SSR504734
目录号 : GC67871SSR504734 是一种具有口服活性、选择性和可逆性的 GlyT1 抑制剂 (hGlyT1，rGlyT1，mGlyT1 IC50 分别为 18、15 和 38 nM)。SSR504734 表现出抗精神分裂、抗焦虑和抗抑郁的活性。
Cas No.:615571-23-8
Sample solution is provided at 25 µL, 10mM.
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SSR504734 is an orally active, selective and reversible inhibitor of human, rat, and mouse GlyT1 (IC50=18, 15, and 38 nM, respectively). SSR504734 shows anti-schizophrenia, anti-anxiety and anti-depression activities[1].
SSR504734 (15 nM-86 μM; 10 min) inhibits glycine uptake in human SK-N-MC and rat C6 cells[1].
Cell Viability Assay[1]
| Cell Line: | Human neuroblastoma (SK-N-MC) and rat astrocytoma (C6) cells |
| Concentration: | 15 nM-86 μM |
| Incubation Time: | 10 min |
| Result: | Showed IC50 values of 18 and 15 nM for human SK-N-MC and rat C6 cells, respectively. |
SSR504734 (i.p. and p.o.; 1-100 mg/kg; once) treatment shows good oral bioavailability[1].
SSR504734 (i.p.; 30 mg/kg; once) induces a rapid and significant decrease of specific glycine uptake[1].
SSR504734 (i.p.; 10 mg/kg; once) increases extracellular levels of Glycine in the prefrontal cortex (PFC) of freely moving rats[1].
| Animal Model: | Male Sprague-Dawley rats[1] |
| Dosage: | 1-100 mg/kg |
| Administration: | Intraperitoneal injection and oral gavage.; 1-100 mg/kg; once |
| Result: | Showed ID50 values of 5.0 and 4.6 mg/kg for i.p. and p.o. treatments, respectively. |
| Animal Model: | Male Sprague-Dawley rats[1] |
| Dosage: | 30 mg/kg |
| Administration: | Intraperitoneal injection; 30 mg/kg; once |
| Result: | Maintained at about 80% inhibition from 1 to 7 h after administration. |
| Animal Model: | Male Sprague-Dawley rats[1] |
| Dosage: | 10 mg/kg |
| Administration: | Intraperitoneal injection; 10 mg/kg; once |
| Result: | Produced a rapid and sustained increase in PFC extracellular levels of glycine. |
[1]. Ronan DepoortÈre, et al. Neurochemical, electrophysiological and pharmacological profiles of the selective inhibitor of the glycine transporter-1 SSR504734, a potential new type of antipsychotic. Neuropsychopharmacology. 2005 Nov;30(11):1963-85.
| Cas No. | 615571-23-8 | SDF | Download SDF |
| 分子式 | C20H21Cl2F3N2O | 分子量 | 433.29 |
| 溶解度 | DMSO : 100 mg/mL (230.79 mM; Need ultrasonic) | 储存条件 | 4°C, away from moisture and light |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3079 mL | 11.5396 mL | 23.0792 mL |
| 5 mM | 0.4616 mL | 2.3079 mL | 4.6158 mL |
| 10 mM | 0.2308 mL | 1.154 mL | 2.3079 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet