Product Name :
Vinyl-L-NIO (hydrochloride)
Description:
IC50: 100 nM, 12 and 60 μM for nNOS, eNOS, and iNOS, respectively Vinyl-L-NIO is a potent and selective inhibitor of nNOS. Nitric oxide synthase (NOS) catalyzes the NADPH- and O2-dependent conversion of L-arginine to nitric oxide (NO) and citrulline. Three isoforms including the neuronal (nNOS), endothelial, and inducible have currently been identified. Since NO overproduction is able to contribute to various pathophysiological conditions, NOS inhibitors are considered as potential therapeutic agents. In vitro: Vinyl-L-NIO was identified as a potent and selective inhibitor of nNOS. The Ki values for inhibition of nNOS, eNOS, and iNOS are 100 nM, 12 and 60 μM, respectively, as determined using initial rate measurements. Moreove, vinyl-L-NIO could irreversibly inactivate nNOS with a kinact of 0.078 min-1 and a Ki value of 90 nM in the presence of NADPH and O2. In additioin, it was found that vinyl-L-NIO was not able to inactivate iNOS and eNOS needed 20-fold higher concentrations of vinyl-L-NIO to achive 75% the rate of inactivation seen with nNOS . In vivo: Vinyl-L-NIO was intracerebroventricularly injected at a dose of 10 microg/rat just before intraperitoneal injection of LPS. Vinyl-L-NIO injected at a selected doses had no effect on normal day-time body temperature and normal night-time. Vinyl-L-NIO at a dose of 10 microg/animal could suppress the LPS-induced fever in rats. The fever index calculated for rats pretreated with vinyl-L-NIO was reduced by 43%, compared to that calculated for water-pretreated and LPS-injected rats . Clinical trial: So far, no clinical study has been conducted.
CAS:
728944-69-2
Molecular Weight:
235.71
Formula:
C9H18ClN3O2
Chemical Name:
(2S)-2-amino-5-(but-3-enimidamido)pentanoic acid hydrochloride
Smiles :
Cl.{{Astemizole} web|{Astemizole} Potassium Channel|{Astemizole} TGF-beta/Smad|{Astemizole} Purity & Documentation|{Astemizole} References|{Astemizole} supplier} C=CCC(=N)NCCC[C@H](N)C(O)=O
InChiKey:
DIWIMDZKSYTKCZ-FJXQXJEOSA-N
InChi :
InChI=1S/C9H17N3O2.{{Afatinib dimaleate} MedChemExpress|{Afatinib dimaleate} p38 MAPK|{Afatinib dimaleate} Immunology/Inflammation|{Afatinib dimaleate} Biological Activity|{Afatinib dimaleate} Description|{Afatinib dimaleate} supplier} ClH/c1-2-4-8(11)12-6-3-5-7(10)9(13)14;/h2,7H,1,3-6,10H2,(H2,11,12)(H,13,14);1H/t7-;/m0.PMID:23805407 /s1
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
IC50: 100 nM, 12 and 60 μM for nNOS, eNOS, and iNOS, respectively Vinyl-L-NIO is a potent and selective inhibitor of nNOS. Nitric oxide synthase (NOS) catalyzes the NADPH- and O2-dependent conversion of L-arginine to nitric oxide (NO) and citrulline. Three isoforms including the neuronal (nNOS), endothelial, and inducible have currently been identified. Since NO overproduction is able to contribute to various pathophysiological conditions, NOS inhibitors are considered as potential therapeutic agents. In vitro: Vinyl-L-NIO was identified as a potent and selective inhibitor of nNOS. The Ki values for inhibition of nNOS, eNOS, and iNOS are 100 nM, 12 and 60 μM, respectively, as determined using initial rate measurements. Moreove, vinyl-L-NIO could irreversibly inactivate nNOS with a kinact of 0.078 min-1 and a Ki value of 90 nM in the presence of NADPH and O2. In additioin, it was found that vinyl-L-NIO was not able to inactivate iNOS and eNOS needed 20-fold higher concentrations of vinyl-L-NIO to achive 75% the rate of inactivation seen with nNOS . In vivo: Vinyl-L-NIO was intracerebroventricularly injected at a dose of 10 microg/rat just before intraperitoneal injection of LPS. Vinyl-L-NIO injected at a selected doses had no effect on normal day-time body temperature and normal night-time. Vinyl-L-NIO at a dose of 10 microg/animal could suppress the LPS-induced fever in rats. The fever index calculated for rats pretreated with vinyl-L-NIO was reduced by 43%, compared to that calculated for water-pretreated and LPS-injected rats . Clinical trial: So far, no clinical study has been conducted.|Product information|CAS Number: 728944-69-2|Molecular Weight: 235.71|Formula: C9H18ClN3O2|Chemical Name: (2S)-2-amino-5-(but-3-enimidamido)pentanoic acid hydrochloride|Smiles: Cl.C=CCC(=N)NCCC[C@H](N)C(O)=O|InChiKey: DIWIMDZKSYTKCZ-FJXQXJEOSA-N|InChi: InChI=1S/C9H17N3O2.ClH/c1-2-4-8(11)12-6-3-5-7(10)9(13)14;/h2,7H,1,3-6,10H2,(H2,11,12)(H,13,14);1H/t7-;/m0./s1|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|Products are for research use only. Not for human use.|
