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Submit ReviewSSR 69071
说明： Potent, orally active human leukocyte elastase inhibitor
化学名： 2-[[6-Methoxy-4-(1-methylethyl)-1,1-dioxido-3-oxo-1,2-benzisothiazol-2(3H)-yl]methoxy]-9-[2-(1-piperidinyl)ethoxy]-4H-pyrido[1,2-a]pyrimidin-4-one
纯度： ≥98% (HPLC)
生物活性 for SSR 69071
SSR 69071 is a high affinity, potent inhibitor of human leukocyte elastase (HLE) (IC50 = 3.9 nM). Displays species-selectivity (Ki values are 0.017, 1.70, 3.01, 58 and > 100 nM for human, mouse, rat, rabbit and porcine elastase respectively). Inhibits HLE-induced lung hemorrhage in mice (ID50 = 2.8 mg/kg) and reduces infarct size in an in vivo acute model of coronary ischemia-reperfusion injury. Orally active.
化合物库 for SSR 69071
SSR 69071 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for SSR 69071
| 分子量 | 556.63 |
| 公式 | C27H32N4O7S |
| 储存 | Store at +4°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 344930-95-6 |
| PubChem ID | 9872438 |
| InChI Key | DRZXDZYWZSKFDL-UHFFFAOYSA-N |
| Smiles | COC1=CC(C(C)C)=C2C(=O)N(COC3=CC(=O)N4C=CC=C(OCCN5CCCCC5)C4=N3)S(=O)(=O)C2=C1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for SSR 69071
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| ethanol | 5.57 | 10 | |
| DMSO | 13.92 | 25 |
制备储备液 for SSR 69071
以下数据基于产品分子量 556.63。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.25 mM | 7.19 mL | 35.93 mL | 71.86 mL |
| 1.25 mM | 1.44 mL | 7.19 mL | 14.37 mL |
| 2.5 mM | 0.72 mL | 3.59 mL | 7.19 mL |
| 12.5 mM | 0.14 mL | 0.72 mL | 1.44 mL |
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产品说明书 for SSR 69071
参考文献 for SSR 69071
参考文献是支持产品生物活性的出版物。
Bidouard et al (2003) SSR69071, an elastase inhibitor, reduces myocardial infarct size following ischemia-reperfusion injury. Eur.J.Pharmacol. 461 49 PMID: 12568915
Varga et al (2003) A novel orally active inhibitor of HLE. Eur.J.Med.Chem. 38 421 PMID: 12750030
Kapui et al (2003) Biochemical and pharmacological characterization of 2-(9-(2-Piperidinoethoxy)-4-oxo-4H-pyrido[1,2-α]pyrimidin-2-yloxymethyl)-4-(1-methylethyl)-6-methoxy-1,2-benzisothiazol-3(2H)-one-1,1-dioxide (SSR69071), a novel, orally active ela J.Pharmacol.Exp.Ther. 305 451 PMID: 12606659
If you know of a relevant reference for SSR 69071, please let us know.
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关键词: SSR 69071, SSR 69071 supplier, Potent, orally, active, human, leukocyte, elastase, inhibitors, inhibits, Neutrophil, Proteinases, Proteases, SSR69071, HLE, inhibitor, Elastase, 2506, Tocris Bioscience
3 篇 SSR 69071 的引用文献
引用文献是使用了 Tocris 产品的出版物。 SSR 69071 的部分引用包括：
Hoffmann et al (2011) Pivotal role for alpha1-antichymotrypsin in skin repair. J Biol Chem 286 28889 PMID: 21693707
Reardon et al (2011) Thymic stromal lymphopoetin-induced expression of the endogenous inhibitory enzyme SLPI mediates recovery from colonic inflammation. Immunity 35 223 PMID: 21820333
Li et al (2013) Solar ultraviolet irradiation induces decorin degradation in human skin likely via neutrophil elastase. PLoS One 8 e72563 PMID: 24023624
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