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220246-81-1

中文名稱(chēng) 左西孟旦雜質(zhì)
英文名稱(chēng) (R)-N-Acetyl-6-(4-aminophenyl)-4,5-dihydro-5-methyl-3(2H)-pyridazinone
CAS 220246-81-1
分子式 C13H15N3O2
分子量 245.28
MOL 文件 220246-81-1.mol
更新日期 2024/12/18 16:47:17
220246-81-1 結(jié)構(gòu)式 220246-81-1 結(jié)構(gòu)式

基本信息

中文別名
化合物 T12315
13C,2H3]-左西孟旦代謝物
英文別名
OR-1896
OR 1896,OR1896
13C,2H3]-Levosimendan metabolite
(R)-N-Acetyl-6-(4-aminophenyl)-4,5-dihydro-5-methyl-3(2H)-p
(R)-N-Acetyl-6-(4-aminophenyl)-4,5-dihydro-5-methyl-3(2H)-pyridazinone
(R)-N-(4-(4-Methyl-6-oxo-1,4,5,6-tetrahydropyridazin-3-yl)phenyl)acetamide
(R)-N-[4-(1,4,5,6-Tetrahydro-4-methyl-6-oxo-3-pyridazinyl)phenyl]-acetamide
Acetamide, N-[4-[(4R)-1,4,5,6-tetrahydro-4-methyl-6-oxo-3-pyridazinyl]phenyl]-

物理化學(xué)性質(zhì)

熔點(diǎn)224-226°C
密度1.27±0.1 g/cm3(Predicted)
儲(chǔ)存條件-20°C冷凍
溶解度可溶于丙酮(少許)、DMSO(少許)、甲醇(少許)
酸度系數(shù)(pKa)13.67±0.60(Predicted)
形態(tài)固體
顏色淡黃色至淡黃色
CAS 數(shù)據(jù)庫(kù)220246-81-1
左西孟旦雜質(zhì)價(jià)格(試劑級(jí))
報(bào)價(jià)日期產(chǎn)品編號(hào)產(chǎn)品名稱(chēng)CAS號(hào)包裝價(jià)格
2024/11/08HY-135746左西孟旦雜質(zhì)
OR-1896
220246-81-15mg2800元
2024/11/08HY-135746左西孟旦雜質(zhì)
OR-1896
220246-81-110mM * 1mLin DMSO3080元
2024/11/08HY-135746左西孟旦雜質(zhì)
OR-1896
220246-81-110mg5000元

常見(jiàn)問(wèn)題列表

生物活性
OR-1896 是 Levosimendan 的活性長(zhǎng)壽代謝產(chǎn)物。OR-1896 是一種高選擇性磷酸二酯酶 (PDE III) 抑制劑,是一種功能強(qiáng)大的血管擴(kuò)張劑。OR-1896 可以打開(kāi) ATP 敏感的 K+ 通道,并具有 Ca2+ 致敏作用。OR-1896 可減輕心肌細(xì)胞的凋亡,心臟重塑和心肌炎癥。
靶點(diǎn)

PDE3/PDE Ⅲ

K+ Channel

Drug Metabolite

體外研究

There are many evidences has accumulated and revealed a variety of beneficial pleiotropic effects OR-1896. OR-1896 evokes prominent vasodilatory responses, activation of ATP-sensitive sarcolemmal K + channels of smooth muscle cells appears as a powerful vasodilator mechanism. Additionally, activation of ATP-sensitive K + channels in the mitochondria potentially extends the range of cellular actions towards the modulation of mitochondrial ATP production and implicates a pharmacological mechanism for cardioprotection.

體內(nèi)研究

During the metabolism of Levosimendan approximately 5% of the drug is converted to the metabolite OR-1855 in the large intestine, and then acetylated in the liver to form the active metabolite OR-1896. Binding to plasma proteins is 98% for Levosimendan but only 40% for OR-1896. Unlike Levosimendan, which has an elimination half-life of 1-1.5 h, the half-life of OR-1896 is about 75 to 80 h allowing cardiovascular effects to persist up to 7 to 9 days after discontinuation of a 24-hour infusion of levosimendan. The pharmacokinetic of the parent drug is unaltered in subjects with severe renal impairment or with moderate hepatic impairment, whereas the elimination of its metabolites (OR-1896) can be prolonged.

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