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212631-61-3

212631-61-3 structure
212631-61-3 structure
  • Name: PD 198306
  • Chemical Name: N-(cyclopropylmethoxy)-3,4,5-trifluoro-2-(4-iodo-2-methylanilino)benzamide
  • CAS Number: 212631-61-3
  • Molecular Formula: C18H16F3IN2O2
  • Molecular Weight: 476.23200
  • Catalog: Signaling Pathways MAPK/ERK Pathway MEK
  • Create Date: 2017-01-31 03:54:32
  • Modify Date: 2024-01-12 18:13:52
  • PD 198306 is a selective MAPK/ERK-kinase (MEK) inhibitor. PD 198306 results in an observable reduction in the Streptozocin induced increase in the level of active ERK1 and 2. Antihyperalgesic effects[1].

Name N-(cyclopropylmethoxy)-3,4,5-trifluoro-2-(4-iodo-2-methylanilino)benzamide
Synonyms hms3269f09
hms3229h15
PD 198306
Description PD 198306 is a selective MAPK/ERK-kinase (MEK) inhibitor. PD 198306 results in an observable reduction in the Streptozocin induced increase in the level of active ERK1 and 2. Antihyperalgesic effects[1].
Related Catalog
Target

MEK

In Vitro PD198306 significantly inhibits Tha-GFP replication by 25% at 10 μM, after 36 h[2]. PD198306 (5 μM) reduces Tha-Crimson replication significantly by 20% at 18 h but such a result could not be confirmed at 36 h[2]. Cell Cycle Analysis[2] Cell Line: Human induced pluripotent stem cells (iPSC) Concentration: 10  μM Incubation Time: 6  hours Result: Inhibited Tha-Crimson replication at 10 μM, reducing it by 30% at 18 h and 50% at 36 h.
In Vivo Intrathecal administration of PD 198306 (1-30 μg per 10 μL) dose-dependently (1-30 μg) blocks static allodynia in both the streptozocin and the chronic constriction injury (CCI) models of neuropathic pain[1]. Animal Model: Male Sprague Dawley rats (250-300 g) bearing neuropathic pain[1] Dosage: 1-30 μg per 10 μL and 3 mg per 100 μL (PD 198306 is suspended in cremophor:ethanol:water, 1 : 1 : 8.) Administration: Single doses of intrathecal (i.t.) or intraplantar (ipl) of PD 198306 (1-30 μg per 10 μL and 3 mg per 100 μL respectively Result: Intrathecal administration dose-dependently (1-30 μg) blocked static allodynia the streptozocin model of neuropathic pain. The minimum effective doses (MED) of 3 μg significantly blocked static allodynia 30 min after treatment. Both 10 μg and the highest dose used (30 μg) totally blocked the maintenance of static allodynia, for up to 1 h.
References

[1]. A Ciruela, et al. Identification of MEK1 as a novel target for the treatment of neuropathic pain. Br J Pharmacol. 2003 Mar;138(5):751-6.

[2]. Benoit Besson, et al. Kinome-Wide RNA Interference Screening Identifies Mitogen-Activated Protein Kinases and Phosphatidylinositol Metabolism as Key Factors for Rabies Virus Infection. mSphere. 2019 May 22;4(3):e00047-19.

Density 1.686g/cm3
Molecular Formula C18H16F3IN2O2
Molecular Weight 476.23200
Exact Mass 476.02100
PSA 50.36000
LogP 5.29580
Index of Refraction 1.631
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