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A-317491 sodium salt hydrate
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
A-317491 sodium salt hydrate图片

A-317491 sodium salt hydrate 是非核苷酸类P2X3和P2X2/3受体拮抗剂，能抑制由其介导的钙流。
Canonical SMILESO=C(C1=CC(C(N(CC2=CC=CC(OC3=CC=CC=C3)=C2)[C@H]4CCCC5=C4C=CC=C5)=O)=C(C(O)=O)C=C1C(O)=O)O.[Na].O
分子式C33H29NNaO9
分子量606.57
溶解度Water: ≥ 100 mg/mL (164.86 mM); DMSO: ≥ 100 mg/mL (164.86 mM)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

A-317491 sodium salt hydrate is a non-nucleotide P2X3 and P2X2/3 receptor antagonist, which inhibits calcium flux mediated by the receptors.IC50 value:Target: P2X2/3 receptor It is known that P2X3 and P2X2/3 receptors stimulate the pronociceptive effects of ATP upon activation. Studies indicate that the P2X3 receptor is implicated in both neuropathic and inflammatory pain. P2X3 receptor is a promising target for therapeutic intervention in cancer patients for pain management.

[1]. Hansen RR, Nasser A, Falk S, et al. Chronic administration of the selective P2X3, P2X2/3 receptor antagonist, A-317491, transiently attenuates cancer-induced bone pain in mice. Eur J Pharmacol. 2012 Aug 5;688(1-3):27-34. [2]. Wu JX, Xu MY, Miao XR, et al. Functional up-regulation of P2X3 receptors in dorsal root ganglion in a rat model of bone cancer pain. Eur J Pain. 2012;16(10):1378-88. [3]. Xu J, Chu KL, Brederson JD, et al. Spontaneous firing and evoked responses of spinal nociceptive neurons are attenuated by blockade of P2X3 and P2X2/3 receptors in inflamed rats. J Neurosci Res. 2012;90(8):1597-606. [4]. Yasuda M, Shinoda M, Kiyomoto M, et al. P2X3 receptor mediates ectopic mechanical allodynia with inflamed lower lip in mice. Neurosci Lett. 2012 18;528(1):67-72. [5]. Maria ClÁudia G. Oliveiraa, Adriana Pelegrini-da-Silvaa, et al. Peripheral mechanisms underlying the essential role of P2X3,2/3 receptors in the development of inflammatory hyperalgesia. PAIN. 2009,141(1-2): 127-134.

 
 
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