Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C8H17N3O2S |
Molecular Weight | 219.304 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(=N)NCCSCC[C@H](N)C(O)=O
InChI
InChIKey=MOLOJNHYNHBPCW-ZETCQYMHSA-N
InChI=1S/C8H17N3O2S/c1-6(9)11-3-5-14-4-2-7(10)8(12)13/h7H,2-5,10H2,1H3,(H2,9,11)(H,12,13)/t7-/m0/s1
GW 274150 was developed by GlaxoSmithKline as a selective inhibitor of inducible nitric oxide synthase (iNOS; also known as NOS2). Nitric oxide synthase (NOS) is an important chemical involved in the production of NO. Reduction of NOS, and therefore NO, may be an effective technique for the treatment of migraine headache. GW 274150 offered the potential of anti-inflammatory activity in migraine through a novel mechanism of action. The drug has completed phase II of the clinical trials for patients with rheumatoid arthritis and migraine disorders. In addition, GW 274150 was involved in phase I clinical trial for patients with mild asthma. However, all these studied were discontinued.
Originator
Approval Year
PubMed
Title | Date | PubMed |
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Inhibition of inducible nitric oxide synthase by acetamidine derivatives of hetero-substituted lysine and homolysine. | 2000 Mar 20 |
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NOS-II is involved in early differentiation of murine cortical, retinal and ES cell-derived neurons-an immunocytochemical and functional approach. | 2002 Apr |
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Role of inducible nitric oxide synthase in the reduced responsiveness of the myocardium to catecholamines in a hyperdynamic, murine model of septic shock. | 2006 Feb |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://clinicaltrials.gov/ct2/show/NCT00370435
90mg GW274150 will be safe and well-tolerated in this adult and elderly RA patient population on methotrexate
Route of Administration:
Oral
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SUBSTANCE RECORD