NCB8761(PF-4136309)
INCB8761(PF-4136309)
CAS: 1341224-83-6
Molecular Formula: C29H31F3N6O3
NCB8761(PF-4136309) - Names and Identifiers
NCB8761(PF-4136309) - Physico-chemical Properties
| Molecular Formula | C29H31F3N6O3 |
| Molar Mass | 568.59 |
| Density | 1.40±0.1 g/cm3(Predicted) |
| Boling Point | 712.2±60.0 °C(Predicted) |
| Solubility | Soluble in DMSO (up to at least 25 mg/ml) |
| Appearance | solid |
| Color | Off-white |
| pKa | 13.17±0.46(Predicted) |
| Storage Condition | Keep in dark place,Inert atmosphere,Store in freezer, under -20°C |
| Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
| In vitro study | 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. |
| In vivo study | 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. |
NCB8761(PF-4136309) - Preparation solution concentration reference
| 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 |
Last Update：2024-01-02 23:10:35
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CAS: 1341224-83-6
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CAS: 1341224-83-6
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Product Name: INCB8761(PF-4136309) Visit Supplier Webpage Request for quotation
CAS: 1341224-83-6
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 1341224-83-6
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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