Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C18H16F3IN2O2 |
| Molecular Weight | 476.2315 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1=CC(I)=CC=C1NC2=C(F)C(F)=C(F)C=C2C(=O)NOCC3CC3
InChI
InChIKey=UHAXDAKQGVISBZ-UHFFFAOYSA-N
InChI=1S/C18H16F3IN2O2/c1-9-6-11(22)4-5-14(9)23-17-12(7-13(19)15(20)16(17)21)18(25)24-26-8-10-2-3-10/h4-7,10,23H,2-3,8H2,1H3,(H,24,25)
DescriptionCurator's Comment: The description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/12642375 | https://encrypted.google.com/patents/WO1998037881A1 | http://www.google.com.na/patents/WO2001005390A3
Curator's Comment: The description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/12642375 | https://encrypted.google.com/patents/WO1998037881A1 | http://www.google.com.na/patents/WO2001005390A3
PD-198306 is a cell-permeable, amino-benzamide derivative that acts as a potent and non-ATP-competitive inhibitor of MEK1/2 with an excellent selectivity over ERK, c-Src, Cdk's, and phosphatidylinositol 3-kinase γ. In vitro PD-198306 inhibits MEK activity in synovial fibroblasts at concentrations of 30–100 nM, depending on the species. PD 198306 has a bioavailability of 62% when taken orally and is active in several animal models of rheumatoid arthritis, including rat streptococcal cell wall-induced arthritis and rat adjuvant arthritis. PD 198306 can partially decrease the development of some of the structural changes in experimental osteoarthritis model. PD 198306 dose-dependently blocked static allodynia in both the streptozocin and the chronic constriction injury (CCI) models of neuropathic pain. The antihyperalgesic effects of PD 198306, in both the streptozocin and CCI models of neuropathic pain, correlated with a reduction in the elevated levels of active ERK1 and 2 in a lumbar spinal cord.
Originator
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| Cannabinoid receptor agonists upregulate and enhance serotonin 2A (5-HT(2A)) receptor activity via ERK1/2 signaling. | 2013-03 |
|
| Cannabinoid agonists increase the interaction between β-Arrestin 2 and ERK1/2 and upregulate β-Arrestin 2 and 5-HT(2A) receptors. | 2013-02 |
|
| Cannabinoid-induced enhanced interaction and protein levels of serotonin 5-HT(2A) and dopamine D₂ receptors in rat prefrontal cortex. | 2012-10 |
|
| Identification of MEK1 as a novel target for the treatment of neuropathic pain. | 2003-03 |
Sample Use Guides
New Zealand male rabbits were treated with PD 198306 at dosages of 10 mg/kg/day or 30 mg/kg/day for 8 weeks.
PD 198306 was administered once daily at 8:00 AM as a liquid solution, by oral gavage into the stomach.
Route of Administration:
Oral
T47D cells were used for evaluation the effect of MEK inhibitor PD-198306 on ERK phosphorylation upon treatment with different doses of EGF. Cells were preincubated with PD 198306 (200 nM) for 30 min and stimulated with EGF (1 nM) for the 2, 5, 15, 30 ,45, 60, 90 and 120 min. Equal amounts of total cell lysates were resolved by NuPAGE and subjected to Multistrip Western blotting. Immunoblots (IBs) were probed with anti-phospho-p44/42 MAPK (ERK1/2) (labeled as p-ERK).
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DTXSID70433306
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9956637
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212631-61-3
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ACTIVE MOIETY
