl)-quinolin-3-ylmethyl]-triphenyl-phosphonium bromido [2-Cyclopropyl-4-(4-fluorophenyl)-quinolin-3-ylmethyl]-triphenyl-phosphonium bromide
CAS	154057-58-6
EINECS	1312995-182-4

3-溴甲基-2-环丙基-4-(4′-氟苯基)喹啉三苯基膦 - Physico-chemical Properties

Molecular Formula	C37H30BrFNP
Molar Mass	618.5169642
Melting Point	218-225℃
Solubility	Chloroform (Slightly), DMSO (Slightly)
Appearance	Solid
Color	White to Off-White
Storage Condition	Inert atmosphere,Room Temperature
Sensitive	Irritant
MDL	MFCD19440813

3-溴甲基-2-环丙基-4-(4′-氟苯基)喹啉三苯基膦 - Reference Information

Mechanism of action

The mechanism of action of pitavastatin calcium intermediate is currently believed to inhibit the rate-limiting enzyme in the early stage of intracellular cholesterol synthesis, that is, HMG-COA reductase, It reduces free cholesterol in the cell, and then feeds the expression of low-density lipoprotein (LDL) receptors on the surface of the cells, increasing the number of LDL receptors in the cell and enhancing the activity, the clearance of very low density lipoprotein (VLDL) residues or medium density lipoprotein (IDL) and LDL in the circulating blood was accelerated. In addition, it can also inhibit the synthesis of VLDL in liver. Its effect on reducing total cholesterol (TC) and LDL-C is obvious, and it also reduces triglyceride (TG) and increases high density lipoprotein cholesterol (HDL-C).

pharmacology

the pharmacology of pitavastatin calcium is as follows:(1) inhibition of HMG-CoA reductase pitavastatin calcium has a strong antagonistic inhibitory effect on HMG-Co a enzyme with an IC50 value of 6.8n M, and its intensity is 2.4 times that of simvastatin and 6.8 times that of fluvastatin. (2) Obtaining the synthesis of cholesterol. Pitavastatin calcium can effectively inhibit the process of cholesterol generation in human hepatocytes Hep G2, with IC50 value of 5.8nM, and its intensity is 2.9 times that of simvastatin and 5.7 times that of atorvastatin. However, pitavastatin calcium has a very weak inhibitory effect on the cholesterol production process after mevalonate production. (3) Increasing LDL receptor density Pitavastatin calcium can induce the synthesis of LDS receptor mRNA at an ultra-low concentration of 1 μM, increasing its number, resulting in an increase in LDL receptor density, thereby promoting the clearance of LDL and reducing plasma LDL-cholesterol concentration and plasma total triglyceride concentration.

Last Update：2024-04-10 22:29:15