CyPPA

Product details

• Chemical name: N-Cyclohexyl-N-[2-(3,5-dimethyl-pyrazol-1-yl)-6-methyl-4-pyrimidinamine.
• CAS number: 73029-73-9
• Molecular formula: C16H23N5.
• Purity: >98%
• Concentration: 1-100 μM.
• Form: Lyophilized Powder
• Solubility: DMSO or ethanol. Centrifuge all product preparations before use (10000 x g 5 min).
• Reconstitution: DMSO or ethanol. Centrifuge all product preparations before use (10000 x g 5 min).
• Shipping: Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
• Target: KCa2.2, KCa2.3, TRPM7 channels
• Source: Synthetic
• Activity: CyPPA is an activator of small conductance Ca2+-activated K+ channels KCa2.2 (SK2) and KCa2.3 (SK3) with EC50 values of 5.6 and 14 μM for SK3 and SK2 respectively. It displays no activity at SK1 and intermediate conductance KCa (IK) channels1. CyPPA blocks TRPM7 channels2.

Peptide confirmation

Confirmed by amino acid analysis and mass spectrometry

Scientific background

Ca2+-activated potassium channels (KCa) are a group of 6/7-TM ion channels that selectively transport K+ ions across biological membranes. They are broadly classified into three subtypes: SK, IK and BK channels (small, intermediate and big conductance).Small-conductance Ca2+-activated K+ channels (SK channels) underlie the medium duration after hyperpolarization that follows single or trains of action potentials in many types of neurons. This family is composed of KCa2.1 (SK1), -2.2 (SK2), and -2.3 (SK3) isoforms, which are expressed differentially within the central nervous system (CNS)1,2.CyPPA is an activator of small conductance KCa channels that displays selectivity for SK2 and SK3 channels (EC50 values are 5.6 and 14 µM for SK3 and SK2 respectively and efficacy is 90% and 71% for hSK3 and hSK2, respectively)3. CyPPA displays no activity at SK1 and IK (KCa3.1) channels3.CyPPA is a tool for distinguishing SK2 and SK3 from SK1 and IK; no other agents distinguish these channels from one another. Therefore, it enriches the repertoire of tools available to test the hypothesis that SK channels may be targets for future CNS drugs4.CyPPA was found to block TRPM7 channels, demonstrating an overlap between pharmacological compounds acting on TRP and KCa channels5.

Lead time: 1-2 Business Days

Country of origin: Israel/IL

Applications key

Application key: FC- Flow cytometry, IFC- Indirect flow cytometry, IHC- Immunohistochemistry,LCI- Live cell imaging, Calcium imaging assay,Cell survival assay, Electrophysiology, Neurite outgrowth assay.

Bioassay tested: Yes

• SDS (PDF)

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