| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
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| Targets |
CyPPA targets SK2 and SK3 channels, which are small-conductance calcium-activated potassium channels involved in regulating neuronal excitability. It acts as a positive allosteric modulator, enhancing the activity of these channels. By enhancing SK channel activity, it reduces the activity of dopaminergic neurons and inhibits dopamine release.
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| ln Vitro |
The apparent Ca2+ sensitivity of channel activation is increased concentration-dependently by CyPPA, resulting in a change in the EC50 (Ca2+) from 429 nM to 59 nM [1].
CyPPA is a positive modulator of SK2 and SK3 with EC50 values of 14 μM and 5.6 μM, respectively. It reduces the activity of dopaminergic neurons and inhibits dopamine release. It increases the duration of apamin-sensitive afterhyperpolarization. The compound has demonstrated significant effects on neuronal activity and inflammation. |
| ln Vivo |
CyPPA is a positive regulator of small-conductance Ca2+-activated K+ channels that can delay premature delivery in mice and decrease phasic contractions of the uterus [2].
CyPPA inhibits phasic uterine contractions and delays preterm birth in mice. It has demonstrated significant effects on neuronal activity and inflammation, making it a candidate for therapeutic interventions in neurological disorders. It is valuable for studying disorders such as epilepsy, anxiety, and neurodegeneration. |
| Enzyme Assay |
CyPPA is evaluated in cell-free assays for its ability to modulate SK channel activity. However, specific enzymatic or receptor binding assays are not well-documented. The compound's purity and identity can be confirmed using HPLC and NMR analysis.
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| Cell Assay |
CyPPA is assessed in cell-based electrophysiological assays using neurons or cells expressing SK2 and SK3 channels. The compound's ability to enhance SK channel activity is measured by assessing its effects on afterhyperpolarization and neuronal firing. EC50 values are determined.
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| Animal Protocol |
CyPPA is administered in animal models to evaluate its effects on neurological disorders and preterm birth. It inhibits phasic uterine contractions and delays preterm birth in mice. It is also studied in models of epilepsy, anxiety, and neurodegeneration.
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| ADME/Pharmacokinetics |
CyPPA has a molecular weight of 285.39 and a molecular formula of C16H23N5. It has a CAS number of 73029-73-9. The compound should be stored as a powder at -20°C for long-term stability. It is soluble in DMSO.
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| Toxicity/Toxicokinetics |
No detailed toxicity data is available for CyPPA. The compound is for research use only and is not intended for human therapeutic use. Its safety profile has not been extensively characterized in the available literature.
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| References |
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| Additional Infomation |
CyPPA is a selective positive allosteric modulator of SK2 and SK3 channels. It has a CAS number of 73029-73-9. It is used as a research tool to study the role of SK channels in neuronal excitability, dopamine release, and various neurological and reproductive disorders. It is not approved for clinical use.
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| Molecular Formula |
C16H23N5
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|---|---|
| Molecular Weight |
285.38732
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| Exact Mass |
285.195
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| CAS # |
73029-73-9
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| PubChem CID |
909822
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
512.2±42.0 °C at 760 mmHg
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| Flash Point |
263.6±27.9 °C
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| Vapour Pressure |
0.0±1.3 mmHg at 25°C
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| Index of Refraction |
1.648
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| LogP |
2.13
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
21
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| Complexity |
331
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
USEMRPYUFJNFQN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H23N5/c1-11-10-15(18-14-7-5-4-6-8-14)19-16(17-11)21-13(3)9-12(2)20-21/h9-10,14H,4-8H2,1-3H3,(H,17,18,19)
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| Chemical Name |
N-cyclohexyl-2-(3,5-dimethylpyrazol-1-yl)-6-methylpyrimidin-4-amine
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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 : ~100 mg/mL (~350.40 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.76 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 25.0 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.76 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.5040 mL | 17.5199 mL | 35.0398 mL | |
| 5 mM | 0.7008 mL | 3.5040 mL | 7.0080 mL | |
| 10 mM | 0.3504 mL | 1.7520 mL | 3.5040 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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