GW274150 phosphate

Name: GW274150 phosphate
Brand: MedChemExpress
SKU: HY-12119A
Rating: 5.0 (2 reviews)

Cat. No.: HY-12119A Purity: 99.85%: FAQs
Data Sheet SDS COA Handling Instructions

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GW274150 phosphate is a potent, selective, orally active and NADPH-dependent inhibitor of human inducible nitric oxide synthase (iNOS) (IC₅₀=2.19 μM; K_d=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.

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

GW274150 phosphate Chemical Structure

CAS No. : 438542-15-5

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in Water ready for reconstitution	USD 99	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in Water	USD 99	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 90	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 150	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 310	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 500	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 800	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of GW274150 phosphate:

GW274150 In-stock
GW274150 dihydrochloride Get quote

2 Publications Citing Use of MCE GW274150 phosphate

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nNOS iNOS eNOS

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

iNOS

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].

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

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].

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
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

317.30

Formula

C₈H₂₀N₃O₆PS

CAS No.

438542-15-5

Appearance

Solid

Color

White to off-white

SMILES

CC(NCCSCC[C@H](N)C(O)=O)=N.O=P(O)(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 : 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

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.

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Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: PBS
Solubility: 12.5 mg/mL (39.39 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

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μL

Number of animals

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

Purity: 99.85%

Select Batch:

Data Sheet (276 KB) SDS (251 KB)

COA (247 KB) RP-HPLC (245 KB)

Handling Instructions (2659 KB)

References

[1]. Alderton WK, et al. GW274150 and GW273629 are potent and highly selective inhibitors of inducible nitric oxide synthase in vitro and in vivo.Br J Pharmacol. 2005 Jun;145(3):301-12. [Content Brief]

[2]. Dugo L, et al. Effects of GW274150, a novel and selective inhibitor of iNOS activity, in acute lung inflammation. Br J Pharmacol. 2004 Mar;141(6):979-87. Epub 2004 Feb [Content Brief]

[3]. Broom L, et al. Neuroprotection by the selective iNOS inhibitor GW274150 in a model of Parkinson disease.Free Radic Biol Med. 2011 Mar 1;50(5):633-40. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O	1 mM	3.1516 mL	15.7580 mL	31.5159 mL	78.7898 mL
	5 mM	0.6303 mL	3.1516 mL	6.3032 mL	15.7580 mL
	10 mM	0.3152 mL	1.5758 mL	3.1516 mL	7.8790 mL
	15 mM	0.2101 mL	1.0505 mL	2.1011 mL	5.2527 mL
	20 mM	0.1576 mL	0.7879 mL	1.5758 mL	3.9395 mL
	25 mM	0.1261 mL	0.6303 mL	1.2606 mL	3.1516 mL
	30 mM	0.1051 mL	0.5253 mL	1.0505 mL	2.6263 mL
	40 mM	0.0788 mL	0.3939 mL	0.7879 mL	1.9697 mL
	50 mM	0.0630 mL	0.3152 mL	0.6303 mL	1.5758 mL
	60 mM	0.0525 mL	0.2626 mL	0.5253 mL	1.3132 mL
	80 mM	0.0394 mL	0.1970 mL	0.3939 mL	0.9849 mL
	100 mM	0.0315 mL	0.1576 mL	0.3152 mL	0.7879 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.