GW274150 phosphate

GW274150 phosphate is a potent, selective, orally active and NADPH-dependent inhibitor of human inducible nitric oxide synthase (iNOS) (IC50=2.19 μM; Kd=40 nM) and rat iNOS (ED50=1.15 μM). GW274150 phosphate displays less potency for both humans or rats endothelial NOS (eNOS) and neuronal NOS (nNOS). GW274150 phosphate exerts a protective role in an acute model of lung injury inflammation.

Product information

CAS Number: 438542-15-5

Molecular Weight: 316.29

Formula: C8H19N3O6PS

Chemical Name: 1-amino-3-({2-[(1-aminoethylidene)amino]ethyl}sulfanyl)-1-carboxypropyl; phosphoric acid

Smiles: CC(N)=NCCSCC[C](N)C(O)=O.OP(O)(O)=O |^1:9|

InChiKey: VNFWWRXSCKHPMN-UHFFFAOYSA-N

InChi: InChI=1S/C8H16N3O2S.H3O4P/c1-6(9)11-3-5-14-4-2-7(10)8(12)13;1-5(2,3)4/h2-5,10H2,1H3,(H2,9,11)(H,12,13);(H3,1,2,3,4)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: H2O : 100 mg/mL (315.16 mM; Need ultrasonic).

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

How to use

In Vitro:

GW274150 phosphate inhibits intracellular iNOS in J774 cells in a time-dependent manner, reaching IC50 values of 0.2±0.04 μM. GW274150 is >260-fold and 219-fold selective for iNOS against eNOS and nNOS in rat tissues, respectively. And it displays >100-fold and >80-fold for human iNOS against human eNOS and nNOS, respectively.

In Vivo:

GW274150 phosphate is a long-acting (5 h half‐life in rats) iNOS inhibitor and is able to inhibit LPS‐mediated increase in plasma NO2-, NO3- levels 14 h after single intraperitoneal dose (ED50=3 mg/kg). GW274150 phosphate (intraperitoneal injection; 2.5, 5, and 10 mg/kg; before carrageenan injection) reduces the degree of lung injury induced by carrageenan in a dose-related fashion. Oedema formation and PMNs infiltration in the pleural cavity are also significantly attenuated in a dose‐related manner in rats. GW274150 phosphate (oral adminstration; 30 mg/kg; twice daily; 7 days) leads to significant neuroprotection, however, it displays a bell-shaped neuroprotective profile, being ineffective at high doses in 6-OHDA rat model of Parkinson disease (PD).

Products are for research use only. Not for human use.