货号	规格	价格	上海	北京	珠海	重庆	武汉
S85405-1mg买3赠1	99.30%	￥190.00 S85405-1mg ￥190.00 现货（买3赠1）	5 5	-	-	-	-
S85405-5mg买3赠1	99.30%	￥290.00 S85405-5mg ￥290.00 现货（买3赠1）	4 4	-	-	-	-
S85405-10mg	99.30%	￥350.00 S85405-10mg ￥350.00 现货	7 7	-	-	-	-
S85405-25mg	99.30%	￥470.00 S85405-25mg ￥470.00 现货	6 6	-	-	-	-
S85405-50mg	≥99%	￥830.00 S85405-50mg ￥830.00 2-3天	0 货期：2-3天	-	-	-	-
S85405-100mg	≥99%	￥1600.00 S85405-100mg ￥1600.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

CP671305 is a potent, orally active, selective inhibitor of phosphodiesterase-4-D, and possesses high activities.

靶点：

PDE

体外研究：

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

体内研究：

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)

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.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.201 ml	11.003 ml	22.007 ml
5 mM	0.44 ml	2.201 ml	4.401 ml
10 mM	0.22 ml	1.1 ml	2.201 ml
50 mM	0.044 ml	0.22 ml	0.44 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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