PF 04531083

Name: PF 04531083
Brand: TargetMol
SKU: T16514
Price: 328 CNY
Availability: InStock
Rating: 5 (10 reviews)

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很棒

纯度: 99.85%

货号 T16514Cas号 1079400-07-9

PF 04531083 是 NaV1.8 通道的特异性阻断剂。 PF 04531083 可用于神经性和炎症性疼痛的相关研究。

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PF 04531083

一键复制产品信息

很棒

纯度: 99.85%

货号 T16514Cas号 1079400-07-9

PF 04531083 是 NaV1.8 通道的特异性阻断剂。 PF 04531083 可用于神经性和炎症性疼痛的相关研究。

规格	价格	库存
1 mg	¥ 328	现货
5 mg	¥ 828	现货
10 mg	¥ 1,490	现货
25 mg	¥ 2,320	现货
50 mg	¥ 3,480	现货
100 mg	¥ 4,890	现货
1 mL x 10 mM (in DMSO)	¥ 733	现货

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COA HNMR LCMS 产品操作手册

产品介绍

PF 04531083 AI Summary

PF 04531083 exhibits potent inhibition of human Nav1.8, with an IC50 of 700.0 nM, and shows selective inhibition of human Nav1.8/beta1 with an IC50 of 190.0 nM. It also inhibits voltage-gated sodium channels in rat and human DRG neurons, with IC50 values ranging from 200.0 to 540.0 nM. In a rat model, the compound demonstrates a half-life of 3.9 hours at 1 mg/kg and a Tmax of 1.3 hours at 2 mg/kg. It has moderate oral bioavailability with an F value of 59.0% at 2 mg/kg. Additionally, PF 04531083 shows an antiallodynic effect in a rat tibial nerve transection-induced mechanical allodynia model at 40 mg/kg and has a favorable unbound plasma concentration (Fu = 0.2). Notably, it penetrates the blood-brain barrier with a ratio of drug level from CSF to unbound plasma concentration at 40 mg/kg of 0.75 and at 250 mg/kg of 0.33..

Note: Summary generated by AI. Data source: ChEMBL

生物活性

产品描述	PF 04531083 is a selective blocker of the NaV1.8 channel. PF 04531083 can be used for neuropathic and inflammatory pain studies.

化学信息

分子量	357.79
分子式	C₁₇H₁₆ClN₅O₂
CAS No.	1079400-07-9
Smiles	COc1ccc(Cl)c(c1)-c1ccc(NC(=O)c2ccnn2C)nc1N
密度	1.41 g/cm3 (Predicted)
颜色	White
物理性状	Solid

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: 120 mg/mL (335.39 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (11.18 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	2.7949 mL	13.9747 mL	27.9494 mL	139.7468 mL
5 mM	0.5590 mL	2.7949 mL	5.5899 mL	27.9494 mL
10 mM	0.2795 mL	1.3975 mL	2.7949 mL	13.9747 mL
20 mM	0.1397 mL	0.6987 mL	1.3975 mL	6.9873 mL
50 mM	0.0559 mL	0.2795 mL	0.5590 mL	2.7949 mL
100 mM	0.0279 mL	0.1397 mL	0.2795 mL	1.3975 mL