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

GW274150 phosphate 

Cat. No.: HY-12119A
Handling Instructions

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.

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GW274150 phosphate Chemical Structure

GW274150 phosphate Chemical Structure

CAS No. : 438542-15-5

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10 mM * 1 mL in Water USD 330 In-stock
Estimated Time of Arrival: December 31
5 mg USD 300 In-stock
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10 mg USD 450 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1000 In-stock
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100 mg USD 1500 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

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[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 phosphate inhibits intracellular iNOS in J774 cells in a time-dependent manner, reaching IC50 values of 0.2±0.04 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 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)[2].
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[2].
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)[3].

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

317.30

Formula

C₈H₂₀N₃O₆PS

CAS No.

438542-15-5

SMILES

CC(NCCSCC[[email protected]](N)C(O)=O)=N.O=P(O)(O)O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

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

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1516 mL 15.7580 mL 31.5159 mL
5 mM 0.6303 mL 3.1516 mL 6.3032 mL
10 mM 0.3152 mL 1.5758 mL 3.1516 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 phosphate
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HY-12119A
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