INCB8761(PF-4136309)
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- CAS号:
- 1341224-83-6
- 英文名:
- INCB8761(PF-4136309)
- 英文别名:
- CS-1440;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);INCB8761; PF-4136309; PF4136309; PF 4136309; INCB-8761;INCB-8761,INCB 8761,inhibit,PF-4136309,CC chemokine receptor,CCR,Inhibitor,PF4136309;N-(2-((S)-3-((trans-4-hydroxy-4-(5-(pyrimidin-2-yl)pyridin-2-yl)cyclohexyl)amino)pyrrolidin-1-yl)-2-oxoethyl)-3-(trifluoromethyl)benzamide
- 中文名:
- INCB8761(PF-4136309)
- 中文别名:
- 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
- CBNumber:
- CB62627975
- 分子式:
- C29H31F3N6O3
- 分子量:
- 568.59
- MOL File:
- 1341224-83-6.mol
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INCB8761(PF-4136309)化学性质
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沸点:
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712.2±60.0 °C(Predicted)
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密度:
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1.40±0.1 g/cm3(Predicted)
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储存条件:
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Keep in dark place,Inert atmosphere,Store in freezer, under -20°C
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溶解度:
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Soluble in DMSO (up to at least 25 mg/ml)
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形态:
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solid
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酸度系数(pKa):
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13.17±0.46(Predicted)
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颜色:
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Off-white
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稳定性:
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Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
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INCB8761(PF-4136309)性质、用途与生产工艺
PF-4136309 是一种高效，选择性，可口服的 CCR2 拮抗剂，能够抑制人，小鼠和大鼠 CCR2，IC50 值分别为 5.2 nM，17 nM 和 13 nM。
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Human CCR2
5.2 nM (IC
50
)
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Mouse CCR2
13 nM (IC
50
)
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Rat CCR2
17 nM (IC
50
)
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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.
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.
INCB8761(PF-4136309)
上下游产品信息
上游原料
下游产品
INCB8761(PF-4136309)
生产厂家
1341224-83-6, INCB8761(PF-4136309) 相关搜索:
- 精细化工产品
- 生物活性分子-API
- G蛋白偶联受体&G蛋白
- 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
- 化合物PF4136309
- 1341224-83-6
- INCB-8761,INCB 8761,inhibit,PF-4136309,CC chemokine receptor,CCR,Inhibitor,PF4136309
- N-(2-((S)-3-((trans-4-hydroxy-4-(5-(pyrimidin-2-yl)pyridin-2-yl)cyclohexyl)amino)pyrrolidin-1-yl)-2-oxoethyl)-3-(trifluoromethyl)benzamide
- INCB8761; PF-4136309; PF4136309; PF 4136309; INCB-8761
- CS-1440
- N-(2-((S)-3-(((1R,4S)-4-HYDROXY-4-(5-(PYRIMIDIN-2-YL)
- ZNSVOHSYDRPBGI-LXWOLXCRSA-N
- 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
- EOS-61910
- Benzamide, N-[2-[(3S)-3-[[trans-4-hydroxy-4-[5-(2-pyrimidinyl)-2-pyridinyl]cyclohexyl]amino]-1-pyrrolidinyl]-2-oxoethyl]-3-(trifluoromethyl)-
- PF-04136309(INCB-8761)
- NCB8761(PF-4136309)
- INCB8761(PF-4136309)