貨號	規(guī)格	價格	上海	北京	武漢	南京	購買數(shù)量
S82659-5mg	≥99%	￥1200.00 S82659-5mg ￥1200.00 2-3天	0 貨期：2-3天	-	-	-
S82659-10mg	≥99%	￥2000.00 S82659-10mg ￥2000.00 2-3天	0 貨期：2-3天	-	-	-

產(chǎn)品介紹

S1RA (E-52862) hydrochloride is an orally active and selective sigma-1 receptor (σ1R) antagonist with a Ki value of 17 nM. S1RA hydrochloride shows good selectivity against σ2R (Ki >1000 nM). S1RA hydrochloride is a human 5-HT2B receptor antagonist with an IC50 value of 4.7 μM. S1RA hydrochloride inhibits neuropathic pain and activity-induced spinal sensitization

產(chǎn)品描述：

靶點(diǎn)：

Sigma 1 Receptor;Sigmareceptor

體外研究：

S1RA hydrochloride (0.1-10000 nM) 對人和豚鼠的 σ1R 的 Ki 值分別為 17 和 23.5 nM。 S1RA hydrochloride (0.1-10000 nM) 對人 σ2R 具有親和力，Ki 值為 9.3 μM。 S1RA hydrochloride 對人 5-HT2B 受體具有親和力，Ki 值為 328 nM，IC50 值為 4.7 μM

體內(nèi)研究：

S1RA hydrochloride (腹腔注射 16-80 mg/kg 或口服 32-128 mg/kg；一次) 劑量依賴性地抑制小鼠中福爾馬林誘導(dǎo)的痛覺，辣椒素誘導(dǎo)的機(jī)械超敏反應(yīng)和坐骨神經(jīng)損傷誘導(dǎo)的機(jī)械和熱超敏反應(yīng)。 Animal Model: Male CD1 mice Dosage: 32, 64, 128 and 160 mg/kg Administration: Intraperitoneal injection; 32, 64, 128 and 160 mg/kg, once Result: Reduced the permanence time on the rotating rod in rotarod test. Animal Model: Male CD1 mice with formalin-evoked nociception Dosage: 20, 40 and 80 mg/kg Administration: Intraperitoneal injection; 20, 40 and 80 mg/kg, once Result: Dose-dependently showed analgesic effect on of formalin-evoked nociceptive behaviours of mice. Animal Model: Male CD1 mice with capsaicin-induced mechanical hypersensitivity Dosage: 16, 32 and 64 mg/kg (i.p.); 32, 64 and 128 mg/kg (oral administration) Administration: Intraperitoneal injection or oral administration; 16, 32 and 64 mg/kg (i.p.); 32, 64 and 128 mg/kg (oral administration), once Result: Dose-dependently reversed capsaicin-induced mechanical hypersensitivity in mice.

參考文獻(xiàn)：

1. Romero L, et al. Pharmacological properties of S1RA, a new sigma-1 receptor antagonist that inhibits neuropathic pain and activity-induced spinal sensitization. Br J Pharmacol. 2012 Aug;166(8):2289-306. 2. Vidal-Torres A, et al. Effects of the selective sigma-1 receptor antagonist S1RA on formalin-induced pain behavior and neurotransmitter release in the spinal cord in rats. J Neurochem. 2014 Jan 3.

溶解性：

soluble in DMSO

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	2.675 ml	13.373 ml	26.747 ml
5 mM	0.535 ml	2.675 ml	5.349 ml
10 mM	0.267 ml	1.337 ml	2.675 ml
50 mM	0.053 ml	0.267 ml	0.535 ml

注意：

部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。

參考文獻(xiàn)

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S1RA (hydrochloride)