| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Neuropeptide Y Y2 receptor (NPY Y2); IC50 = 19 nM [1];
Inactive at NPY Y1 receptor (highest tested concentration 10 μM) [1]. Neuropeptide Y (NPY) Y2 receptor - selective, highly potent antagonist (IC50 = 19 nM). |
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| ln Vitro |
SF-11 is a selective antagonist of the NPY Y2 receptor that penetrates the brain with an IC50 of 190 nM. After a thorough investigation of the hit chemical SF-11's surface area receptor (SAR), the effective and selective small molecule CYM 9484 (compound 16), an antagonist of the NPY Y2 receptor, was discovered. Ten times as powerful as the popular chemical SF-11 is CYM 9484. CYM 9484 is synthesized by reacting several aryl isothiocyanates with α,α-diphenylpiperidinyl-4-methanol [1].
CYM 9484 exhibited potent antagonist activity at the NPY Y2 receptor with an IC50 value of 19 nM in a cAMP biosensor assay [1]; The compound showed no activity at the NPY Y1 receptor up to 10 μM [1]; It is selective against NPY Y1 and 38 off-target receptors including GPCRs, transporters and ion-channels (based on the hit chemotype SF-11 from which CYM 9484 was derived) [1]. In vitro studies demonstrate that CYM 9484 is a selective and highly potent antagonist of the NPY Y2 receptor with an IC50 of approximately 19 nM. The compound effectively blocks Y2 receptor-mediated signaling, preventing the activation of downstream pathways by NPY or other Y2 receptor agonists. The NPY Y2 receptor is a G protein-coupled receptor that plays important roles in the regulation of food intake, anxiety, mood, and neuroendocrine function. By selectively antagonizing the Y2 receptor, CYM 9484 allows researchers to study the specific role of this receptor in various physiological and pathological processes. |
| ln Vivo |
In vivo studies on CYM 9484 are limited, as the compound is primarily used as a research tool for in vitro investigations of NPY Y2 receptor function. The compound's potent and selective antagonism of the Y2 receptor suggests potential applications in studying appetite regulation, where Y2 receptor activation is known to stimulate food intake. The compound may also be useful for studying anxiety and mood disorders, as the NPY system is implicated in the regulation of these processes. Further studies are needed to assess the compound's pharmacokinetic properties, brain penetration, and efficacy in animal models of eating disorders, anxiety, and depression.
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| Enzyme Assay |
For receptor binding studies, competitive binding assays are performed using membrane preparations from cells expressing the NPY Y2 receptor. Membranes are incubated with a radiolabeled Y2 receptor ligand (e.g., [125I]-PYY3-36) and varying concentrations of CYM 9484. Bound radioactivity is separated by filtration and measured by scintillation counting. Binding affinity (IC50) is calculated from competition curves by non-linear regression analysis. For functional studies, cells expressing Y2 receptors are treated with CYM 9484 and stimulated with a Y2 agonist (e.g., NPY or PYY3-36), and downstream signaling is measured by cAMP accumulation (inhibition) or other signaling readouts.
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| Cell Assay |
Cellular assays for CYM 9484 typically involve culturing cells that express the NPY Y2 receptor, such as recombinant cell lines or neuronal cell lines. Cells are treated with the compound at various concentrations and stimulated with a Y2 agonist. Receptor activation is assessed by measuring inhibition of cAMP accumulation using ELISA or HTRF-based cAMP assays, or by measuring other downstream signaling events such as calcium mobilization or ERK phosphorylation. The compound's ability to block agonist-induced signaling is quantified, and IC50 values are calculated. Selectivity over other NPY receptors (Y1, Y4, Y5) and other GPCRs is assessed using similar assay formats to confirm the compound's specificity for Y2.
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| Animal Protocol |
In vivo efficacy of CYM 9484 is evaluated in animal models relevant to NPY Y2 receptor function, such as models of feeding behavior, anxiety, and mood disorders. For feeding studies, mice or rats are treated with CYM 9484 via intracerebroventricular or peripheral administration, and food intake is measured. For anxiety studies, behavioral tests such as the elevated plus maze, open field test, or light-dark box are used. For mood disorders, models of depression such as the forced swim test or tail suspension test are used. The compound's ability to modulate Y2 receptor-mediated behaviors is assessed. Pharmacokinetic studies are conducted to determine the compound's bioavailability and brain penetration.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of CYM 9484 have been characterized to support its use as a research tool. The compound has a molecular weight of 509.68 and the molecular formula C27H31N3O3S2. Key PK parameters including half-life, clearance, volume of distribution, and bioavailability are determined using LC-MS/MS analysis of plasma and brain tissue samples following administration. The compound's ability to cross the blood-brain barrier is essential for studying central nervous system targets such as the NPY Y2 receptor. The compound should be stored as a powder at -20°C.
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| Toxicity/Toxicokinetics |
Toxicological evaluation of CYM 9484 is typically conducted in parallel with efficacy studies in animal models. Standard toxicology assessments include in vitro cytotoxicity assays against a panel of mammalian cell lines to determine the compound's selectivity index. In vivo toxicity studies in rodents include acute and repeated-dose toxicity testing, observation of clinical signs and body weight changes, and histopathological examination of major organs including the brain. As a Y2 receptor antagonist that modulates NPY signaling, potential effects on feeding behavior, mood, and neuroendocrine function are carefully monitored.
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| References | |
| Additional Infomation |
CYM 9484 is a thiourea analogue (4-substituted phenyl ring with N,N-dimethyl sulfonamide group) derived from hit SF-11 [1];
It was synthesized by coupling α,α-diphenylpiperidino-4-methanol with 4-isothiocyanato-N,N-dimethylbenzenesulfonamide [1]; The compound represents one of the two most potent NPY Y2 antagonists identified in this study (the other being CYM 9552 with IC50 = 12 nM) [1]; Further investigation of in vivo pharmacokinetics and lead optimization was planned but not reported in this paper [1]. CYM 9484 is a research tool compound used for studying the role of the NPY Y2 receptor in neurobiology, appetite regulation, and anxiety or mood disorders. The compound is not approved for clinical use and is intended for laboratory research purposes only. Its mechanism of action involves selective and potent antagonism of the NPY Y2 receptor, which blocks Y2 receptor-mediated signaling and allows researchers to study the specific role of this receptor in various physiological and pathological processes. This compound is valuable for validating the Y2 receptor as a therapeutic target for eating disorders, anxiety, and depression, and for investigating the role of NPY signaling in neurobiology. |
| Molecular Formula |
C₂₇H₃₁N₃O₃S₂MOLECULARWEIGHT
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|---|---|
| Molecular Weight |
509.68
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| Exact Mass |
509.181
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| CAS # |
1383478-94-1
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| PubChem CID |
66561564
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| Appearance |
White to off-white solid powder
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| LogP |
5.373
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
35
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| Complexity |
767
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| Defined Atom Stereocenter Count |
0
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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 : ~50.97 mg/mL (~100.00 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.08 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.08 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.08 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9620 mL | 9.8101 mL | 19.6202 mL | |
| 5 mM | 0.3924 mL | 1.9620 mL | 3.9240 mL | |
| 10 mM | 0.1962 mL | 0.9810 mL | 1.9620 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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