货号	规格	价格	上海	北京	珠海	重庆	武汉
S86811-10mg买3赠1	99.90%	￥390.00 S86811-10mg ￥390.00 现货（买3赠1）	10 10	-	-	-	-
S86811-50mg	99.90%	￥495.00 S86811-50mg ￥495.00 现货	6 6	-	-	-	-
S86811-100mg	≥97%	￥666.00 S86811-100mg ￥666.00 2-3天	0 货期：2-3天	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

S86811-10mg买3赠1

99.90%

￥390.00

S86811-50mg

99.90%

￥495.00

S86811-100mg

≥97%

￥666.00

货期：2-3天

产品描述：

A-740003 is a potent, selective and competitive P2X7 receptor antagonist with IC50 values are 18 and 40 nM for rat and human P2X7 receptors, respectively.

靶点：

IC50: 18 nM (rat P2X7 receptor), 40 nM (human P2X7 receptor);P2XReceptor

体内研究：

Systemic administration of A-740003 produces dose-dependent antinociception in a spinal nerve ligation model (ED50=19 mg/kg i.p.) in the rat. A-740003 also attenuates tactile allodynia in two other models of neuropathic pain, chronic constriction injury of the sciatic nerve and vincristine-induced neuropathy. In addition, A-740003 effectively reduces thermal hyperalgesia observed following intraplantar administration of carrageenan or complete Freund's adjuvant (ED50=38-54 mg/kg i.p.). A-740003 is ineffective in attenuating acute thermal nociception in normal rats and does not alter motor performance at analgesic doses

参考文献：

1. Grol MW, et al. P2X?-mediated calcium influx triggers a sustained, PI3K-dependent increase in metabolic acid production by osteoblast-like cells. Am J Physiol Endocrinol Metab. 2012 Mar 1;302(5):E561-75. 2. Kim JE, et al. P2X7 receptor activation ameliorates CA3 neuronal damage via a tumor necrosis factor-α-mediated pathway in the rat hippocampus following status epilepticus. J Neuroinflammation. 2011 Jun 2;8:62. 3. Donnelly-Roberts DL, et al. Mammalian P2X7 receptor pharmacology: comparison of recombinant mouse, rat and human P2X7 receptors.Br J Pharmacol. 2009 Aug;157(7):1203-14. Epub 2009 Jun 22. 4. Honore P, et al. A-740003 [N-(1-{[(cyanoimino)(5-quinolinylamino) methyl]amino}-2,2-dimethylpropyl)-2-(3,4-dimethoxyphenyl)acetamide], a novel and selective P2X7 receptor antagonist, dose-dependently reduces neuropathic pain in the rat. J Pharmacol Exp Th 5. Y. H. Gao, et al. Effect of electroacupuncture on the cervicospinal P2X7 receptor/fractalkine/CX3CR1 signaling pathway in a rat neck-incision pain model. Purinergic Signal. 2017 Jun;13(2):215-225.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.107 ml	10.536 ml	21.073 ml
5 mM	0.421 ml	2.107 ml	4.215 ml
10 mM	0.211 ml	1.054 ml	2.107 ml
50 mM	0.042 ml	0.211 ml	0.421 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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