KLYP961
KLYP961 is a selective and orally active dual inhibitor of inducible and neuronal NO synthase (IC50 = 50-400 nM). KLYP961 can inhibit endotoxin-evoked plasma nitrates increases and attenuate pain behaviors in a mouse formalin model. KLYP961 can attenuate carrageenin-induced edema and inflammatory hyperalgesia and writhing response elicited by Phenylbenzoquinone (HY-W275039). KLYP961 can be used for the research of neurological disease.
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- CAS No.: 1125746-49-7
- Formule: C19H15F2N5O
- Masse moléculaire:367.35
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
Description
IC50 & Target
[1]|
iNOS |
nNOS |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
0.091 μM
Compound: 42
|
Inhibition of human iNOS expressed in HEK293 cells assessed as inhibition of nitric oxide production after 18 hrs using 2,3-diaminonaphthalene by fluorescence assay
Inhibition of human iNOS expressed in HEK293 cells assessed as inhibition of nitric oxide production after 18 hrs using 2,3-diaminonaphthalene by fluorescence assay
|
[PMID: 20931971] |
| HEK293 | EC50 |
0.3 μM
Compound: 42
|
Inhibition of human nNOS expressed in HEK293 cells assessed as inhibition ionomycin induced nitric oxide production incubated for 24 hrs measured after 18 hrs of ionomycin challenge using 2,3-diaminonaphthalene by fluorescence assay
Inhibition of human nNOS expressed in HEK293 cells assessed as inhibition ionomycin induced nitric oxide production incubated for 24 hrs measured after 18 hrs of ionomycin challenge using 2,3-diaminonaphthalene by fluorescence assay
|
[PMID: 20931971] |
| HEK293 | EC50 |
0.43 μM
Compound: 42
|
Inhibition of mouse iNOS expressed in HEK293 cells assessed as inhibition of nitric oxide production after 18 hrs using 2,3-diaminonaphthalene by fluorescence assay
Inhibition of mouse iNOS expressed in HEK293 cells assessed as inhibition of nitric oxide production after 18 hrs using 2,3-diaminonaphthalene by fluorescence assay
|
[PMID: 20931971] |
| HEK293 | EC50 |
16.5 μM
Compound: 42
|
Inhibition of human eNOS expressed in HEK293 cells assessed as inhibition A23187 induced nitric oxide production incubated for 24 hrs measured after 18 hrs of ionomycin challenge using 2,3-diaminonaphthalene by fluorescence assay
Inhibition of human eNOS expressed in HEK293 cells assessed as inhibition A23187 induced nitric oxide production incubated for 24 hrs measured after 18 hrs of ionomycin challenge using 2,3-diaminonaphthalene by fluorescence assay
|
[PMID: 20931971] |
| HEK293 | IC50 |
0.091 μM
Compound: 5, KD7332, KLYP961
|
Inhibition of human iNOS expressed in HEK293 cells assessed as NO production by 2,3-diaminonapthalene-based fluorescence assay
Inhibition of human iNOS expressed in HEK293 cells assessed as NO production by 2,3-diaminonapthalene-based fluorescence assay
|
[PMID: 22182498] |
Chemical Information
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CAS No. 1125746-49-7
-
Masse moléculaire 367.35
-
Formule C19H15F2N5O
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SMILES
O=C1C=C(CN2C3=C(N=C2C4CCC4)N=CC=N3)C5=C(N1)C(F)=C(F)C=C5
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)