| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
RS-102221 HCl targets the 5-HT2C receptor, a subtype of the serotonin (5-HT) receptor that binds the endogenous neurotransmitter serotonin. It is a selective antagonist of this receptor, with a Ki of 10 nM and nearly 100-fold selectivity over 5-HT2A and 5-HT2B receptors. By blocking 5-HT2C receptors, it modulates serotonergic signaling in the central nervous system.
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| ln Vitro |
RS102221 (0.3-300nM; 24 h) dramatically raises the overall number of MAP-2+ cells and stimulates the production of mouse hippocampus neural precursor cells (ahNPCs) [1]. Concentrations of progenitor cells (ahNPC): 0.3, 1, 10, 30, 100, and 300 nM; incubation period: 24 hours; findings: At 10 nM, the proportion of MAP-2+ cells increased dramatically.
RS-102221 HCl is a potent and selective 5-HT2C receptor antagonist with a Ki of 10 nM. It shows nearly 100-fold selectivity for the 5-HT2C receptor over 5-HT2A and 5-HT2B receptors. It has pKi values of 8.4 and 8.5 for human and rat 5-HT2C, respectively. This demonstrates its potent and highly selective in vitro activity. |
| ln Vivo |
RS-102221 hydrochloride enhances body weight growth and meal component volume (2 mg/kg; i.p.; once daily for 14 days) [2]. sub-model) in conjunction with 3,4-methylenediphenyl-N-methamphetamine (MDMA, also known as the "report pill") in mice can reverse the effects of MDMA-induced hyperplasia and anorexia for the first hour [4]. Additionally, RS-102221 hydrochloride (2 mg/kg; intraperitoneal injection; single dose) can lessen mice's anxiety during the light-dark test and decrease the startle reflex's amplitude.
RS-102221 HCl has demonstrated in vivo activity. At a dose of 2 mg/kg, it reduces anxiety in the light-dark test in mice and reduces the amplitude of the startle response. This confirms its ability to modulate 5-HT2C receptor-mediated behaviors in vivo. |
| Enzyme Assay |
The in vitro activity of RS-102221 HCl is assessed using radioligand binding assays. Membrane preparations from cells expressing human or rat 5-HT2C, 5-HT2A, or 5-HT2B receptors are incubated with a labeled ligand in the presence of various concentrations of RS-102221 HCl. The Ki values are calculated from displacement curves.
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| Cell Assay |
The antagonist activity of RS-102221 HCl is assessed in functional cell-based assays. Cells expressing 5-HT2C receptors are treated with a 5-HT2 agonist (such as serotonin or DOI) in the presence or absence of RS-102221 HCl. The compound's ability to block agonist-induced calcium mobilization or other signaling events is measured. IC50 or Kb values are calculated.
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| Animal Protocol |
RS-102221 HCl has been evaluated in animal models of anxiety and startle response. In these studies, the compound is typically administered systemically (e.g., intraperitoneally) to rodents. Its effects on anxiety-like behavior (assessed in the light-dark test) and startle response are measured.
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| ADME/Pharmacokinetics |
RS-102221 HCl has a molecular weight of 649.08 and a molecular formula of C27H31F3N4O7S·HCl. It is soluble in DMSO. Purity is typically 98% by HPLC. The compound is a selective 5-HT2C receptor antagonist and is a valuable research tool for studying serotonin receptor pharmacology and the role of 5-HT2C receptors in anxiety, depression, and other neuropsychiatric disorders.
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| Toxicity/Toxicokinetics |
RS-102221 HCl is a research compound and its full toxicological profile is not detailed in the available literature. As a selective 5-HT2C receptor antagonist, it has been used in animal studies at doses that produce behavioral effects without significant adverse effects reported. Standard safety precautions should be followed when handling the compound.
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| References |
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| Additional Infomation |
RS-102221 HCl (CAS#: 187397-18-8) is a selective 5-HT2C receptor antagonist with a Ki of 10 nM and nearly 100-fold selectivity over 5-HT2A and 5-HT2B receptors. It has pKi values of 8.4 and 8.5 for human and rat 5-HT2C, respectively. RS-102221 HCl reduces anxiety in the light-dark test and reduces startle response in mice at 2 mg/kg. It is a valuable research tool for studying 5-HT2C receptor function.
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| Molecular Formula |
C27H32CLF3N4O7S
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| Molecular Weight |
649.08
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| Exact Mass |
648.163
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| CAS # |
187397-18-8
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| Related CAS # |
RS-102221;185376-97-0
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| PubChem CID |
18931299
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
12
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
43
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| Complexity |
1080
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
SZJZEJZLRDIHPB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C27H31F3N4O7S.ClH/c1-40-22-16-23(41-2)20(33-42(38,39)18-8-6-17(7-9-18)27(28,29)30)15-19(22)21(35)5-3-4-12-34-13-10-26(11-14-34)24(36)31-25(37)32-26;/h6-9,15-16,33H,3-5,10-14H2,1-2H3,(H2,31,32,36,37);1H
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| Chemical Name |
N-[5-[5-(2,4-dioxo-1,3,8-triazaspiro[4.5]decan-8-yl)pentanoyl]-2,4-dimethoxyphenyl]-4-(trifluoromethyl)benzenesulfonamide;hydrochloride
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| Synonyms |
RS 102221 HCl RS102221 HCl RS-102221 HCl
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~192.58 mM)
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| 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 | 1.5406 mL | 7.7032 mL | 15.4064 mL | |
| 5 mM | 0.3081 mL | 1.5406 mL | 3.0813 mL | |
| 10 mM | 0.1541 mL | 0.7703 mL | 1.5406 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.
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