Fosaprepitant dimeglumine / CAS：265121-04-8
Kev Piav Qhia Luv:
Lub npe khoom: Fosaprepitant dimeglumine
Hom: ZA-N
CAS: 265121-04-8
MF:C30H39F7N5O11P
MW: 809.63
QAUV:
cov lus qhia tshwj xeeb
| Khoom Siv Kuaj | Cov Qauv Txais Yuav | Qhov tshwm sim |
| Qhov tsos | Hmoov dawb los yog dawb tawm | Hmoov dawb |
| Kev yaj tau | Cov khoom no yooj yim soluble hauv dej thiab methanol, tab sis insoluble hauv ethanol lossis acetonitrile | Ua raws li |
| Kev sib hloov tshwj xeeb | +28.0° mus rau＋33.0°
| +31.5°
|
| Kev txheeb xyuas UV | Muaj qhov nqus siab tshaj plaws ntawm qhov ntev ntawm 210nm thiab 263nm | Ua raws li
|
| Kev txheeb xyuas infrared | Lub spectrum nqus infrared yuav tsum sib xws nrog lub spectrum ntawm cov khoom siv siv. | Ua raws li
|
| Kev txheeb xyuas Chromatographic | Lub sijhawm khaws cia ntawm lub ncov tseem ceeb ntawm cov tshuaj sim yuav tsum sib xws nrog cov tshuaj siv piv txwv. | Ua raws li
|
| Alkalinity | 7.0~9.0 | 7.7 |
| Kev meej ntawm kev daws teeb meem | Yuav tsum pom tseeb; Txhua qhov opalescence tsim tawm tsis pom tseeb dua li ntawm qhov kev ncua ncua II | Ua raws li
|
| Cov khoom muaj feem xyuam | Kev Ua Phem A ≤ 0.15% Kev Tsis Huv B ≤ 0.1% Kev Tsis Huv I3-1 ≤ 0.15% Lwm yam tsis huv ≤ 0.10% Tag nrho cov khoom tsis huv ≤ 1.0% | 0.08% Tsis pom 0.04% 0.03% 0.15% |
| Enantiomer | Tsis pub tshaj 0.15% | Tsis pom |
| Cov tshuaj yaj seem 1 | Methanol ≤3000ppm Ethanol ≤5000ppm Acetonitrile ≤410ppm Ether ≤ 5000ppm Acetone ≤5000ppm Methyl tert butyl ether ≤5000ppm Toluene ≤890ppm
| 1667ppm 92ppm Tsis pom 54ppm 2636ppm 187ppm Tsis pom
|
| Cov tshuaj yaj seem 2 | Triethylamine ≤5000ppm
| 58ppm
|
| Cov dej ntsiab lus | ≤2.0% | 1.4% |
| Cov hlau hnyav | Yuav tsum tsis pub tshaj 10 ppm | Ua raws li |
| Palladium | Tsis pub tshaj tsib ppm | Tsis pom |
| Chloride | Nws yuav tsum tsis pub tshaj 0.01% | Ua raws li |
| Sulfate | Nws yuav tsum tsis pub tshaj 0.1% | Ua raws li |
| Meglumine | Raws li kev xam anhydrous, cov ntsiab lus ntawm C7H17NO5 yuav tsum yog 37.8% txog 39.8% | 38.5% |
| Kev Ntsuas | Raws li kev xam anhydrous, cov ntsiab lus ntawm C23H22F7N4O6P·2(C7H17NO5) yuav tsum yog 98.0% ~ 102.0% | 100.4%
|
| Cov kab mob endotoxin | Tus nqi ntawm endotoxin ib mg ntawm Fosaprepitant Dimeglumine yuav tsum tsawg dua 0.16 EU | Ua raws li
|
| Kev Txwv ntawm Cov Kab Mob Me Me | Tag nrho cov kab mob aerobic tsis pub ntau tshaj 100 cfu, tag nrho cov pwm thiab cov poov xab ua ke tsis pub ntau tshaj 50 cfu ib g ntawm cov qauv kuaj thiab Escherichia coli tsis muaj. | Tag nrho cov kab mob aerobic: 3cfu / g Tag nrho cov pwm thiab cov poov xab ua ke suav tau:＜10cfu/g Escherichia coli: Tsis tau kuaj pom
|
| Xaus lus | Cov khoom lees paub tus qauv lag luam | |
Kev Siv
Muaj peb hom neurokinin receptors: NK1, NK2 thiab NK3. Ntawm lawv, NK1 receptor muaj peev xwm khi tau cov tshuaj P zoo tshaj plaws thiab muaj cov ntsiab lus siab tshaj plaws hauv qhov chaw ntuav ntawm lub hlwb. Tom qab NK1 receptor khi rau cov tshuaj P hauv lub paj hlwb, nws ua rau muaj ntau yam txheej txheem pathophysiological xws li ntuav, ntxhov siab thiab mob taub hau. NK1RAs xws li apirpitan thiab fosapirpitan tiv thaiv thiab kho CINV tau zoo los ntawm kev xaiv khi rau NK1 receptor. Feem ntau, CINV mob hnyav yog cuam tshuam nrog kev ua haujlwm ntawm txoj kev siv zog 5-HT3, thaum CINV qeeb yog cuam tshuam nrog cov tshuaj P hauv nruab nrab. Yog li ntawd, piv nrog 5-HT3RAs, apirpitan thiab fosapirpitan qhia tau tias muaj txiaj ntsig zoo rau kev ntuav qeeb.
Fosapirtan dimethylmeglumine yog ib qho neurokinin-1receptorantagonist (NK-1RA) tsim los ntawm Merck. Nws tau tso tawm thawj zaug hauv Tebchaws Meskas thaum Lub Ib Hlis 2008. Fosarpitan dimethylmegalamine yog cov tshuaj ua ntej ntawm aprepitant, thawj cov tshuaj NK-1RA. Tom qab nkag mus rau hauv lub cev, nws tuaj yeem hloov pauv sai sai mus rau hauv aprepitant thiab siv hauv kev kho mob los tiv thaiv thiab kho mob xeev siab lossis ntuav qeeb uas tshwm sim los ntawm kev siv thawj zaug thiab rov ua dua ntawm kev kho mob chemotherapy nruab nrab mus rau siab (suav nrog cov tshuaj cisplatin siab).
Fosaprepitant dimeglumine ntsev (MK-0517) yog cov tshuaj phosphoacyl precursor uas yaj tau hauv dej ntawm aprepitant thiab yog NK1 antagonist.
Ntim thiab Xa Khoom
5kg, 25kg raws li cov neeg siv khoom xav tau.
Yog cov khoom siv dav dav thiab tuaj yeem xa los ntawm dej hiav txwv thiab huab cua
Khaws cia thiab khaws cia
Lub neej txee: 24 lub hlis txij li hnub tsim khoom hauv cov ntim khoom tsis tau qhib khaws cia rau hauv qhov chaw txias thiab qhuav kom tsis txhob raug tshav ntuj ncaj qha, dej.
Lub tsev rau khoom muaj cua nkag, ziab kom qhuav kub tsawg, Sib cais ntawm cov tshuaj oxidants, cov kua qaub.
