Rosuvastatin Calcium CAS NO.147098-20-2

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Rosuvastatin calcium Basic information

Product Name:

Rosuvastatin calcium

Synonyms:

Rosuvastatin Calcium(W.S);calcium (3R,5S,E)-7-(4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethan-3-ylsulfonamido)pyrimidin-5-yl)-3,5-dihydroxyhept-6-enoate;ZD4522;(3R,5S,6E)-7-[4-(4-fluorophenyl)-6-(1-methylethyl)-2-[N-methyl(n-methylsulfonyl)amino]-5-pyrimidinyl]-3,5-dihydroxy-6-Hep;Rosuvastatin (as Ca salt);Calcium (3R,5S,E)-7-(4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethylsulfonamido)pyrimidin-5-y;Rosuvastatin CalciuM (3R,5S,6E)-7-[4-(4-fluorophenyl)-6-(1-Methylethyl)-2-[N-Methyl(n-Methylsulfonyl)aMino]-5-pyriMidinyl]-3,5-dihydroxy-6-Heptenoic calciuM;ROSUVASTATIN, CALCIUM SALT

CAS:

147098-20-2

MF:

C44H54CaF2N6O12S2

MW:

1001.14

EINECS:

627-028-1


Rosuvastatin calcium Chemical Properties

Melting point

122°C

alpha

D24 +14.8° (c = 1.012 in 50% methanol)

storage temp.

-20°C Freezer

form

powder

color

white to beige

optical activity

[α]/D +12 to +18°, c = 1 in methanol: water (1:1)

λmax

243nm(Phosphate buffer sol.)(lit.)

Merck

14,8270


Rosuvastatin calcium Usage And Synthesis

Uses

For making lipid-lowering drugs.

Description

Rosuvastatin, one of the two new statins launched for the treatment of hypercholesterolemia, has high hepato-selectivity and more potent inhibitory effect on HMG-CoA reductase than the previously marketed statins. In rat hepatocytes, it inhibits cholesterol biosynthesis with an IC50 of 1.12 nM, which is ~100-fold higher potency than pravastatin. Rosuvastatin is synthesized in a 12-step sequence, entailing the construction of a pyrimidinyl aldehyde intermediate in eight steps and subsequent introduction of the dihydroxyheptenoate side chain via Wittig reaction with a bketophosphorane reagent and stereoselective carbonyl reduction of the resultant enone. Pharmacokinetic properties of rosuvastatin in humans, dosed at 5–80 mg, are approximately linear with dose. Following oral administration, rosuvastatin is rapidly absorbed with an oral bioavailability of ~20% and tmax of ~3 h. It has a prolonged duration of action, with terminal t1/2 of ~20 h, compatible with once-daily dosing. In humans, rosuvastatin is minimally metabolized through CYP2C9 and CYP2C19, with little or no metabolism via the CYP3A4. Approximately 90% of the administered oral dose is eliminated in the feces (92% as the parent compound) and the rest in the urine. Rosuvastatin is considered a “superstatin” due to its ability, at well-tolerated doses, to lower LDL cholesterol and triglycerides to a much greater extent than first generation statins. In patients with hypercholesterolemia, rosuvastatin treatment at doses of 5 and 10 mg/day over 12-week period resulted in 40–43% reduction of LDL-cholesterol levels, 12–13% increase in HDL-cholesterol, and 17– 19% reduction in triglycerides. In comparison, the efficacy range of LDL-cholesterol reductions by atorvastatin (10 mg/day), pravastatin (20 mg/day), and simvastatin (20 mg/day) was 28–35%. Rosuvastatin is a well-tolerated drug at doses of 1–20 mg and the most common side effects at these doses are headache, myalgia, pain and pharyngitis, which are consistent with those previously reported for statin therapy.

Chemical Properties

White to Off-White Crystalline Solid


Rosuvastatin calcium Specification

Character

White to yellow?powder

Identification

A: IR-Spectrum
 B: UV

Calcium content

3.5%-4.5%

water

≤5.0%

Specific rotation

14.0-20.0

Heavy Metals

≤0.002%

Related substance
 (HPLC)

Diastereomer

≤0.2%

Rosuvastatin Lactone

≤0.2%

Diene

≤0.1%

Unknown single impurity

≤0.1%

Total impurity

≤1.0%

Assay (on dry basis)%

98.0-102.0

http://www.jecibiochem.com/

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