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103878-83-7

中文名稱 拉扎貝胺鹽酸鹽
英文名稱 N-(2-Aminoethyl)-5-chlor-2-pyridincarboxamid-hydrochlorid
CAS 103878-83-7
分子式 C8H10ClN3O.HCl
MOL 文件 103878-83-7.mol
更新日期 2023/03/20 15:41:17
103878-83-7 結(jié)構(gòu)式 103878-83-7 結(jié)構(gòu)式

基本信息

中文別名
拉扎貝胺鹽酸鹽
英文別名
TeMpiuM
Ro 19-6327/001
JMFKTFLARGGXCC-UHFFFAOYSA-N
N-(2-Aminoethyl)-5-chlor-2-pyridincarbox
N-(2-Aminoethyl)-5-chlor-2-pyridincarboxamid-hydrochlorid
N-(2-Aminoethyl)-5-chloro-2-pyridinecarboxamide hydrochloride
2-PyridinecarboxaMide, N-(2-aMinoethyl)-5-chloro-, Monohydrochloride

物理化學(xué)性質(zhì)

熔點(diǎn)193-195°
儲(chǔ)存條件Desiccate at RT
溶解度Soluble to 100 mM in water and to 100 mM in DMSO
酸度系數(shù)(pKa)8.9(at 25℃)
形態(tài)粉末

安全數(shù)據(jù)

毒性LD50 orally in mice: 1000-2000 mg/kg (Imhof, Kyburz, 1986)
拉扎貝胺鹽酸鹽價(jià)格(試劑級(jí))
報(bào)價(jià)日期產(chǎn)品編號(hào)產(chǎn)品名稱CAS號(hào)包裝價(jià)格
2024/11/08S6422拉扎貝胺鹽酸鹽
Lazabemide
103878-83-725mg1286.7元

常見(jiàn)問(wèn)題列表

生物活性
Lazabemide (Ro 19-6327)是可逆性、選擇性MAO-B抑制劑,Ki值為7.9 nM。
靶點(diǎn)
TargetValue
MAO-B
(Cell-free assay)
7.9 nM(Ki)
體外研究

The in vitro binding characteristics of both radiolabeled inhibitors revealed them to be selective, high-affinity ligands for the respective enzymes. K D and B max values for 3 H-Ro 19-6327 in rat cerebral cortex are 18.4 nM and 3.45 pmol/mg protein, respectively. The IC 50 values for lazabemide are: 86 μM for NA uptake; 123 μM for 5HT uptake; > 500 μM for DA uptake, respectively.. Lazabemide (5 μM) inhibits human MAO-B and MAO-A with IC 50 of 6.9 nM and >10 nM, respectively. And it inhibits rat MAO-B and MAO-A with IC 50 of 37 nM and >10 μM, respectively ina enzymatic assay.Lazabemide differs from L-deprenyl in their ability to induce release of endogenous monoamines from synaptosomes. Thus, Lazabemide (500 μM) induces a greater 5 HT release than does L-deprenyl, but is less effective than L-deprenyl in releasing DA. On the contrary, lazabemide was almost completely inactive on either 5 HT and DA release. Lazabemide (250 nM) results in a clear inhibition of DOPAC formation, while does not increase the accumulation of newly-formed DA in those tubular epithelial cells loaded with 50 microM L-DOPA.

體內(nèi)研究

Lazabemide (3 mg/kg) attenuates ichemia reperfusion-induced hydroxyl radical generation and pretreatment with Lazabemide showed decreased DOPAC levels in comparison with those of their respective vehicle-treated control groups.

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