S-22153

Modify Date: 2024-01-03 17:48:16

S-22153 Structure
S-22153 structure
Common Name S-22153
CAS Number 180304-07-8 Molecular Weight 247.35600
Density N/A Boiling Point N/A
Molecular Formula C14H17NOS Melting Point N/A
MSDS N/A Flash Point N/A

 Use of S-22153


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].

 Names

Name N-[2-(5-Ethyl-1-benzothiophen-3-yl)ethyl]acetamide

 S-22153 Biological Activity

Description 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].
Related Catalog
Target

MT1:19 nM (EC50)

MT2:4.6 nM (EC50)

In Vivo 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] . Animal Model: 7 weeks old Male B6D2F1 mice, which exposed to continuous light for 10-18 days[1] Dosage: 20 mg/kg Administration: Daily intraperitoneal (i.p.) for 19 days Result: Set the temperature and activity periods to approximately 24 hr and increased the circadian amplitude of both rhythms in mice, which exposed to continuous light.
References

[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.

 Chemical & Physical Properties

Molecular Formula C14H17NOS
Molecular Weight 247.35600
Exact Mass 247.10300
PSA 60.83000
LogP 3.98260