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| 5mg |
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| 25mg |
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CYM 9484 is a novel, potent and selective neuropeptide Y (NPY) Y2 receptor antagonist with an IC50 value of 19 nM.
| Targets |
Neuropeptide Y Y2 receptor (NPY Y2); IC50 = 19 nM [1];
Inactive at NPY Y1 receptor (highest tested concentration 10 μM) [1]. |
|---|---|
| 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]. |
| 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]. |
| Molecular Formula |
C₂₇H₃₁N₃O₃S₂MOLECULARWEIGHT
|
|---|---|
| Molecular Weight |
509.68
|
| Exact Mass |
509.181
|
| CAS # |
1383478-94-1
|
| PubChem CID |
66561564
|
| Appearance |
White to off-white solid powder
|
| LogP |
5.373
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
35
|
| Complexity |
767
|
| Defined Atom Stereocenter Count |
0
|
| 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) |
DMSO : ~50.97 mg/mL (~100.00 mM)
|
|---|---|
| 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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