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Details

Stereochemistry ACHIRAL
Molecular Formula C14H12FN3O2
Molecular Weight 273.2624
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 1
Charge 0

SHOW SMILES / InChI
Structure of CO-102862

SMILES

NC(=O)N\N=C\C1=CC=C(OC2=CC=C(F)C=C2)C=C1

InChI

InChIKey=MHUUDVZSPFRUSK-RQZCQDPDSA-N
InChI=1S/C14H12FN3O2/c15-11-3-7-13(8-4-11)20-12-5-1-10(2-6-12)9-17-18-14(16)19/h1-9H,(H3,16,18,19)/b17-9+

HIDE SMILES / InChI

Molecular Formula C14H12FN3O2
Molecular Weight 273.2624
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 1
Optical Activity NONE

CO-102862, also known as V102862, is a potent, broad-spectrum state-dependent blocker of mammalian voltage-gated sodium channels. A key feature of the mechanism of inhibition is that V102862 has up to 80-fold higher affinity for inactivated Na channels as compared to channels in resting states. V102862 is an orally active anticonvulsant with robust activity in a variety of rodent models of epilepsy.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
360.0 nM [Ki]
180.0 nM [Ki]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Unknown

Approved Use

Unknown
PubMed

PubMed

TitleDatePubMed
In vivo metabolism and mass balance of 4-[4-fluorophenoxy]benzaldehyde semicarbazone in rats.
2000 Oct
V102862 (Co 102862): a potent, broad-spectrum state-dependent blocker of mammalian voltage-gated sodium channels.
2005 Mar
Functional and pharmacological properties of human and rat NaV1.8 channels.
2009 Apr
Patents

Patents

Sample Use Guides

In an experimental rat model of peripheral neuropathic pain, CO-102862 demonstrated marked antiallodynic effects, producing dose-dependent reversals of tactile sensitivity at oral doses ≥2.5 mg/kg (plasma levels of 480 ng/ml) in a 10% Tween 80 formulation.
Route of Administration: Oral
CO-102862 (V102862) was a potent state-dependent blocker of rNa(v)1.2 channels with a K(I) of approximately 0.4 uM and K(R) approximately 30 uM. V102862 binding to inactivated channels was relatively slow (k(+) approximately = 1.7 uM(-1) s(-1)).
Substance Class Chemical
Created
by admin
on Sat Dec 16 09:23:14 GMT 2023
Edited
by admin
on Sat Dec 16 09:23:14 GMT 2023
Record UNII
0KN11H90GF
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
CO-102862
Common Name English
4-(4-FLUOROPHENOXY)BENZALDEHYDE SEMICARBAZONE
Systematic Name English
V-102862
Code English
2-((4-(4-FLUOROPHENOXY)PHENYL)METHYLENE)HYDRAZINECARBOXAMIDE
Systematic Name English
HYDRAZINECARBOXAMIDE, 2-((4-(4-FLUOROPHENOXY)PHENYL)METHYLENE)-
Systematic Name English
Code System Code Type Description
FDA UNII
0KN11H90GF
Created by admin on Sat Dec 16 09:23:14 GMT 2023 , Edited by admin on Sat Dec 16 09:23:14 GMT 2023
PRIMARY
EPA CompTox
DTXSID70171079
Created by admin on Sat Dec 16 09:23:14 GMT 2023 , Edited by admin on Sat Dec 16 09:23:14 GMT 2023
PRIMARY
PUBCHEM
9816959
Created by admin on Sat Dec 16 09:23:14 GMT 2023 , Edited by admin on Sat Dec 16 09:23:14 GMT 2023
PRIMARY
CAS
181144-66-1
Created by admin on Sat Dec 16 09:23:14 GMT 2023 , Edited by admin on Sat Dec 16 09:23:14 GMT 2023
PRIMARY
Related Record Type Details
ACTIVE MOIETY