Synonym
PF05020182; PF-05020182; PF 05020182; PF5020182; PF-5020182; PF 5020182.
IUPAC/Chemical Name
N-[4,6-Dimethoxy-2-(4-methoxy-1-piperidinyl)-5-pyrimidinyl]-3,3-dimethyl-butanamide
InChi Key
XHJMCIALHJMEBB-UHFFFAOYSA-N
InChi Code
InChI=1S/C18H30N4O4/c1-18(2,3)11-13(23)19-14-15(25-5)20-17(21-16(14)26-6)22-9-7-12(24-4)8-10-22/h12H,7-11H2,1-6H3,(H,19,23)
SMILES Code
CC(C)(C)CC(NC1=C(OC)N=C(N2CCC(OC)CC2)N=C1OC)=O
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Biological target:
PF05020182 is novel potent and selective Kv7.2/4 potassium channel opener.
In vitro activity:
PF-05020182 (2) demonstrated suitable properties for further testing in vivo where it dose-dependently decreased the number of animals exhibiting full tonic extension convulsions in response to corneal stimulation in the maximal electroshock (MES) assay. In addition, PF-05020182 (2) significantly inhibited convulsions in the MES assay at doses tested, consistent with in vitro activity measure.
Reference: Bioorg Med Chem Lett. 2015 Nov 1;25(21):4941-4944. https://pubmed.ncbi.nlm.nih.gov/25987375/
In vivo activity:
PF-05020182 (2) demonstrated suitable properties for further testing in vivo where it dose-dependently decreased the number of animals exhibiting full tonic extension convulsions in response to corneal stimulation in the maximal electroshock (MES) assay. In addition, PF-05020182 (2) significantly inhibited convulsions in the MES assay at doses tested, consistent with in vitro activity measure.
Reference: Bioorg Med Chem Lett. 2015 Nov 1;25(21):4941-4944. https://pubmed.ncbi.nlm.nih.gov/25987375/
Preparing Stock Solutions
The following data is based on the
product
molecular weight
366.46
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
Formulation protocol:
Davoren JE, Claffey MM, Snow SL, Reese MR, Arora G, Butler CR, Boscoe BP, Chenard L, DeNinno SL, Drozda SE, Duplantier AJ, Moine L, Rogers BN, Rong S, Schuyten K, Wright AS, Zhang L, Serpa KA, Weber ML, Stolyar P, Whisman TL, Baker K, Tse K, Clark AJ, Rong H, Mather RJ, Lowe JA 3rd. Discovery of a novel Kv7 channel opener as a treatment for epilepsy. Bioorg Med Chem Lett. 2015 Nov 1;25(21):4941-4944. doi: 10.1016/j.bmcl.2015.04.074. Epub 2015 May 1. PMID: 25987375.
In vitro protocol:
Davoren JE, Claffey MM, Snow SL, Reese MR, Arora G, Butler CR, Boscoe BP, Chenard L, DeNinno SL, Drozda SE, Duplantier AJ, Moine L, Rogers BN, Rong S, Schuyten K, Wright AS, Zhang L, Serpa KA, Weber ML, Stolyar P, Whisman TL, Baker K, Tse K, Clark AJ, Rong H, Mather RJ, Lowe JA 3rd. Discovery of a novel Kv7 channel opener as a treatment for epilepsy. Bioorg Med Chem Lett. 2015 Nov 1;25(21):4941-4944. doi: 10.1016/j.bmcl.2015.04.074. Epub 2015 May 1. PMID: 25987375.
In vivo protocol:
Davoren JE, Claffey MM, Snow SL, Reese MR, Arora G, Butler CR, Boscoe BP, Chenard L, DeNinno SL, Drozda SE, Duplantier AJ, Moine L, Rogers BN, Rong S, Schuyten K, Wright AS, Zhang L, Serpa KA, Weber ML, Stolyar P, Whisman TL, Baker K, Tse K, Clark AJ, Rong H, Mather RJ, Lowe JA 3rd. Discovery of a novel Kv7 channel opener as a treatment for epilepsy. Bioorg Med Chem Lett. 2015 Nov 1;25(21):4941-4944. doi: 10.1016/j.bmcl.2015.04.074. Epub 2015 May 1. PMID: 25987375.
1: Davoren JE, Claffey MM, Snow SL, Reese MR, Arora G, Butler CR, Boscoe BP,
Chenard L, DeNinno SL, Drozda SE, Duplantier AJ, Moine L, Rogers BN, Rong S,
Schuyten K, Wright AS, Zhang L, Serpa KA, Weber ML, Stolyar P, Whisman TL, Baker
K, Tse K, Clark AJ, Rong H, Mather RJ, Lowe JA 3rd. Discovery of a novel Kv7
channel opener as a treatment for epilepsy. Bioorg Med Chem Lett. 2015 Nov
1;25(21):4941-4. doi: 10.1016/j.bmcl.2015.04.074. Epub 2015 May 1. PubMed PMID:
25987375.
