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
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+
| 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.
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL4296 Sources: https://www.ncbi.nlm.nih.gov/pubmed/20709552 |
360.0 nM [Ki] | ||
Target ID: CHEMBL2072 Sources: https://www.ncbi.nlm.nih.gov/pubmed/14998340 |
180.0 nM [Ki] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | Unknown Approved UseUnknown |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Functional and pharmacological properties of human and rat NaV1.8 channels. | 2009-04 |
|
| V102862 (Co 102862): a potent, broad-spectrum state-dependent blocker of mammalian voltage-gated sodium channels. | 2005-03 |
|
| In vivo metabolism and mass balance of 4-[4-fluorophenoxy]benzaldehyde semicarbazone in rats. | 2000-10 |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/11129068
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
Sources: https://www.ncbi.nlm.nih.gov/pubmed/15778702
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
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0KN11H90GF
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