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A7665458

PitavastatinCalcium , 10mMinDMSO , 147526-32-7

CAS NO.:147526-32-7

Empirical Formula: C25H26CaFNO4

Molecular Weight: 463.56

MDL number: MFCD01937979

EINECS: 807-641-2

Pack Size Price Stock Quantity
1ml RMB559.20 In Stock
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Update time: 2022-07-08

PRODUCT Properties

Melting point: >138oC (dec.)
alpha  D20 +23.1° (c = 1.00 in acetonitrile/water)
storage temp.  2-8°C
solubility  DMSO (Slightly), Methanol (Slightly)
form  Solid
color  White to Off-White
Stability: Hygroscopic
InChIKey ADXNRJCYUMOXPZ-MNGIKBOWNA-N
SMILES C(/C1C(C2CC2)=NC2C=CC=CC=2C=1C1C=CC(F)=CC=1)=C\[C@@H](O)C[C@@H](O)CC(=O)O.[Ca] |&1:22,25,r|
CAS DataBase Reference 147526-32-7(CAS DataBase Reference)

Description and Uses

Pitavastatin, launched for the treatment of hypercholesterolemia, belongs to the family of second-generation statins, also referred to as superstatins due to their improved efficacy as cholesterol lowering agents. Like other statins, pitavastatin reduces plasma cholesterol levels by competitively inhibiting HMG-CoA reductase, the rate-limiting enzyme of cholesterol biosynthesis in the liver. It is a more potent inhibitor of HMG-CoA reductase than the previously marketed statins and has the potential benefit of not undergoing significant metabolism by CYP3A4. Pitavastatin is synthesized in a multi-step sequence, including the key step of introducing the dihydroxyheptenoate side chain by cross-coupling of a 3-iodoquinoline intermediate with an alkenylborane reagent. Unlike rosuvastatin, pitavastatin has a high oral bioavailability (~80%). Plasma protein binding is also high for pitavastatin (>95%), and regardless of the dosing, the highest tissue levels are found in the liver, its target organ. After oral administration, the peak plasma concentration is reached at ,0.8 h and the mean elimination half-life is ~11 h. Pitavastatin is only minimally metabolized, mainly by CYP2C8 and CYP2C9, and the predominant route of elimination of the parent drug and its metabolites is by means of bile excretion followed by elimination in the feces. In clinical studies, oral doses of 2–4 mg/day of pitavastatin produced dose-dependent reduction in LDL-cholesterol levels by 40–48% from baseline in patients with heterozygous familial hypercholesterolemia. In a 12-week double-blind comparative study, pitavastatin (2 mg/day) was more effective than pravastatin (10 mg/day) in reducing LDL-cholesterol levels (38 and 18%, respectively); however, both agents produced similar increases in HDL-cholesterol (~9%). The drug was well tolerated and the adverse reactions were mild and transient.

A competitive inhibitor of HMG-CoA reductase. Antilipemic.

Safety

Symbol(GHS) 
GHS06
Signal word  Danger
Hazard statements  H301+H311+H331-H315-H319
Precautionary statements  P501-P261-P270-P271-P264-P280-P337+P313-P305+P351+P338-P361+P364-P332+P313-P301+P310+P330-P302+P352+P312-P304+P340+P311-P403+P233-P405
Safety Statements  24/25
HS Code  29339900
Toxicity LDLo orl-rat: 500 mg/kg OYYAA2 56,67,1998

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