Details
Stereochemistry | ACHIRAL |
Molecular Formula | C16H10ClF3N2O3 |
Molecular Weight | 370.71 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
OC1=CC=C(Cl)C=C1CN2N=C(OC2=O)C3=CC=C(C=C3)C(F)(F)F
InChI
InChIKey=QKOWACXSXTXRKA-UHFFFAOYSA-N
InChI=1S/C16H10ClF3N2O3/c17-12-5-6-13(23)10(7-12)8-22-15(24)25-14(21-22)9-1-3-11(4-2-9)16(18,19)20/h1-7,23H,8H2
BMS-191011, an opener of the cloned large-conductance, Ca2+-activated potassium (maxi-K) channel, demonstrated efficacy in in vivo stroke models, which led to its nomination as a candidate for clinical evaluation. Its maxi-K channel opening properties were consistent with its structural topology, being derived by combining elements from other known maxi-K openers. BMS-191011 demonstrated efficacy as an opener of the cloned large-conductance Ca2+-activated potassium (maxi-K) channel in in vivo stroke models
Originator
Sources: https://www.ncbi.nlm.nih.gov/pubmed/17266205
Curator's Comment: # Bristol-Myers Squibb
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL4304 Sources: https://www.ncbi.nlm.nih.gov/pubmed/17266205 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Primary | Unknown Approved UseUnknown |
PubMed
Title | Date | PubMed |
---|---|---|
Synthesis of water-soluble prodrugs of BMS-191011: a maxi-K channel opener targeted for post-stroke neuroprotection. | 2003 May 19 |
|
3-[(5-Chloro-2-hydroxyphenyl)methyl]-5-[4-(trifluoromethyl)phenyl ]-1,3,4-oxadiazol-2(3H)-one, BMS-191011: opener of large-conductance Ca(2+)-activated potassium (maxi-K) channels, identification, solubility, and SAR. | 2007 Feb 8 |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/21212534
Rats: BMS-191011 (10-100 µg/kg, i.v.) increased the diameter of retinal arterioles without altering systemic blood pressure and heart rate significantly.
Route of Administration:
Intravenous
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/27021102
Selective activator of BKCa BMS-191011 (10 uM) prevented the inhibitory
effects of IL-10 on hypoxia-induced decrease in population spikes (PS) amplitude of CA1 pyramidal neurons in rat hippocampal slices.
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ACTIVE MOIETY