| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
|
| Targets |
MT1 (EC50 = 19 nM); MT2 (EC50 = 4.6 nM)
|
|---|---|
| ln Vitro |
S22153 is a specific ligand of MT1 and MT2 melatonin receptor subtypes, which displayed both in vitro and in vivo antagonistic properties in rodents. S22153 antagonized the in vitro melatonin-induced potentiation of electrically evoked contractions of isolated rat tail arteries[1].
|
| ln Vivo |
S-22153 increases the circadian amplitude of both rhythms in mice exposed to continuous light, and it sets the temperature and activity cycles to roughly 24 hours [1].
The ability of daily melatonin and the melatonin receptor antagonist, S22153, to entrain circadian system function was investigated in mice with atypical melatonin rhythm. B6D2F(1) mice were first synchronized to a LD 12:12 for approximately 2 wk, then exposed to continuous light (LL) until study completion. After 10-18 days of LL exposure, mice received daily subcutaneous (s.c.) melatonin at a dose of 0.1, 1 or 10 mg/kg/day (exp. 1) or daily intraperitoneal (i.p.) S22153 (20 mg/kg/day) with or without melatonin (1 mg/kg/day, exp. 2) at subjective zeitgeber time (ZT) 10 for 19 days. Then all the mice were exposed to LL for another 10 days. Spectral analysis showed that initial LL lengthened the period of both rhythms by approximately 1.5 hr as compared with LD 12:12. No entrainment of either rhythm was found in controls. Conversely, daily melatonin-only, S22153-only or their combination set the temperature and activity periods to approximately 24 hr and produced a significant increase of the circadian amplitude of both rhythms as compared with controls. However, after treatment withdrawal, the dominant period lengthened to approximately 25.5 hr in mice receiving either melatonin or S22153. On the contrary, the period remained close to 24 hr for the 10 days following withdrawal of combined S22153 and melatonin. Such sustained pharmacological resetting of circadian function could display therapeutic potential against external resynchronization resulting from defective photoperiodic entrainment[1]. |
| Animal Protocol |
Animal/Disease Models: 7weeks old male B6D2F1 mice, continuous light exposure for 10-18 days [1]
Doses: 20 mg/kg Route of Administration: daily intraperitonealfor 19 days Experimental Results: Temperature and activity cycles were set to approximately 24 hrs (hrs (hours)) and increased the circadian amplitude of both rhythms in mice exposed to continuous light. |
| References |
|
| Additional Infomation |
Melatonin has a key role in the circadian rhythm relay to periphery organs. Melatonin exerts its multiple roles mainly through two seven transmembrane domain, G-coupled receptors, namely MT1 or MT2 receptors. A pharmacological characterization of these human cloned melatonin hMT1 and hMT2 receptors stably expressed in HEK-293 or CHO cells is presented using a 2-[125I]-iodo-melatonin binding assay and a [35S]-GTPgammaS functional assay. Both reference compounds and new chemically diverse ligands were evaluated. Binding affinities at each receptor were found to be comparable on either HEK-293 or CHO cell membranes. Novel non-selective or selective hMT1 and hMT2 ligands are described. The [35S]-GTPgammaS functional assay was used to define the functional activity of these compounds which included partial, full agonist and/or antagonist activity. None of the compounds acted as an inverse agonist. We report new types of selective antagonists, such as S 25567 and S 26131 for MT1 and S 24601 for MT2. These studies brought other new molecular tools such as the selective MT1 agonist, S 24268, as well as the non-selective antagonist, S 22153. Finally, we also discovered S 25150, the most potent melatonin receptor agonist, so far reported in the literature.[2]
|
| Molecular Formula |
C14H17NOS
|
|---|---|
| Molecular Weight |
247.35588
|
| Exact Mass |
247.103
|
| Elemental Analysis |
C, 67.98; H, 6.93; N, 5.66; O, 6.47; S, 12.96
|
| CAS # |
180304-07-8
|
| PubChem CID |
9816339
|
| Appearance |
White to off-white solid powder
|
| LogP |
3.982
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
17
|
| Complexity |
269
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
PICRXJDULXLJCZ-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C14H17NOS/c1-3-11-4-5-14-13(8-11)12(9-17-14)6-7-15-10(2)16/h4-5,8-9H,3,6-7H2,1-2H3,(H,15,16)
|
| Chemical Name |
N-[2-(5-ethyl-1-benzothiophen-3-yl)ethyl]acetamide
|
| Synonyms |
N-[2-(5-ethyl-1-benzothiophen-3-yl)ethyl]acetamide; S-22153; N-(2-(5-ethylbenzo[b]thiophen-3-yl)ethyl)acetamide; starbld0003449;
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
