CyPPA is a positive modulator of hSK3 and hSK2 with EC50s of 14 μM and 5.6 μM, respectively. CyPPA is inactive against hSK1 and hIK channels.

Physicochemical Properties

Molecular Formula	C16H23N5
Molecular Weight	285.38732
Exact Mass	285.195
CAS #	73029-73-9
PubChem CID	909822
Appearance	White to off-white solid powder
Density	1.2±0.1 g/cm3
Boiling Point	512.2±42.0 °C at 760 mmHg
Flash Point	263.6±27.9 °C
Vapour Pressure	0.0±1.3 mmHg at 25°C
Index of Refraction	1.648
LogP	2.13
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	4
Rotatable Bond Count	3
Heavy Atom Count	21
Complexity	331
Defined Atom Stereocenter Count	0
InChi Key	USEMRPYUFJNFQN-UHFFFAOYSA-N
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)
Chemical Name	N-cyclohexyl-2-(3,5-dimethylpyrazol-1-yl)-6-methylpyrimidin-4-amine
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)

Biological Activity

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].
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].
References	[1]. Neurons, Inhibits Dopamine Release, and Counteracts Hyperdopaminergic Behaviors Induced by Methylphenidate. Br J Pharmacol. 2007 Jul;151(5):655-65. [2]. CyPPA, a positive modulator of small-conductance Ca(2+)-activated K(+) channels, inhibits phasic uterine contractions and delays preterm birth in mice. Am J Physiol Cell Physiol. 2011 Nov;301(5):C1027-35.

Solubility Data

Solubility (In Vitro)

DMSO : ~100 mg/mL (~350.40 mM)

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.