RO0270608

• 常用名: RO0270608
• 英文名: RO0270608
• CAS号: 220846-33-3
• 分子量: 505.77800
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₄H₁₉Cl₃N₂O₄
• 熔点: N/A
• 闪点: N/A

RO0270608用途

R411的活性代谢产物RO0270608是一种双α4beta1-α4beta7(α4β1/α4β7)整合素拮抗剂。抗炎活性[1][2]。

RO0270608名称

• 英文名: Ro 0270608

RO0270608生物活性

• 描述: R411的活性代谢产物RO0270608是一种双α4beta1-α4beta7(α4β1/α4β7)整合素拮抗剂。抗炎活性[1][2]。
• 相关类别:
  研究领域 >> 炎症/免疫
  信号通路 >> 细胞骨架 >> Integrin
• 靶点实验:

  α4β1

  α4β7

• 体外研究: RO0270608抑制α4/β7介导的细胞粘附,IC50为33 nM。在人类T细胞VCAM/抗CD3共刺激试验中,RO0270608可显著抑制T细胞增殖(IC50=30 nM)[2]。
• 体内研究: 在小鼠OVA气道炎症模型中,RO0270608 i.n.消除了过敏原诱导的炎症细胞积聚[2]
• 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):1368-1378.

  [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.

RO0270608物理化学性质

• 分子式: C₂₄H₁₉Cl₃N₂O₄
• 分子量: 505.77800
• 精确质量: 504.04100
• PSA: 95.50000
• LogP: 6.09710
• InChIKey: JTVWJXUGGJTGDA-IBGZPJMESA-N
• SMILES: Cc1cccc(Cl)c1C(=O)NC(Cc1ccc(NC(=O)c2c(Cl)cccc2Cl)cc1)C(=O)O

RO0270608靶点实验

查看更多实验

实验名称：Inhibition of human VCAM1 binding to integrin alpha4beta1 receptor in human Ramos cel... 来源：ChEMBL 靶标：Integrin alpha-4 External Id：CHEMBL2346015

实验名称：Inhibition of human MAdCAM1 binding to integrin alpha4beta7 receptor in human RPMI 88... 来源：ChEMBL 靶标：Integrin alpha-4 External Id：CHEMBL2346014

实验名称：Antagonist activity at recombinant integrin alpha2 beta1 receptor (unknown origin) as... 来源：ChEMBL 靶标：Integrin alpha-2 External Id：CHEMBL3116955

实验名称：Inhibitory binding concentration against VCAM/VLA-4 in ELISA. 来源：ChEMBL 靶标：Integrin alpha-4 External Id：CHEMBL819216

实验名称：Inhibition of human VCAM1 binding to integrin alpha4beta1 receptor in human Ramos cel... 来源：ChEMBL 靶标：Integrin alpha-4 External Id：CHEMBL2339235

实验名称：Inhibition of human MAdCAM1 binding to integrin alpha4beta7 receptor in human RPMI 88... 来源：ChEMBL 靶标：Integrin alpha-4 External Id：CHEMBL2339234

实验名称：Inhibitory binding concentration against VCAM/VLA-4 in Ramos. 来源：ChEMBL 靶标：Integrin alpha-4 External Id：CHEMBL818391

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RO0270608英文别名

• (S)-2-(2-Chloro-6-methyl-benzoylamino)-3-[4-(2,6-dichloro-benzoylamino)-phenyl]-propionic acid
• 4-[[(2,6-dichlorophenyl)carbonyl]amino]-N-[(2-chloro-6-methylphenyl)carbonyl]-L-phenylalanine
• (S)-2-(2-chloro-6-methyl-benzoylamino)-3-[4-(2,6-dichloro-benzoylamino)-phenyl]-propionic acid
• N-(2-chloro-6-methylbenzoyl)-4-[(2,6-dichlorobenzoyl)amino]-L-phenylalanine