化合物PF4136309_化工百科

中文名	INCB8761(PF-4136309)
英文名	INCB8761(PF-4136309)
别名	化合物PF4136309 N-(2-((S)-3-((TRANS-4-反式-4-羟基-4-(5-(嘧啶-2-基)吡啶-2-基)环己基)氨基)吡咯烷-1-基)-2-OXOETHYL)-3-(三氟甲基)苯甲酰胺
英文别名	EOS-61910 NCB8761(PF-4136309) INCB8761(PF-4136309) PF-04136309(INCB-8761) ZNSVOHSYDRPBGI-LXWOLXCRSA-N N-(2-((S)-3-(((1R,4S)-4-HYDROXY-4-(5-(PYRIMIDIN-2-YL) N-(2-((S)-3-(((1r,4S)-4-hydroxy-4-(5-(pyrimidin-2-yl) yridine-2-yl)cyclohexyl)amino)pyrrolidin-1-yl)-2-oxoethyl)-3-(trifluoromethyl)benzamide Benzamide, N-[2-[(3S)-3-[[trans-4-hydroxy-4-[5-(2-pyrimidinyl)-2-pyridinyl]cyclohexyl]amino]-1-pyrrolidinyl]-2-oxoethyl]-3-(trifluoromethyl)-
CAS	1341224-83-6
化学式	C29H31F3N6O3
分子量	568.59
密度	1.40±0.1 g/cm3(Predicted)
沸点	712.2±60.0 °C(Predicted)
溶解度	溶于DMSO (至少25 mg/ml)
酸度系数	13.17±0.46(Predicted)
存储条件	Keep in dark place,Inert atmosphere,Store in freezer, under -20°C
稳定性	从提供的购买之日起稳定1年。DMSO中的溶液可以在-20 °C下储存长达3个月。
外观	固体
颜色	Off-white
体外研究	PF-4136309 is potent in human chemotaxis activity (IC 50 =3.9 nM) and in the whole blood assay (IC 50 =19 nM), with IC 50 of 16 and 2.8 nM in mouse and rat chemotaxis assays. PF-4136309 is potent in inhibiting CCR2 mediated signaling events such as intracellular calcium mobilization and ERK (extracellular signal-regulated kinase) phosphorylation with IC 50 values of 3.3 and 0.5 nM, respectively. In hERG patch clamp assay, PF-4136309 inhibits hERG potassium current with an IC 50 of 20 μM. PF-4136309 is not a cytochrome P450 (CYP) inhibitor, with IC 50 values of >30 μM against five major CYP isozymes CYP1A2, CYP2C9, CYP2C19, CYP2D6, and CYP3A4. Moreover, PF-4136309 is not a CYP inducer at concentrations up to 30 μM.
体内研究	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 (T max ) 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.
上游原料	8-(5-溴-2-吡啶基)-8-羟基-1,4-二氧杂螺[4.5]癸烷 (S)-N-(2-(3-氨基吡咯烷-1-基)-2-氧代乙基)-3-(三氟甲基)苯甲酰胺盐酸盐 1,4-环己二酮单乙二醇缩酮

化合物PF4136309 - 配置溶液浓度参考

	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
5 mM	0.035 ml	0.176 ml	0.352 ml

最后更新：2024-01-02 23:10:35

北京索莱宝科技有限公司

提供多种规格现货供应

产品名: N-(2-((S)-3-((trans-4-反式-4-羟基-4-(5-(嘧啶-2-基)吡啶-2-基)环己基)氨基)吡咯烷-1-基)-2-oxoethyl)-3-(三氟甲基)苯甲酰胺去供应商网站查看询盘
CAS: 1341224-83-6
产地: 北京
包装: 瓶
规格: YS151519-100mg,YS151519-1g,YS151519-50mg,YS151519-250mg,YS151519-10mg,YS151519-25mg
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上海吉至生化科技有限公司

现货供应

产品名: PF-4136309 去供应商网站查看询盘
CAS: 1341224-83-6
产地: 中国上海
包装: 50mg
规格: 99%
价格: 7998.00
库存: 现货
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产品描述: 中文名：PF-4136309 英文名:PF-4136309 CAS:1341224-83-6 规格:99% 产地:中国上海

上海麦克林生化科技股份有限公司

现货供应

产品名: PF-4136309 去供应商网站查看询盘
CAS: 1341224-83-6
产地: 上海
规格: P883130
价格: 100mg-2000,25mg-888,10mg-485,5mg-329
库存: 15天内发货
电话: 13816333479/13918391375
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上海源叶生物科技有限公司

产品名: INCB8761(PF-4136309) 去供应商网站查看询盘
CAS: 1341224-83-6
产地: 上海
规格: 99%
价格: 1mg 300,2mg 500,5mg 800,10mg 1050,25mg 1950,50mg 2950,100mg 4400
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