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CP671305

目录号: PL09715 纯度: ≥99%

CP671305 是一种有效的，可口服的，选择性的 phosphodiesterase-4-D 抑制剂，具有很高的活性。

CAS No. :445295-04-5

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中文名称	CP671305
中文别名	CP671305
英文名称	CP671305
英文别名	CP671305;CP-671305
Cas No.	445295-04-5
分子式	C₂₃H₁₉FN₂O₇
分子量	454.40
包装储存	Powder -20°C 3 years；4°C 2 years
详情描述	CP671305 是一种有效的，可口服的，选择性的 phosphodiesterase-4-D 抑制剂，具有很高的活性。

产品详情	CP671305 是一种有效的，可口服的，选择性的 phosphodiesterase-4-D 抑制剂，具有很高的活性。
生物活性	CP671305 is a potent, orally active, selective inhibitor of phosphodiesterase-4-D, and possesses high activities.
性状	Solid
体外研究(In Vitro)	CP-671,305 is identified as a substrate of MRP2 and BCRP, but not MDR1. CP-671,305 is a substrate of human OATP2B1 with a high affinity (Km=4 μM) but not a substrate for human OATP1B1 or OATP1B3. CP-671,305 displays high affinity (Km=12 μM) for rat hepatic Oatp1a4. CP-671,305 does not exhibit competitive inhibition of the five major cytochrome P450 enzymes, namely CYP1A2, 2C9, 2C19, 2D6 and 3A4 (IC50s >?50 μM). Likewise, no time-dependent inactivation of the five major cytochrome P450 enzymes is discernible with CP-671,305. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	CP-671,305 pharmacokinetics are largely unaltered, and compromised biliary clearance of CP-671,305 is compensated by increased urinary clearance. CP-671,305 demonstrates generally favourable pharmacokinetic properties, systemic plasma clearance after intravenous administration is low in Sprague-Dawley rats (9.60?±?1.16?mL/min/kg), beagle dogs (2.90?±?0.81?mL/min/kg) and cynomolgus monkeys (2.94?±?0.87?mL/min/kg) resulting in plasma half-lives >?5?h. Moderate to high bioavailability in rats (43-80%), dogs (45%) and monkeys (26%) is observed after oral dosing. In rats, oral pharmacokinetics are dose dependent over the dose range studied (10 and 25?mg/kg). 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]. Kalgutkar AS, et al. Role of transporters in the disposition of the selective phosphodiesterase-4 inhibitor (+)-2-[4-({[2-(benzo[1,3]dioxol-5-yloxy)-pyridine-3-carbonyl]-amino}-methyl)-3-fluoro-phenoxy]-propionic acid in rat and human. Drug Metab Dispos. 2007 Nov;35(11):2111-8. Epub 2007 Aug 8. [2]. Kalgutkar AS, et al. Disposition of CP-671, 305, a selective phosphodiesterase 4 inhibitor in preclinical species. Xenobiotica. 2004 Aug;34(8):755-70.

溶解度数据	In Vitro: DMSO : 100 mg/mL (220.07 mM; Need ultrasonic)配制储备液

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[1]. Kalgutkar AS, et al. Role of transporters in the disposition of the selective phosphodiesterase-4 inhibitor (+)-2-[4-({[2-(benzo[1,3]dioxol-5-yloxy)-pyridine-3-carbonyl]-amino}-methyl)-3-fluoro-phenoxy]-propionic acid in rat and human. Drug Metab Dispos. 2007 Nov;35(11):2111-8. Epub 2007 Aug 8.
[2]. Kalgutkar AS, et al. Disposition of CP-671, 305, a selective phosphodiesterase 4 inhibitor in preclinical species. Xenobiotica. 2004 Aug;34(8):755-70.

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。

CP671305

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