S-22153
目录号 : GC64204
S-22153 是一种有效的褪黑素受体 (melatonin receptor) 拮抗剂，对 hMT1 和 hMT2 的 EC50 值分别为 19 nM 和 4.6 nM。S-22153 对 hMT1 的 Ki 值为 8.6 nM (CHO 细胞) 和 16.3 nM (HEK 细胞)，hMT2 的 Ki 值为 6.0 nM (CHO 细胞) 和 8.2 nM (HEK 细胞)。S-22153 是 MT1 和 MT2 褪黑素受体亚型的特异性配体。
Cas No.:180304-07-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
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- Purity: >98.00%
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- SDS (Safety Data Sheet)
- Datasheet
S-22153 is a potent melatonin receptor antagonist with EC50 values of 19 nM, 4.6 nM for hMT1 and hMT2 melatonin receptor, respectively. S-22153 has Ki values of 8.6 nM (CHO cells) and 16.3 nM (HEK cells) for hMT1, and 6.0 nM (CHO cells) and 8.2 nM (HEK cells) for hMT2. S-22153 is a specific ligand of MT1 and MT2 melatonin receptors subtypes[1][2].
S-22153 sets the temperature and activity periods to approximately 24 hr and increase the circadian amplitude of both rhythms in mice, which exposed to continuous light[1] .
[1]. Li XM, et al. Circadian rhythm entrainment with melatonin, melatonin receptor antagonist S22153 or their combination in mice exposed to constant light. J Pineal Res. 2004;37(3):176-184. [2]. Audinot V, et al. New selective ligands of human cloned melatonin MT1 and MT2 receptors. Naunyn Schmiedebergs Arch Pharmacol. 2003;367(6):553-561.
| Cas No. | 180304-07-8 | SDF | Download SDF |
| 分子式 | C14H17NOS | 分子量 | 247.36 |
| 溶解度 | DMSO : 100 mg/mL (404.27 mM; Need ultrasonic) | 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。 | ||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.0427 mL | 20.2135 mL | 40.4269 mL |
| 5 mM | 0.8085 mL | 4.0427 mL | 8.0854 mL |
| 10 mM | 0.4043 mL | 2.0213 mL | 4.0427 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 | ||||||||||
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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。
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Melatonin as a modulator of the ileal brake mechanism
Scand J Gastroenterol 2005 May;40(5):559-63.PMID:16036508DOI:10.1080/00365520510012316.
Objective: The gastrointestinal tract represents the most important extrapineal source of melatonin. Intestinal melatonin release is induced by the ileal passage of nutrients and could play a part in the control of postprandial gut motility. The specific aim of this study was to determine the putative role of melatonin in the "ileal brake" reflex, an important mechanism released by ileal lipids that regulates the gastric emptying of chyme. Material and methods: Under general anaesthesia rats were fitted with ileal cannula exteriorized at the back of the neck. After a 1-week recovery, experiments were performed in conscious fasted animals. Rats were fed by gavage 1.5 ml casein hydrolyse plus 0.05% phenol red and either saline or Intralipid were continuously infused (2 ml/h) into the ileum. Gastric emptying was measured 50 min after ingestion by gastric lavage and determination of phenol red by spectrophotometry. The effects of melatonin (1 mg/kg) and melatonin antagonist S-22153 (dose-response study 0.2-25 mg/kg) were tested versus vehicle in paired experiments at 1-week intervals. Results: Ileal infusion of lipids delayed gastric emptying. During ileal infusion of lipids, melatonin antagonist S-22153, but not melatonin, potentiated the delay in gastric emptying induced by the ileal brake mechanism. The inhibition of gastric emptying induced by S-22153 was dose related. Neither melatonin nor S-22153 had noticeable effects on gastric emptying during ileal infusion of saline. Conclusions: Our data suggest that melatonin, released in response to ileal lipids, exerts a modulatory influence that decreases the inhibitory effects of the ileal brake on gastric emptying of nutrients.
Reentrainment of the spontaneous locomotor activity rhythm to a daylight reversal in C57BL/6 and C3H/He mice: implication of melatonin
Physiol Behav 2000 Jul;70(1-2):171-6.PMID:10978493DOI:10.1016/s0031-9384(00)00251-1.
The adaptation of the locomotor activity rhythm to a daylight reversal was previously found to be faster in C57BL/6 mice, which present a low level of melatonin, than in C3H/He mice, which exhibit a large nocturnal melatonin peak. Because pinealectomy has been shown to accelerate resynchronisation time in rats after a daylight reversal, we investigated the involvement of melatonin in the resynchronisation rate of locomotor activity rhythm in C57BL/6 and C3H/He strains. We first tested the effects of melatonin, administered at zeitgeber time (ZT) 20 (with ZT0 corresponding to light onset) for the 3 days preceding the daylight reversal, on the reentrainment of locomotor activity rhythm in both strains. Second, the effects of S-22153, a melatonin receptor antagonist, on the reentrainment of locomotor activity rhythm in C3H/He mice were examined. S-22153 was administered for the 3 days preceding the daylight reversal either at ZT12 or at ZT20, i.e., when endogenous melatonin levels are respectively low and high. Melatonin significantly delayed the resynchronisation of locomotor activity rhythm in C57BL/6 mice without affecting this parameter in C3H/He mice. S-22153 significantly accelerated the resynchronisation in C3H/He mice when administered at ZT20, but had no effect when administered at ZT12. These results support the hypothesis that the differences between C3H/He and C57BL/6 in the reentrainment of their locomotor activity rhythm depend, at least in part, on the interstrain differences in melatonin synthesis.