1. Immunology/Inflammation
  2. NO Synthase
  3. GW274150

GW274150 

Cat. No.: HY-12119 Purity: 98.15%
Handling Instructions

GW274150 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 also displays less potency for both humans or rats endothelial NOS (eNOS) and neuronal NOS (nNOS). GW274150 exerts a protective role in an acute model of lung injury inflammation.

For research use only. We do not sell to patients.

GW274150 Chemical Structure

GW274150 Chemical Structure

CAS No. : 210354-22-6

Size Price Stock Quantity
10 mM * 1  mL in Water USD 362 In-stock
Estimated Time of Arrival: December 31
5 mg USD 300 In-stock
Estimated Time of Arrival: December 31
10 mg USD 450 In-stock
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25 mg USD 700 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1000 In-stock
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100 mg USD 1500 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

GW274150 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 also displays less potency for both humans or rats endothelial NOS (eNOS) and neuronal NOS (nNOS). GW274150 exerts a protective role in an acute model of lung injury inflammation[1][2].

IC50 & Target

Kd: 40 nM (iNOS)[1]
IC50: 2.19 μM (human iNOS); 544 μM (human eNOS); 177 μM (human nNOS)
ED50: 1.15 μM (rat iNOS); 252 μM (rat nNOS)[1]

In Vitro

GW274150 inhibits intracellular iNOS in J774 cells in a time-dependent manner, reaching IC50 values of 0.2 μM[1].
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[1].

In Vivo

GW274150 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)[2].
GW274150 (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[2].
GW274150 (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)[3].

Animal Model: SD-rat[2]
Dosage: 2.5, 5 and 10 mg/kg; single dose
Administration: Intraperitoneal injection 5 min before carrageenan injection
Result: Exerted a protective role in an acute model of inflammation, carrageenan-induced lung injury.
Clinical Trial
Molecular Weight

219.30

Formula

C₈H₁₇N₃O₂S

CAS No.

210354-22-6

SMILES

N[[email protected]@H](CCSCCNC(C)=N)C(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

H2O : ≥ 62 mg/mL (282.72 mM)

DMSO : < 1 mg/mL (insoluble or slightly soluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.5600 mL 22.7998 mL 45.5996 mL
5 mM 0.9120 mL 4.5600 mL 9.1199 mL
10 mM 0.4560 mL 2.2800 mL 4.5600 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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Keywords:

GW274150GW 274150GW-274150NO SynthaseNitric oxide synthasesNOSiNOSlunginjuryacuteinflammationParkinsondiseaseasthmaInhibitorinhibitorinhibit

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GW274150
Cat. No.:
HY-12119
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