2. Membrane Transporter/Ion Channel
  3. P2X Receptor
  4. JNJ-54166060

JNJ-54166060 是一种 P2X7 受体 (P2X7 receptor) 拮抗剂，对人/大鼠/小鼠 P2X7 受体作用的 IC50 值分别为 4/115/72 nM。

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JNJ-54166060 Chemical Structure

JNJ-54166060 Chemical Structure

CAS No. : 1627900-41-7

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JNJ-54166060 相关抗体

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P2X1 Receptor P2X2 Receptor P2X3 Receptor P2X4 Receptor P2X7 Receptor

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

JNJ-54166060 is a potent and selective P2X7 receptor antagonist, with IC50s of 4/115/72 nM for human/rat/mouse P2X7 receptor, respectively[1].

IC50 & Target

IC50: 4/115/72 nM (human/rat/mouse P2X7 receptor)[1]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 IC50
> 10 μM
Compound: 1; JNJ 54166060
Displacement of [3H]astemizole from human ERG expressed in HEK293 cells by competitive binding assay
Displacement of [3H]astemizole from human ERG expressed in HEK293 cells by competitive binding assay
[PMID: 27548392]
体内研究
(In Vivo)

JNJ-54166060 exhibits high oral bioavailability (rat 55%, dog >100%, monkey 54 %) and Cmax (rat 375, dog 1249, monkey 389 ng/mL) following oral administration (rat 5 and, dog 5 mg/kg, monkey 5 mg/kg)[1].
JNJ-54166060 exhibits terminal elimination half-lives (rat 1.7 and, dog 11.9 h, monkey 4.2 h) due to low-moderate clearance (30, 5.5, and 14 mL/min/kg respectively) following intravenous administration (rat 1.0 and, dog 1.0 mg/kg, monkey 1.0 mg/kg)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Sprague-Dawley rats[1]
Dosage: 1 mg/kg for i.v.; 5 mg/kg for oral (Pharmacokinetic Analysis)
Administration: Intravenous administration and oral administration
Result: Oral bioavailability (55%), Cmax (375 ng/mL), T1/2 (1.7 h).
Animal Model: Beagle dogs[1]
Dosage: 1 mg/kg for i.v.; 5 mg/kg for oral (Pharmacokinetic Analysis)
Administration: Intravenous administration and oral administration
Result: Oral bioavailability (>100%), Cmax (1249 ng/mL), T1/2 (11.9 h).
Animal Model: Cynomolgus monkeys[1]
Dosage: 1 mg/kg for i.v.; 5 mg/kg for oral (Pharmacokinetic Analysis)
Administration: Intravenous administration and oral administration
Result: Oral bioavailability (54%), Cmax (389 ng/mL), T1/2 (4.2 h).
分子量

438.81

Formula

C20H15ClF4N4O
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

JNJ-54166060 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

JNJ-541660601627900-41-7JNJ54166060JNJ 54166060P2X ReceptorP2XRsP2X7ATPgatedpurinergicionchannelproinflammatorycytokinesInhibitorinhibitorinhibit

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产品名称：
JNJ-54166060
目录号：
HY-124300
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