Rosuvastatin Calcium Cov ntaub ntawv yooj yim
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Khoom npe: |
Calcium Rosuvastatin |
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Synonyms: |
6-Heptenoic acid, 7-[4-(4-fluorophenyl)-6-(1-methylethyl)-2-[methyl (methylsulfonyl) amino]-5-pyrimidinyl]-3,5-dihydroxy-, calcium ntsev (2:1), (3R,5S,6E)-;(3R,5S,6E){20 }}[4-(4-Fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl])-3,{ {27}}dihydroxyhept-6-enoic acid hemicalcium ntsev; Rosuvastatin Calcium (WS); ZD 4522 Calcium; ROSUVASTATIN CALCIUM (ROSUVASTATIN HEMICALCIUM); Rosuvastadine; Rosuvastatin CalciuM (3R,5{36E) {34}}(4-fluorophenyl)-6-(1-Methylethyl)-2-[N-Methyl (n-Methylsulfonyl)aMino]-5-pyriMidinyl]{{ 42}}, 5-dihydroxy-6-Heptenoic calciuM; Rosuvastatin Calium |
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CAS: |
147098-20-2 |
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MF: |
C44H54CaF2N6O12S2 |
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MW: |
1001.14 |
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EINECS: |
627-028-1 |
Rosuvastatin calcium Chemical Properties
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Melting point |
122 degree |
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alpha |
D24 ntxiv rau 14.8 degree (c=1.012 hauv 50 feem pua methanol) |
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cia temp. |
2-8 degree |
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daim ntawv |
hmoov |
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xim |
dawb rau beige |
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kev ua haujlwm kho qhov muag |
[ ]/D ntxiv rau 12 txog 18 degree, c=1 hauv methanol: dej (1: 1) |
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lw max |
243nm (phosphate buffer sol.) (lit.) |
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Merck |
14,8270 |
Rosuvastatin Calcium Siv thiab Synthesis
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Siv |
Rau kev ua cov tshuaj lipid-txo qis. |
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Kev piav qhia |
Rosuvastatin, ib qho ntawm ob qhov tshiab statins tau tsim tawm rau kev kho mob hypercholesterolemia, muaj siab hepato-xaiv thiab muaj zog inhibitory nyhuv ntawm HMG-CoA reductase dua li yav dhau los ua lag luam statins. Hauv nas hepatocytes, nws inhibits cov roj cholesterol biosynthesis nrog IC50 ntawm 1.12 nM, uas yog -100-fold muaj zog dua pravastatin. Rosuvastatin yog synthesized nyob rau hauv ib tug 12- kauj ruam ib theem zuj zus, entailing kev tsim kho ntawm ib tug pyrimidinyl aldehyde intermediate nyob rau hauv yim kauj ruam thiab tom qab kev taw qhia ntawm lub dihydroxyheptenoate sab saw ntawm Wittig cov tshuaj tiv thaiv nrog ib tug bketophosphorane reagent thiab stereoselective carbonyl txo ntawm cov resultant encryption. Pharmacokinetic zog ntawm rosuvastatin nyob rau hauv tib neeg, koob tshuaj ntawm 5-80 mg, yog kwv yees li linear nrog koob. Tom qab kev tswj hwm qhov ncauj, rosuvastatin tau nqus sai nrog qhov ncauj bioavailability ntawm -20 feem pua thiab tmax ntawm -3 h. Nws muaj lub sijhawm ntev ntawm kev ua, nrog lub davhlau ya nyob twg t1/2 ntawm -20 h, sib xws nrog kev noj ib zaug ib hnub. Hauv tib neeg, rosuvastatin yog metabolized tsawg heev los ntawm CYP2C9 thiab CYP2C19, nrog me me los yog tsis muaj metabolism ntawm CYP3A4. Kwv yees li ntawm 90 feem pua ntawm cov tshuaj noj qhov ncauj raug tshem tawm hauv cov quav (92 feem pua ntawm cov niam txiv sib xyaw) thiab cov seem hauv cov zis. Rosuvastatin yog suav tias yog "superstatin" vim nws lub peev xwm, ntawm cov koob tshuaj zoo, kom txo qis LDL roj cholesterol thiab triglycerides ntau dua li thawj tiam statins. Hauv cov neeg mob hypercholesterolemia, kev kho rosuvastatin ntawm koob tshuaj 5 thiab 10 mg / hnub dhau ntawm 12-lub lim tiam ua rau txo qis LDL-cholesterol 40-43%, 12-13 feem pua nce hauv HDL-cholesterol, thiab 17- 19% txo qis hauv triglycerides. Hauv kev sib piv, qhov ua tau zoo ntawm LDL-cholesterol txo los ntawm atorvastatin (10 mg / hnub), pravastatin (20 mg / hnub), thiab simvastatin (20 mg / hnub) yog 28-35 feem pua. Rosuvastatin yog ib qho tshuaj uas tau txais txiaj ntsig zoo ntawm koob tshuaj 1-20 mg thiab cov kev mob tshwm sim feem ntau ntawm cov koob tshuaj no yog mob taub hau, myalgia, mob thiab pharyngitis, uas zoo ib yam nrog cov yav tas los qhia rau kev kho statin. |
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Chemical Properties |
Dawb rau Off-White Crystalline Khoom |
Rosuvastatin Calcium Specification
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Cim |
Dawb rau daj? hmoov |
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Kev txheeb xyuas |
A: IR-Spectrum |
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Cov ntsiab lus calcium |
3.5 feem pua -4.5 feem pua |
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dej |
Tsawg dua lossis sib npaug li 5.0 feem pua |
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Kev sib hloov tshwj xeeb |
14.0-20.0 |
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Hnyav Hlau |
Tsawg dua lossis sib npaug rau 0.002 feem pua |
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Muaj feem xyuam |
Diastereomer |
Tsawg dua los yog sib npaug rau 0.2 feem pua |
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Rosuvastatin Lactone |
Tsawg dua los yog sib npaug rau 0.2 feem pua |
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Diene |
Tsawg dua lossis sib npaug rau 0.1 feem pua |
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Unknown ib impurity |
Tsawg dua lossis sib npaug rau 0.1 feem pua |
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Tag nrho impurity |
Tsawg dua lossis sib npaug rau 1.0 feem pua |
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Assay (ntawm qhuav hauv paus) feem pua |
98.0-102.0 |
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Cim npe nrov: rosuvastatin calcium cas no.147098-20-2, Suav teb, manufacturers, lwm tus neeg, Hoobkas, kev cai, wholesale
