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  • 化合物 CP671305|T4695|TargetMol

化合物 CP671305|T4695|TargetMol

CP671305
445295-04-5
￥683 1mg 起订
￥1660 5mg 起订
￥2490 10mg 起订
上海 更新日期：2024-12-12

TargetMol中国（陶术生物）

VIP3年
联系人：邵小姐
手机：4008200310 拨打
邮箱：marketing@tsbiochem.com

产品详情:

中文名称：
化合物 CP671305
英文名称：
CP671305
CAS号：
445295-04-5
品牌：
TargetMol
产地：
美国
保存条件：
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
纯度规格：
99.22%
产品类别：
抑制剂
货号：
T4695

Product Introduction

Bioactivity

名称CP671305
描述CP671305 is an orally active, potent and selective inhibitor of phosphodiesterase-4-D.
动物实验Jugular vein cannulated and bile duct-exteriorized male Sprague-Dawley rats (230-250 g) are used in the assay. All animals are fasted overnight before dosing, whereas access to water is provided ad libitum. Animals are fed following collection of the 2-h blood samples. CP-671,305 (3 mg/kg) in glycerol formal is administered intravenously (i.v.) via the jugular vein to three rats over 30 s, and serial plasma samples are collected before dosing and 0.033, 0.15, 0.5, 1, 2, 4, 6, 8, and 24 h after dosing. All plasma samples are kept frozen until analysis. In addition, an i.v. dose of 3 mg/kg is also given to bile duct-exteriorized rats (n=3), where plasma, bile, and urine samples are collected on ice for up to 24 h and stored at -20°C until analysis. For the DDI studies, cyclosporin A (20 mg/kg in glycerol formal) is administered i.v. 30 min before intravenous administration of CP-671,305. Rifampicin (50 mg/kg) in saline is administered i.v. 5 min before the administration of CP-671,305. Plasma samples from the various pharmacokinetic studies are generated by centrifugation at 3000 rpm for 10 min at 4°C. Samples are stored at -20°C, pending analysis by LC-MS/MS.
体外活性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 is identified as a substrate of MRP2 and BCRP, but not MDR1. 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.
体内活性The pharmacokinetics of CP-671,305 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).
存储条件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度DMSO : > 150 mg/mL (330.11 mM)
关键字Inhibitor | CP 671305 | Phosphodiesterase (PDE) | CP671305 | inhibit | CP-671305
相关产品Icariin | Vardenafil hydrochloride | Apremilast | Indomethacin | Roflumilast | Sildenafil citrate | Theophylline | Acefylline | Theobromine | Theophylline monohydrate | Isoprenaline hydrochloride | Doxofylline
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CP671305|TargetMol

公司简介

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。 凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

成立日期 (12年)
注册资本 566.265100万人民币
员工人数 100-500人
年营业额 ￥ 1亿以上
经营模式 贸易,工厂,试剂,定制,服务
主营行业 天然产物,生化试剂,分子生物学,分子砌块,生物技术服务

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