JNJ-54175446|1627902-21-9|-陌孚医药/Medlife

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JNJ-54175446

目录号: PL08674 纯度: ≥99%

CAS No. :1627902-21-9

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中文名称	JNJ-54175446
英文名称	JNJ-54175446
英文别名	32524GLF40;(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;CWFVVQFVGMFTBD-SECBINFHSA-N;BDBM254266;SB18846;US9464084, 158;Methanone, (2-chloro-3-(trifluoromethyl)phenyl)((4R)-1-(5-fluoro-2-pyrimidinyl)-1,4,6,7-tetrahydro-4-methyl-5H-1,2,3-triazolo(4,5-C)pyridin-5-yl)-;(R)-(2-chloro-3-(trif;[2-Chloro-3-(trifluoromethyl)phenyl]-[(4R)-1-(5-fluoropyrimidin-2-yl)-4-methyl-6,7-dihydro-4H-triazolo[4,5-c]pyridin-5-yl]methanone;JNJ-54175446
Cas No.	1627902-21-9
分子式	C₁₈H₁₃ClF₄N₆O
分子量	440.78
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

JNJ-54175446 是一种有效、选择性、可透过血脑屏障的 P2X7 受体拮抗剂，对人和大鼠的 P2X7 受体的 pIC₅₀ 值分别为 8.46 和 8.81。

生物活性

JNJ-54175446 is a potent and selective brain penetrant P2X7 receptor antagonist, with pIC 50 s of 8.46 and 8.81 for hP2X7 receptor and rP2X7 receptor, respectively.

性状

Solid

IC50 & Target[1][2]

pIC50: 8.46 (hP2X7 receptor), 8.81 (rP2X7 receptor)

体外研究(In Vitro)

JNJ-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). has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

JNJ-54175446 shows dose-dependent occupancy with the ED 50 of 0.46 mg/kg, corresponding to plasma EC 50 of 105 ng/mL. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[1]. Letavic MA, et al. 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. Send to

溶解度数据	In Vitro: DMSO : 62.5 mg/mL (141.79 mM; Need ultrasonic)配制储备液

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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