| CAS NO: | 88546-55-8 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 361.4 |
| Cas No. | 88546-55-8 |
| Formula | C17H19N3O4S |
| Solubility | ≥40.6 mg/mL in DMSO,≥19.9 mg/mL in EtOH,insoluble in H2O |
| Chemical Name | 6-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfonyl]-1H-benzimidazole |
| Canonical SMILES | COC1=CC=C2C(N=C(S(CC3=C(C)C(OC)=C(C)C=N3)(=O)=O)N2)=C1 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
Omeprazole sulfone is the major metabolite of the gastric proton pump inhibitor, omeprazole [1]. The Proton Pump Inhibitor, Omeprazole, is a metabolism-dependent inhibitor of CYP2C19 with a relatively low incidence of adverse events and pharmacokinetic drug-drug interactions (DDIs) [1]. Omeprazole sulfone is produced by cytochrome P450 (CYP)3A4 sulfoxidation of esomeprazole and has been found in plasma [2]. Cytochrome P450 was once believed to be mainly a hepatic drug detoxication system, but is now understood to include a myriad of enzymic reactions implicated in important life processes. Mutations in many CYP genes cause inborn errors of metabolism and lead to many clinically relevant diseases [3].
In vitro: Omeprazole sulfone has been shown to act as a reversible direct-acting and metabolism-dependent inhibitor of CYP2C19 in pooled human liver microsomes with an IC50 of 18 μM [1].
In vivo: Three hours after intake of 20 mg omeprazole only, the geometric mean plasma concentration of omeprazole sulfone were 106 nmol/l in 22 samples from subjects known to be extensive CYP2C19 metabolizers (EM) and 672 nmol/l in the five subjects known to be poor CYP2C19 metabolizers (PM). The mean log10(omeprazole/omeprazole sulfone) ratio was 0.18 [4].
References:
[1] Nebert D W, Russell D W. Clinical importance of the cytochromes P450[J]. The Lancet, 2002, 360(9340): 1155-1162.
[2] bel A, Andersson T B, Antonsson M, et al. Stereoselective metabolism of omeprazole by human cytochrome P450 enzymes[J]. Drug Metabolism and Disposition, 2000, 28(8): 966-972.
[3] Nebert D W, Russell D W. Clinical importance of the cytochromes P450[J]. The Lancet, 2002, 360(9340): 1155-1162.
[4] Bttiger Y. Use of omeprazole sulfone in a single plasma sample as a probe for CYP3A4[J]. European journal of clinical pharmacology, 2006, 62(8): 621-625.
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