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產品描述： PF-4136309 is a potent, selective, and orally bioavailable CCR2 antagonist, with IC50s of 5.2 nM, 17 nM and 13 nM for human, mouse and rat CCR2. |
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靶點：
Human CCR2:5.2 nM (IC50);Mouse CCR2:13 nM (IC50);Rat CCR2:17 nM (IC50);CCR |
體內研究：
PF-4136309 (2 mg/kg) exhibits a moderate half-life in both species after iv administration (2.5 and 2.4 h). When administered orally, PF-4136309 (10 mg/kg) is absorbed rapidly, with peak concentration time (Tmax) at 1.2 h for rats and 0.25 h for dogs. A similar half-life is observed in both species between iv dosing and po dosing. PF-4136309 is well absorbed, with an oral bioavailability of 78% in both species |
參考文獻：
1. Xue CB, et al. Discovery of INCB8761/PF-4136309, a Potent, Selective, and Orally Bioavailable CCR2 Antagonist. ACS Med. Chem. Lett., 2011, 2 (12), pp 913-918. |
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溶解性：
Soluble in DMSO、Ethanol |
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保存條件：
-20℃ |
配置溶液濃度參考：
|
1mg |
5mg |
10mg |
| 1 mM |
1.759 ml |
8.794 ml |
17.587 ml |
| 5 mM |
0.352 ml |
1.759 ml |
3.517 ml |
| 10 mM |
0.176 ml |
0.879 ml |
1.759 ml |
| 50 mM |
0.035 ml |
0.176 ml |
0.352 ml |
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| 注意： |
部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。 |
上海工商
危險品化學品經營許可證（不帶存儲）
營業執照(三證合一)
北京