| 中文名称 |
RO0270608
|
| 英文名称 |
RO0270608
|
| 英文别名 |
L-Phenylalanine,N-(2-chloro-6-methylbenzoyl)-4-[(2,6-dichlorobenzoyl)amino]-;RO0270608
|
| Cas No. |
220846-33-3
|
| 分子式 |
C24H19N2O4Cl3
|
| 分子量 |
505.78
|
| 包装储存 |
Powder -20°C 3 years;4°C 2 years
|
| 详情描述 |
RO0270608,是 R411 的活性代谢物,是一种双重 alpha4beta1-alpha4beta7 (α4β1/α4β7) 整合素拮抗剂。具有抗炎活性。
|
| 产品详情 |
RO0270608,是 R411 的活性代谢物,是一种双重 alpha4beta1-alpha4beta7 (α4β1/α4β7) 整合素拮抗剂。具有抗炎活性。
|
| 生物活性 |
RO0270608, the active metabolite of R411, is a dual alpha4beta1-alpha4beta7 (α4β1/α4β7) integrin antagonist. Antiinflammatory activity.
|
| 性状 |
Solid
|
| IC50 & Target[1][2] |
α4β1 α4β7
|
| 体外研究(In Vitro) |
RO0270608 inhibits α4/β7 mediated cell adhesion with an IC50 of 33 nM. In a human T-cell VCAM/anti CD3 costimulation assay RO0270608 causes a pronounced inhibition of T-cell proliferation (IC50=30 nM). has not independently confirmed the accuracy of these methods. They are for reference only.
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| 体内研究(In Vivo) |
In a murine OVA-model of airway inflammation, RO0270608 i.n. abolishes allergen-induced inflammatory cell accumulation has not independently confirmed the accuracy of these methods. They are for reference only.
|
| 运输条件 |
Room temperature in continental US; may vary elsewhere.
|
| 储存方式 |
Powder -20°C 3 years;4°C 2 years
|
| 参考文献 |
[1]. Hijazi Y, et al. Pharmacokinetics, safety, and tolerability of R411, a dual alpha4beta1-alpha4beta7 integrin antagonist after oral administration at single and multiple once-daily ascending doses in healthy volunteers. J Clin Pharmacol. 2004;44(12):1368-1[2]. M. Renzetti, et al. Dual α4/β1–α4/β7 vs α4/β1 selective antagonism is required for attenuation of allergic inflammatory responses. Journal of Allergy and Clinical Immunology. Volume 113, Issue 2, Supplement, February 2004, Page S221.
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| 溶解度数据 |
In Vitro: DMSO : 12.5 mg/mL (24.71 mM; ultrasonic and warming and heat to 60°C)配制储备液
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[1]. Hijazi Y, et al. Pharmacokinetics, safety, and tolerability of R411, a dual alpha4beta1-alpha4beta7 integrin antagonist after oral administration at single and multiple once-daily ascending doses in healthy volunteers. J Clin Pharmacol. 2004;44(12):1368-1[2]. M. Renzetti, et al. Dual α4/β1–α4/β7 vs α4/β1 selective antagonism is required for attenuation of allergic inflammatory responses. Journal of Allergy and Clinical Immunology. Volume 113, Issue 2, Supplement, February 2004, Page S221.
1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。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。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。
2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。