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Ro 25-6981 maleate salt, NR2B antagonist
NMR and HPLC COA下载 MSDS下载 - Names：
Ro 25-6981 maleate salt, NR2B antagonist
- CAS号：
169274-78-6
MDL Number： - MF(分子式)： C22H29NO2 MW(分子量)： 339.47
- EINECS:Not available Reaxys Number:
- Pubchem ID: Brand:BIOFOUNT
Ro 25-6981 maleate salt, NR2B antagonist（马来酸盐）是一种有效的、选择性活性依赖性的 NMDA 受体阻滞剂，含有 NR2B 亚基（对于克隆的受体亚基组合 NR1C/NR2B 和 NR1C/NR2A，IC50 分别为 9 nM 和 52 μM）。 Ro 25 -6981（马来酸盐）在体外表现出神经保护作用，保护皮层神经元免受谷氨酸毒性和联合氧气和葡萄糖剥夺，IC50 值分别为 0.4 和 0.04 μM.
| 货品编码 | 规格 | 纯度 | 价格 (¥) | 现价(¥) | 特价(¥) | 库存描述 | 数量 | 总计 (¥) |
|---|---|---|---|---|---|---|---|---|
| YZM010412-5mg | 1mg | ¥ 1440.00 | ¥ 1440.00 | 4-7weeks | ¥ 0.00 | |||
| YZM010412-10mg | 10mg | ¥ 3680.00 | ¥ 3680.00 | 4-7weeks | ¥ 0.00 |
| 中文别名 | 169274-78-6;Ro 25-6981 maleate salt，NR2B拮抗剂;NR2B拮抗剂;2Z-丁烯二酸酯;马来酸盐 |
| 英文别名 | Ro 25-6981,169274-78-6;NR2B antagonist;2Z-butenedioate |
| CAS号 | 169274-78-6 |
| Inchi | InChI=1S/C22H29NO2.C4H4O4/c1-17(22(25)20-7-9-21(24)10-8-20)16-23-13-11-19(12-14-23)15-18-5-3-2-4-6-18;5-3(6)1-2-4(7)8/h2-10,17,19,22,24-25H,11-16H2,1H3;1-2H,(H,5,6)(H,7,8)/b;2-1-/t17-,22+;/m0./s1 |
| InchiKey | FYJZEHCQSUBZDY-SEELMCCHSA-N |
| 分子式 Molecular Weight | C22H29NO2 |
| 分子量 Formula | 339.47 |
| 溶解度Solubility | DMSO: 100 mM ;Water: 25 mM |
| 性状 | Solid |
| 储藏条件 Storage conditions | 请根据产品建议的存储条件进行存储，Please store the product under the recommended condition sin the description. |
Ro 25-6981(CAS:169274-78-6)实验注意事项：
1.实验前需戴好防护眼镜，穿戴防护服和口罩，佩戴手套，避免与皮肤接触。
2.实验过程中如遇到有毒或者刺激性物质及有害物质产生，必要时实验操作需要手套箱内完成以免对实验人员造成伤害
3.实验后产生的废弃物需分类存储，并交于专业生物废气物处理公司处理，以免造成环境污染Experimental considerations:
1. Wear protective glasses, protective clothing and masks, gloves, and avoid contact with the skin during the experiment.
2. The waste generated after the experiment needs to be stored separately, and handed over to a professional biological waste gas treatment company to avoid environmental pollution.
1.实验前需戴好防护眼镜，穿戴防护服和口罩，佩戴手套，避免与皮肤接触。
2.实验过程中如遇到有毒或者刺激性物质及有害物质产生，必要时实验操作需要手套箱内完成以免对实验人员造成伤害
3.实验后产生的废弃物需分类存储，并交于专业生物废气物处理公司处理，以免造成环境污染Experimental considerations:
1. Wear protective glasses, protective clothing and masks, gloves, and avoid contact with the skin during the experiment.
2. The waste generated after the experiment needs to be stored separately, and handed over to a professional biological waste gas treatment company to avoid environmental pollution.
| 产品说明 | Ro 25-6981 maleate salt, NR2B antagonist（马来酸盐）是一种有效的、选择性活性依赖性的 NMDA 受体阻滞剂，含有 NR2B 亚基（对于克隆的受体亚基组合 NR1C/NR2B 和 NR1C/NR2A，IC50 分别为 9 nM 和 52 μM）。 Ro 25 -6981（马来酸盐）在体外表现出神经保护作用，保护皮层神经元免受谷氨酸毒性和联合氧气和葡萄糖剥夺，I |
| Introduction | Ro 25-6981 is a potent and selective activity-dependent blocker of NMDA receptors containing the NR2B subunit. IC50 values are 0.009 and 52 μM for cloned receptor subunit combinations NR1C/NR2B and NR1C/NR2A respectively.IC50 value: 9 nM Target: NMDA receptor subtype of NR1C & NR2Bin vitro: Ro 25-6981 inhibited 3H-MK-801 binding to rat forebrain membranes in a biphasic manner with IC50 values of 0.003 microM and 149 microM for high- (about 60%) and low-affinity sites, respectively. NMDA receptor subtypes expressed in Xenopus oocytes were blocked with IC50 values of 0.009 microM and 52 microM for the subunit combinations NR1C & NR2B and NR1C & NR2A, respectively, which indicated a >5000-fold selectivity . Increasing the concentration of spermidine did not change the efficacy of RO 25-6981 and minimally changed the IC(50) value. Epsilon1Q336R receptors were more inhibited by ifenprodil and RO 25-9681 than wildtype epsilon1 receptors in ligand binding assays but not in functional assays .in vivo: Intrathecal injection of Ro 25-6981 significantly enhanced the paw withdrawal mechanical threshold and paw withdrawal thermal latency after the operation. Significant change has been observed after intrathecal injection of 800.0 μg of Ro 25-6981 and at 2h after operation in the oblique pull test degree and BBB rating score. Pretreatment of Ro 25-6981 decreased the high level expression of NR2B with tyrosine phosphorylation in spinal dorsal horn of the rat model after the operation . |
| Application1 | |
| Application2 | |
| Application3 |
| 警示图 | |
| 危险性 | warning |
| 危险性警示 | Not available |
| 安全声明 | H303吞入可能有害+H313皮肤接触可能有害+H2413吸入可能对身体有害 |
| 安全防护 | P264处理后彻底清洗+P280戴防护手套/穿防护服/戴防护眼罩/戴防护面具+P305如果进入眼睛+P351用水小心冲洗几分钟+P338取出隐形眼镜（如果有）并且易于操作,继续冲洗+P337如果眼睛刺激持续+P2393获得医疗建议/护理 |
| 备注 | 实验过程中防止吸入、食入，做好安全防护 |
| 【1】.Fischer G, et al. Ro 25-6981, a highly potent and selective blocker of N-methyl-D-aspartate receptors containing the NR2B subunit. Characterization in vitro. J Pharmacol Exp Ther. 1997 Dec;283(3):1285-92. |
| 【2】.Lynch DR, et al. Pharmacological characterization of interactions of RO 25-6981 with the NR2B (epsilon2) subunit. Eur J Pharmacol. 2001 Mar 30;416(3):185-95. |
| 【3】.Jiang M, et al. Antinociception and prevention of hyperalgesia by intrathecal administration of Ro 25-6981, a highly selective antagonist of the 2B subunit of N-methyl-D-aspartate receptor. Pharmacol Biochem Behav. 2013 Nov;112:56-63. |
| 【4】.Le Roux N et al. Input-specific learning rules at excitatory synapses onto hippocampal parvalbumin-expressing interneurons. J Physiol 591:1809-22 (2013). |
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