SX-3228
目录号 : GC31196
SX-3228是一种选择性苯二氮卓类(benzodiazepine1，BZ1)受体激动剂，IC50为17nM。
Cas No.:156364-04-4
Sample solution is provided at 25 µL, 10mM.
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SX-3228 is a selective benzodiazepine1 (BZ1) receptor agonist with an IC50 of 17 nM.
SX-3228 is a selective ligand for the BZ1 receptor. Among the BZ-receptor subtypes, SX-3228 preferentially binds to the BZ1 receptor (IC50=17 nM). It has very weak affinity for the BZ2 receptor (spinal cord: IC50=127 nM), and virtually no affinity for the peripheral type BZ receptor (kidney: IC50>10000 nM). A compound with similar selectivity, SX-3228 has been shown to bind to BZ receptors, but not to dopamine (D1, D2), serotonin (5-HT1, 5-HT2 and 5-HT3 subtypes), noradrenaline (α1, α2, β), GABA or acetylcholine (muscarinic) subtypes[1].
Administration of 0.5-2.5 mg/kg SX-3228 to rats during the light phase induces a significant reduction of rapid-eye-movement sleep (REMS) (P<0.05) during the third recording hour. Administration of SX-3228 (0.5-2.5 mg/kg) at the beginning of the dark period significantly and dose-dependently reduces waking (W) and increases slow wave sleep (SWS) during the 6-h recording period (P<0.05-0.01); however, significant changes during the last recording hour are restricted to the 2.5 mg/kg dose (P<0.01)[1].
[1]. Alvari?o F, et al. Effect of SX-3228, a selective ligand for the BZ1 receptor, on sleep and waking during the light-dark cycle in the rat. Braz J Med Biol Res. 1999 Aug;32(8):1007-14.
Animal experiment: | Rats[1]Twelve male Wistar rats (350-380 g) are used. Subcutaneous (sc) injections are given in a final volume of 1.0 mL/kg. All rats are given the corresponding volume of control solution (saline+Tween-80) in the control sessions. Following sc injection, a 6-h sleep recording is started at approximately 8:00 a.m. At least 4 days are allowed to elapse between injections to avoid long-lasting and rebound effects on sleep. The effects of SX-3228 0.5-2.5 mg/kg are studied in one group of animals (N=6) during the light phase of the 12-h light:12-h dark cycle, starting 1 h after the beginning of the light period. Polysomnographic recordings are started immediately after control solution or drug administration. Each rat receives all four treatments (control, and 0.5, 1.0, 2.5 mg/kg SX-3228). |
References: [1]. Alvariño F, et al. Effect of SX-3228, a selective ligand for the BZ1 receptor, on sleep and waking during the light-dark cycle in the rat. Braz J Med Biol Res. 1999 Aug;32(8):1007-14. | |
| Cas No. | 156364-04-4 | SDF | |
| Canonical SMILES | O=C1NC2=C(CN(CC3=CC=CC=C3)CC2)C=C1C4=NN=C(OC)O4 | ||
| 分子式 | C18H18N4O3 | 分子量 | 338.36 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| 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 | 2.9554 mL | 14.7772 mL | 29.5543 mL |
| 5 mM | 0.5911 mL | 2.9554 mL | 5.9109 mL |
| 10 mM | 0.2955 mL | 1.4777 mL | 2.9554 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