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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

Description

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.

CNS Activity

Originator

Approval Year

Unknown
139594
Targets

Targets

Primary TargetPharmacologyConditionPotency
Blocker
537
 360.0 nM [Ki]
Blocker
537
 180.0 nM [Ki]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Phase I
428
Unknown

Approved Use

Unknown
Sourcing

Sourcing

Vendor/AggregatorIDURL
Alichem
250001667
http://www.alichem.com/en/products/181144-66-1.html
BePharm Ltd.
B234092
Oxchem Corporation
AX8234092
Smolecule
S524145
http://www.smolecule.com/products/s524145
THE BioTek
bt-264062
https://www.thebiotek.com/product/inhibitors/bt-264062
Tocris
2642
https://www.tocris.com/products/co-102862_2642
eNovation Chemicals
D675190
https://www.enovationchem.com/ProductDetails.asp?ProductID=D675190
PubMed

PubMed

TitleDatePubMed
Functional and pharmacological properties of human and rat NaV1.8 channels.
2009 Apr
Patents

Patents

6281211
1

Sample Use Guides

In Vivo Use Guide
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
In Vitro Use Guide
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
Structure of CO-102862
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