Cilomilast-d9

• 常用名: Cilomilast-d9
• 英文名: Cilomilast-d9
• CAS号: 1794779-92-2
• 分子量: 352.47
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₀H₁₆D₉NO₄
• 熔点: N/A
• 闪点: N/A

Cilomilast-d9用途

Cilomilast-d9(SB-207499-d9)是氘标记的Cilomilast。西洛司他(SB-207499)是一种有效、选择性和口服活性的磷酸二酯酶4(PDE4)抑制剂,LPDE4和HPDE4的IC50分别为~100和120nm。Cilomilast显示PDE4对PDE1、PDE2、PDE3和PDE5的选择性(IC50分别为74、65、>100和83µM)。Cilomilast具有抗炎和免疫调节作用,可用于哮喘和慢性阻塞性肺疾病(COPD)的thr研究[1][2][3][4]。

Cilomilast-d9名称

• 英文名: Cilomilast-d9

Cilomilast-d9生物活性

• 描述: Cilomilast-d9(SB-207499-d9)是氘标记的Cilomilast。西洛司他(SB-207499)是一种有效、选择性和口服活性的磷酸二酯酶4(PDE4)抑制剂,LPDE4和HPDE4的IC50分别为~100和120nm。Cilomilast显示PDE4对PDE1、PDE2、PDE3和PDE5的选择性(IC50分别为74、65、>100和83µM)。Cilomilast具有抗炎和免疫调节作用,可用于哮喘和慢性阻塞性肺疾病(COPD)的thr研究[1][2][3][4]。
• 相关类别:
  信号通路 >> 代谢酶/蛋白酶 >> 磷酸二酯酶(PDE)
  研究领域 >> 炎症/免疫
• 体外研究: 氢、碳和其他元素的稳定重同位素已被纳入药物分子,主要作为药物开发过程中定量的示踪剂。氘化因其可能影响药物的药代动力学和代谢特征而受到关注[1]。
• 参考文献:

  [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

  [2]. Griswold DE, et, al. SB 207499 (Ariflo), a second generation phosphodiesterase 4 inhibitor, reduces tumor necrosis factor alpha and interleukin-4 production in vivo. J Pharmacol Exp Ther. 1998 Nov;287(2):705-11.

  [3]. Hatzelmann A, et, al. Anti-inflammatory and immunomodulatory potential of the novel PDE4 inhibitor roflumilast in vitro. J Pharmacol Exp Ther. 2001 Apr;297(1):267-79.

  [4]. Barnette MS, et, al. SB 207499 (Ariflo), a potent and selective second-generation phosphodiesterase 4 inhibitor: in vitro anti-inflammatory actions. J Pharmacol Exp Ther. 1998 Jan;284(1):420-6.

Cilomilast-d9物理化学性质

• 分子式: C₂₀H₁₆D₉NO₄
• 分子量: 352.47
• InChIKey: CFBUZOUXXHZCFB-PAWOCJNQSA-N
• SMILES: COc1ccc(C2(C#N)CCC(C(=O)O)CC2)cc1OC1CCCC1

Cilomilast-d9靶点实验

查看更多实验

实验名称：Inhibition of LPS stimulated TNF-alpha release in mice at 10 mg/kg 来源：ChEMBL 靶标：Mus musculus External Id：CHEMBL719209

实验名称：Primary qHTS assay for inhibitors of alpha-synuclein gene (SNCA) expression 来源：NCGC External Id：SNCA-p-activity-luciferase

实验名称：Inhibition of human PDE4 at 0.075 uM after 20 mins 来源：ChEMBL 靶标：cAMP-specific 3',5'-cyclic phosphodiesterase 4A External Id：CHEMBL999656

实验名称：Percent inhibition of neutrophil activation in BALF from actively sensitized Brown no... 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL795369

实验名称：Quantitative High-Throughput drug screen in 47 multiple myeloma cell lines against th... 来源：NCGC 靶标：N/A External Id：s-my-keats_OPM1-m4-1

实验名称：Quantitative High-Throughput drug screen in 47 multiple myeloma cell lines against th... 来源：NCGC 靶标：N/A External Id：s-my-OC1MY5-m4-1

实验名称：Anti-inflammatory activity against ovalbumin induced lung inflammatory rat model asse... 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL5236729

实验名称：Inhibition of Phosphodiesterase 3 (PDE3) from dog aorta (not tested) 来源：ChEMBL 靶标：cGMP-inhibited 3',5'-cyclic phosphodiesterase B External Id：CHEMBL758789

实验名称：Quantitative High-Throughput drug screen in 47 multiple myeloma cell lines against th... 来源：NCGC 靶标：N/A External Id：s-my-KMS_34-m4-1

实验名称：Quantitative High-Throughput drug screen in 47 multiple myeloma cell lines against th... 来源：NCGC 靶标：N/A External Id：s-my-keats_L363-m4-1

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