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

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.

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GW274150 Chemical Structure

GW274150 Chemical Structure

CAS No. : 210354-22-6

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Solid + Solvent
10 mM * 1 mL in Water
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10 mg USD 150 In-stock
25 mg USD 310 In-stock
50 mg USD 500 In-stock
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Based on 2 publication(s) in Google Scholar

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GW274150 Related Antibodies

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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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

GW274150 Related Antibodies
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Appearance

Solid

Color

White to off-white

SMILES

N[C@@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: 

DMSO : 100 mg/mL (456.00 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : ≥ 62 mg/mL (282.72 mM)

*"≥" 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 4.5600 mL 22.7998 mL 45.5996 mL 113.9991 mL
5 mM 0.9120 mL 4.5600 mL 9.1199 mL 22.7998 mL
10 mM 0.4560 mL 2.2800 mL 4.5600 mL 11.3999 mL
15 mM 0.3040 mL 1.5200 mL 3.0400 mL 7.5999 mL
20 mM 0.2280 mL 1.1400 mL 2.2800 mL 5.7000 mL
25 mM 0.1824 mL 0.9120 mL 1.8240 mL 4.5600 mL
30 mM 0.1520 mL 0.7600 mL 1.5200 mL 3.8000 mL
40 mM 0.1140 mL 0.5700 mL 1.1400 mL 2.8500 mL
50 mM 0.0912 mL 0.4560 mL 0.9120 mL 2.2800 mL
60 mM 0.0760 mL 0.3800 mL 0.7600 mL 1.9000 mL
80 mM 0.0570 mL 0.2850 mL 0.5700 mL 1.4250 mL
100 mM 0.0456 mL 0.2280 mL 0.4560 mL 1.1400 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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GW274150 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GW274150210354-22-6GW 274150GW-274150NO SynthaseNitric oxide synthasesNOSiNOSlunginjuryacuteinflammationParkinsondiseaseasthmaInhibitorinhibitorinhibit

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