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Merck
CN
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安全信息

SML3467

Sigma-Aldrich

Remimazolam

≥98% (HPLC)

别名:

(S)-Methyl 3-(8-bromo-1-methyl-6-(pyridin-2-yl)-4H-benzo[f]imidazo[1,2-a][1,4]diazepin-4-yl)propanoate, CNS 7054 methyl ester, CNS 7056, CNS-7054 methyl ester, CNS-7056, CNS7054 methyl ester, CNS7056, Methyl 3-{(4S)-8-bromo-1-methyl-6-(pyridin-2-yl)-4H-imidazo[1,2-a][1,4]benzodiazepin-4-yl}propanoate, ONO 2745, ONO-2745, ONO2745

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About This Item

经验公式（希尔记法）:
C21H19BrN4O2
CAS号:
308242-62-8
分子量:
439.31
MDL编号:
MFCD18633229
UNSPSC代码:
12352200

质量水平

100

方案

≥98% (HPLC)

表单

powder

药品控制

USDEA Schedule IV

颜色

white to beige

溶解性

DMSO: 2 mg/mL, clear

储存温度

-10 to -25°C

SMILES字符串

CC1=CN=C2[C@H](CCC(OC)=O)N=C(C3=CC=CC=N3)C4=CC(Br)=CC=C4N12

InChI

1S/C21H19BrN4O2/c1-13-12-24-21-17(7-9-19(27)28-2)25-20(16-5-3-4-10-23-16)15-11-14(22)6-8-18(15)26(13)21/h3-6,8,10-12,17H,7,9H2,1-2H3/t17-/m0/s1

InChI key

CYHWMBVXXDIZNZ-KRWDZBQOSA-N

生化/生理作用

Remimazolam (CNS 7056) is a benzodiazepine derivative with positive allosteric modulator (PAM) activity toward γ-aminobutyric acid type A (GABAA) receptor (pKi = 7.53/7.50/7.56 against 2.5 nM flunitrazepam for binding human/rat/yucatan micropig brain homogenates; pEC50/Emax = 6.44/375% (α1β2γ2), 6.18/186% (α2β2γ2), 6.04/210% (α3β2γ2), 5.86/289% (α5β2γ2s) by whole cell patch clamp using cells expressing respective rat αβγ complex). Intravenous injection (25 mg/kg rats, 15-30 mg/kg mice) causes fast onset and short duration of sedative action with rapid recovery when compared with midazolam.

象形图

Exclamation mark
GHS07

警示用语：

Warning

危险声明

H336

危险分类

STOT SE 3

靶器官

Respiratory system

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

法规信息

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分析证书(COA)

Lot/Batch Number
0000220344
0000220343
0000220344
0000220343
0000198426

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Pharmacokinetics and pharmacodynamics of the short-acting sedative CNS 7056 in sheep
R N Upton , A A Somogyi, A M Martinez, J Colvill, C Grant
British Journal of Anaesthesia, 105, 798-809 (2010)
Inhaled Remimazolam Potentiates Inhaled Remifentanil in Rodents
Bevans T, Deering-Rice C, Stockmann C, Rower J, Sakata D, Reilly C
Anesthesia and Analgesia, 124, 1484-1490 (2017)
Metabolism of remimazolam in primary human hepatocytes during continuous long-term infusion in a 3-D bioreactor system
Freyer N, Knospel F, Damm G, Greuel S, Schneider C, Seehofer D, Stohr T, Petersen KU, Zeilinger K
Drug design, development and therapy, 13, 1033-1047 (2019)
Design, Synthesis, and Biological Evaluation of Novel CNS 7056 Derivatives as Sedatives in Rats and Rabbits
Yan Liu , Xiangqing Xu , Jianyong Xie , Huan Ma , Tao Wang , Guisen Zhang , Qingeng Li
Chemical Biology & Drug Design, 88, 38-42 (2016)
Comparison of the sedative properties of CNS 7056, midazolam, and propofol in sheep
R N Upton , A M Martinez, C Grant
British Journal of Anaesthesia, 103, 848-857 (2009)
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