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CI-1044

(Synonyms: PD-189659)

目录号: PL01043 纯度: ≥98%

CI-1044 是一种口服有效的 PDE4 抑制剂，对 PDE4A5，PDE4B2，PDE4C2 和 PDE4D3 的 IC50 值分别为 0.29, 0.08, 0.56, 0.09 μM。

CAS No. :197894-84-1

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中文名称	CI-1044
中文别名	化合物 T14962
英文名称	CI-1044
英文别名	PD-189659;CI-1044;N-[9-Amino-4-oxo-1-phenyl-3,4,6,7-tetrahydropyrrolo[3,2,1-jk][1,4]benzodiazepin- 3(R)-yl]pyridine-3-carboxamide;CI-1044 (CI1044);3-Pyridinecarboxamide, N-[(3R)-9-amino-3,4,6,7-tetrahydro-4-oxo-1-phenylpyrrolo[3,2,1-jk][1,4]benzodiazepin-3-yl]-
Cas No.	197894-84-1
分子式	C₂₃H₁₉N₅O₂
分子量	397.43
包装储存	Powder -20°C 3 years；4°C 2 years
详情描述	CI-1044 是一种口服有效的 PDE4 抑制剂，对 PDE4A5，PDE4B2，PDE4C2 和 PDE4D3 的 IC₅₀ 值分别为 0.29, 0.08, 0.56, 0.09 μM。

产品详情	CI-1044 是一种口服有效的 PDE4 抑制剂，对 PDE4A5，PDE4B2，PDE4C2 和 PDE4D3 的 IC₅₀ 值分别为 0.29, 0.08, 0.56, 0.09 μM。
生物活性	CI-1044 is an orally active PDE4 inhibitor with IC 50 s of 0.29, 0.08, 0.56, 0.09 μM for PDE4A5, PDE4B2, PDE4C2 and PDE4D3, respectively.
性状	Solid
IC50 & Target[1][2]	PDE4A5 0.29 μM (IC50) PDE4B2 0.08 μM (IC
体外研究(In Vitro)	CI-1044 is an orally active PDE4 inhibitor with IC50s of 0.29, 0.08, 0.56, 0.09 μM for PDE4A5, PDE4B2, PDE4C2 and PDE4D3, respectively. CI-1044 selectively inhibits PDE4 crude extract from U937 cells with an IC50 value of 0.27±0.02 μM being threefold more potent than rolipram (IC50=0.91±0.14) and tenfold less potent than cilomilast (IC50=0.026±0.007) in the same assay. In the presence of PDE4 inhibitors, the production of TNF-α is dose dependently decreased with mean IC50 values from three separate experiments of 0.31±0.05, 0.26±0.05 and 0.11±0.01 μM, for CI-1044, cilomilast and rolipram, respectively. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	TNF-α production is dose-dependently inhibited by CI-1044, rolipram and cilomilast with ID 50 s of 0.4, 1.4 and 1.6 mg/kg respectively following single oral administration. Following repeated administration with CI-1044, the ID 50 value represents 0.5 mg/kg p.o.. CI-1044 plasma levels increase proportionally with doses ranging between 0.1 and 40 mg/kg p.o. (R2=0.878). CI-1044 dose dependently inhibits the accumulation of eosinophils in Bronchoalveolar lavages (BAL) fluids with an ID 50 value of 3.25 mg/kg. A single dose treatment with CI-1044 (10 mg/kg, p.o.) 24, 8, 3 or 1 h before the antigen challenge induces 6, 56, 48 and 79% inhibition in the number of eosinophils in BAL. 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]. Pruniaux MP, et al. Relationship between phosphodiesterase type 4 inhibition and anti-inflammatory activity of CI-1044 in rat airways. Fundam Clin Pharmacol. 2010 Feb;24(1):73-82.

溶解度数据	In Vitro: DMSO : 125 mg/mL (314.52 mM; Need ultrasonic)配制储备液

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[1]. Pruniaux MP, et al. Relationship between phosphodiesterase type 4 inhibition and anti-inflammatory activity of CI-1044 in rat airways. Fundam Clin Pharmacol. 2010 Feb;24(1):73-82.

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。

CI-1044

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