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JNJ-54175446
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
JNJ-54175446图片
CAS NO:1627902-21-9
规格:≥98%
包装与价格:
包装价格(元)
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议

产品介绍
理化性质和储存条件


Name: JNJ-54175446
CAS#: 1627902-21-9
Chemical Formula: C18H13ClF4N6O
Exact Mass: 440.0775
Molecular Weight: 440.7866
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Technical InformationSynonym: JNJ54175446; JNJ 54175446; JNJ-54175446
Chemical Name: (R)-(2-chloro-3-(trifluoromethyl)phenyl)(1-(5-fluoropyrimidin-2-yl)-4-methyl-1,4,6,7-tetrahydro-5H-[1,2,3]triazolo[4,5-c]pyridin-5-yl)methanone
InChi Key: CWFVVQFVGMFTBD-SECBINFHSA-N
InChi Code: InChI=1S/C18H13ClF4N6O/c1-9-15-13(29(27-26-15)17-24-7-10(20)8-25-17)5-6-28(9)16(30)11-3-2-4-12(14(11)19)18(21,22)23/h2-4,7-9H,5-6H2,1H3/t9-/m1/s1
SMILES Code: ClC1=C(C(F)(F)F)C=CC=C1C(N(CC2)[C@H](C)C(N=N3)=C2N3C4=NC=C(C=N4)F)=O
实验参考方法
Target

pIC50: 8.46 (hP2X7 receptor), 8.81 (rP2X7 receptor)[1]

In VitroJNJ-54175446 (Compound 14) is a potent and selective brain penetrant P2X7 antagonist, with pIC50s of 8.46 and 8.81 for hP2X7 and rP2X7, respectively. JNJ-54175446 shows less potent activity against mouse, dog and Macaque P2X7 (pIC50, 7.8, 7.9 and 8.1, respectively)[1].
In VivoJNJ-54175446 shows dose-dependent occupancy with the ED50 of 0.46 mg/kg, corresponding to plasma EC50 of 105 ng/mL[1].
References

[1].4-Methyl-6,7-dihydro-4H-triazolo[4,5-c]pyridine-Based P2X7 Receptor Antagonists: Optimization of Pharmacokinetic Properties Leading to the Identification of a Clinical Candidate.