Xylazine
(Synonyms: 赛拉嗪,BAY 1470) 目录号 : GC12073
Xylazine（赛拉嗪；BAY 1470）是一种有效的α2-肾上腺素受体的强激动剂，在兽医学中广泛用作镇静剂，还能诱导肌肉松弛。
Cas No.:7361-61-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
Cell lines | PC12 cells |
Preparation Method | 100μl (approximately 1×104 cells) of cell suspension was added to wells of a 96-well plate. The plate was pre-incubated in the incubator for 24h. Then, 100μl of cell culture medium containing different concentrations of Xylazine (0.9, 1.8, 2.7, 3.6, 4.5, 5.4, 6.3μM) was added to the plate. CCK-8 solution was added to each well at 3h after adding Xylazine, and incubated for 1-4h. The absorbance at 450nm was measured using a microplate reader. |
Reaction Conditions | 0.9, 1.8, 2.7, 3.6, 4.5, 5.4, 6.3μM; 3h |
Applications | Xylazine significantly reduced cell viability, and the cell survival rate reached 61% at a dose of 4.5μM. |
| Animal experiment [2]: | |
Animal models | Sprague-Dawley rats |
Preparation Method | Healthy male Sprague-Dawley rats (n=30) were randomly assigned to control or Xylazine groups. Six rats received intraperitoneal injection of saline (0.5mL, control group) and were sacrificed 10min later. Twenty-four rats in the Xylazine group were further subdivided into four groups. After receiving an injection of Xylazine (5.2mg/kg diluted in 0.5mL saline), the rats were sacrificed 10min(Xyl1 group), 20min(Xyl2 group), 40min(Xyl3 group) or 60min(Xyl4 group) respectively. Then the brains were immediately removed and placed in ice-cold slurry of 0.9% NaCl. Five brain structures were dissected under a microscope: cerebral cortex, cerebellum, hippocampus, thalamus and brainstem. Dissected tissues were immediately frozen in liquid nitrogen and stored at −80°C for pending analysis. |
Dosage form | 5.2mg/kg; i.p. |
Applications | Xylazine induced a significant decrease in the mRNA levels of LKB1 in the brainstem at 40min after rats received Xylazine, whereas a significant increase was observed in the cerebral cortex, hippocampus, thalamus, and cerebellum. |
References: | |
Xylazine (BAY 1470) is a potent agonist of α2-adrenergic receptors and is widely used as a sedative in veterinary medicine. It can also induce muscle relaxation[1, 2]. Xylazine is often co-administered with ketamine for safe and effective anesthesia of small experimental animals[3].
In vitro, Xylazine (0.9, 1.8, 2.7, 3.6, 4.5, 5.4, 6.3μM) treatment of PC12 cells for 3h significantly reduced cell viability. When the dose was 4.5μM, the cell survival rate was 61%. It also inhibited the expression of extracellular regulated protein kinase (ERK) and protein kinase A (PKA)[4]. Xylazine (1, 4, 25mg/mL) was used to treat horse articular chondrocytes for 15min, which reduced cell viability in a dose-dependent manner. At a dose of 25mg/mL, cells showed apoptotic morphologies such as cell shrinkage, membrane blebbing, nuclear chromatin condensation, and nuclear fragmentation[5].
In vivo, Xylazine (5.2mg/kg) was used to treat SD rats by intraperitoneal injection for 10-60min. When the rats were killed 40min after administration, the mRNA level of liver kinase B1 (LKB1) in the brainstem was significantly reduced, while the mRNA level of LKB1 in the cerebral cortex, hippocampus, thalamus, and cerebellum was significantly increased[6].
References:
[1] Park J W, Chung H W, Lee E J, et al. α2-Adrenergic agonists including xylazine and dexmedetomidine inhibit norepinephrine transporter function in SK-N-SH cells[J]. Neuroscience Letters, 2013, 541: 184-189.
[2] Da Silveira J G, Cappelari B E, Varela A P M, et al. Evaluation of the effects of acepromazine and xylazine on viability in an equine dermal cell line[J]. Acta Veterinaria Brasilica, 2020, 14(4).
[3] Saha J K, Xia J, Grondin J M, et al. Acute hyperglycemia induced by ketamine/xylazine anesthesia in rats: mechanisms and implications for preclinical models[J]. Experimental Biology and Medicine, 2005, 230(10): 777-784.
[4] Zhao J, Zhang Y, Liu W, et al. Molecular mechanisms of the sedation and analgesia induced by xylazine on Wistar rats and PC12 cell[J]. Experimental animals, 2019, 68(3): 351-360.
[5] Mancini F, Nannarone S, Buratta S, et al. Effects of xylazine and dexmedetomidine on equine articular chondrocytes in vitro[J]. Veterinary anaesthesia and analgesia, 2017, 44(2): 295-308.
[6] Shi X X, Yin B S, Yang P, et al. Xylazine activates adenosine monophosphate-activated protein kinase pathway in the central nervous system of rats[J]. PLoS One, 2016, 11(4): e0153169.
Xylazine（赛拉嗪；BAY 1470）是一种有效的α2-肾上腺素受体的强激动剂，在兽医学中广泛用作镇静剂，还能诱导肌肉松弛[1, 2]。Xylazine常与氯胺酮（Ketamine）联合给药，用于安全、有效地麻醉小型实验动物[3]。
在体外，Xylazine（0.9, 1.8, 2.7, 3.6, 4.5, 5.4, 6.3μM）处理PC12细胞3h，显著降低了细胞活力，使用剂量为4.5μM时，细胞存活率为61%，还抑制了细胞外调节蛋白激酶（ERK）和蛋白激酶A（PKA）的表达[4]。Xylazine（1，4，25mg/mL）处理马关节软骨细胞15min，以剂量依赖性方式降低了细胞活力，使用剂量为25mg/mL时，细胞表现出细胞收缩、膜起泡、核染色质浓缩和核碎裂等凋亡形态[5]。
在体内，Xylazine（5.2mg/kg）通过腹腔注射处理SD大鼠10-60min，当给药40min后再处死大鼠，显著降低了脑干中肝激酶B1（LKB1）的mRNA水平，而大脑皮层、海马、丘脑和小脑中LKB1的mRNA水平显著升高[6]。
| Cas No. | 7361-61-7 | SDF | |
| 别名 | 赛拉嗪,BAY 1470 | ||
| 化学名 | N-(2,6-dimethylphenyl)-5,6-dihydro-4H-1,3-thiazin-2-amine | ||
| Canonical SMILES | CC1=C(C(=CC=C1)C)NC2=NCCCS2 | ||
| 分子式 | C12H16N2S | 分子量 | 220.33 |
| 溶解度 | ≥ 9.8mg/mL in DMSO，insoluble in water and in alkali solutions | 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 | 4.5386 mL | 22.6932 mL | 45.3865 mL |
| 5 mM | 0.9077 mL | 4.5386 mL | 9.0773 mL |
| 10 mM | 0.4539 mL | 2.2693 mL | 4.5386 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 |
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| % 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，
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2.
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