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Sigma-Aldrich

1′-Hydroxymidazolam

≥97% (HPLC), powder

同義詞:

8-Chloro-6-(2-fluorophenyl)-1-hydroxymethyl-4H-imidazo[1,5a][1,4]benzodiazepine

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About This Item

經驗公式(希爾表示法):
C18H13ClFN3O
CAS號碼:
分子量::
341.77
MDL號碼:
分類程式碼代碼:
12161501
PubChem物質ID:
NACRES:
NA.77

product name

1′-Hydroxymidazolam,

形狀

powder

藥物控制

regulated under CDSA - not available from Sigma-Aldrich Canada

顏色

white to off-white

儲存溫度

2-8°C

SMILES 字串

OCc1ncc2CN=C(c3ccccc3F)c4cc(Cl)ccc4-n12

InChI

1S/C18H13ClFN3O/c19-11-5-6-16-14(7-11)18(13-3-1-2-4-15(13)20)22-9-12-8-21-17(10-24)23(12)16/h1-8,24H,9-10H2

InChI 密鑰

QHSMEGADRFZVNE-UHFFFAOYSA-N

一般說明

1′-Hydroxymidazolam is the metabolite of midazolam.

應用

1′-Hydroxymidazolam (1′-OHMDZ) can be used for assessing Cyp3a11 enzyme activity as well as for pharmacokinetic (PK) study of midazolam.
CYP3A4 metabolite of midazolam.

生化/生理作用

1′-Hydroxymidazolam is the major hydroxylated metabolite of Midazolam (MDZ), forms due to rapid and extensive metabolization of MDZ by the CYP 450 3A isoenzymes in the liver. The product contributes to the pharmacological impact of MDZ.

特點和優勢

This compound is a featured product for ADME Tox research. Click here to discover more featured ADME Tox products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.

包裝

Bottomless glass bottle. Contents are inside inserted fused cone.

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable

個人防護裝備

Eyeshields, Gloves, type N95 (US)


分析證明 (COA)

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A S Gandhi et al.
British journal of pharmacology, 166(7), 2176-2187 (2012-03-08)
Gene expression of Cyp3a11 is reduced by activation of Toll-like receptors (TLRs) by Gram-negative or Gram-positive bacterial components, LPS or lipoteichoic acid (LTA) respectively. The primary adaptor protein in the TLR signalling pathway, TIRAP, plays differential roles in LPS- and
Sussan Ghassabian et al.
The AAPS journal, 21(2), 15-15 (2019-01-11)
The multi-kinase inhibitor sorafenib (SOR) is clinically important in the treatment of hepatocellular and renal cancers and undergoes CYP3A4-dependent oxidation in liver to the pharmacologically active N-oxide metabolite (SNO). There have been reports that kinase inhibitors such as SOR may
Ki Bum Hong et al.
Molecules (Basel, Switzerland), 23(8) (2018-08-17)
Although mollugin, the main ingredient of the oriental medicinal herb Rubia cordifolia, has considerable anti-inflammatory effects, it has poor aqueous solubility as well as poor metabolic and plasma stability. To overcome these shortfalls, various mollugin derivatives have been synthesized and
Kar Lai Poon et al.
Archives of toxicology, 91(3), 1187-1197 (2016-08-04)
Understanding and predicting whether new drug candidates will be safe in the clinic is a critical hurdle in pharmaceutical development, that relies in part on absorption, distribution, metabolism, excretion and toxicology studies in vivo. Zebrafish is a relatively new model
Pharmacokinetics of midazolam and its main metabolite 1-hydroxymidazolam in intensive care patients
Boulieu R, et al.
Eur. J. Drug Metab. Pharmacokinet., 23(2), 255-258 (1998)

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