JNJ-42253432

Name: JNJ-42253432
Brand: TargetMol
SKU: T27683
Price: 708 CNY
Availability: InStock
Rating: 5 (10 reviews)

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纯度: 99.98%

货号 T27683Cas号 1428327-35-8

JNJ-42253432是一种口服活性 P2X7拮抗剂，能够穿透中枢神经系统，大鼠 P2X7通道 pKi 值为9.1，人 P2X7通道 pKi 值为7.9。

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JNJ-42253432

一键复制产品信息

很棒

纯度: 99.98%

货号 T27683Cas号 1428327-35-8

JNJ-42253432是一种口服活性 P2X7拮抗剂，能够穿透中枢神经系统，大鼠 P2X7通道 pKi 值为9.1，人 P2X7通道 pKi 值为7.9。

规格	价格	库存
1 mg	¥ 708	现货
5 mg	¥ 1,750	现货
10 mg	¥ 2,500	现货
25 mg	¥ 3,550	现货
50 mg	¥ 5,000	现货
100 mg	¥ 6,720	现货
200 mg	¥ 8,900	现货
1 mL x 10 mM (in DMSO)	¥ 2,030	现货

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产品介绍

JNJ-42253432 AI Summary

JNJ-42253432 exhibits a range of bioactivities and pharmacokinetic characteristics. It shows moderate inhibition of rat nACHR with an IC50 of 910 nM and significant inhibition of human dopamine transporter with an IC50 of 290 nM. At a concentration of 1 μM, it inhibits rat nACHR by 54% relative to control, and human dopamine transporter by 93%. It also targets the human NK2 receptor, demonstrating 68% inhibition at 1 μM. For P2X7 receptors, JNJ-42253432 acts as an antagonist, displaying an IC50 of 199.53 nM in human whole blood, 39.81 nM in human PBMC, 79.43 nM in mouse receptors, and 15.85 nM in rat receptors. It also inhibits the human recombinant P2X7 receptor in 1321N1 cells with an IC50 of 19.95 nM. The compound binds with high affinity to the human serotonin transporter, displacing [3H]-Citalopram with a Ki of 15.85 nM. In terms of pharmacokinetics, JNJ-42253432 exhibits a high intrinsic clearance rate of 200 mL.min^-1.kg^-1 in rat liver microsomes. Its apparent permeability across the basolateral to apical side in MDCK-MDR1 cells is low, with a Papp value of 0.25 x10^-6 cm/s, and it shows a slight efflux effect with an efflux ratio of 1.1 in MDCK2-MDR1 cells..

Note: Summary generated by AI. Data source: ChEMBL

生物活性

产品描述	JNJ-42253432 is an oral active P2X7 antagonist capable of penetrating the central nervous system with a pKi value of 9.1 for rat and 7.9 for human P2X7 channels.
靶点活性	P2X7:7.9(pKi, human), P2X7:9.1(pKi, rat)

化学信息

分子量	446.63
分子式	C₂₈H₃₈N₄O
CAS No.	1428327-35-8
Smiles	CN1CCc2c(C1)cccc2C(=O)NCC1(CCCCC1)N1CCN(CC1)c1ccccc1
密度	1.130 g/cm3 (Predicted)

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

DMSO: 90 mg/mL (201.51 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (7.39 mM), Sonication is recommended.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.2390 mL	11.1949 mL	22.3899 mL	111.9495 mL
5 mM	0.4478 mL	2.2390 mL	4.4780 mL	22.3899 mL
10 mM	0.2239 mL	1.1195 mL	2.2390 mL	11.1949 mL
20 mM	0.1119 mL	0.5597 mL	1.1195 mL	5.5975 mL
50 mM	0.0448 mL	0.2239 mL	0.4478 mL	2.2390 mL
100 mM	0.0224 mL	0.1119 mL	0.2239 mL	1.1195 mL