| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| ln Vitro |
GW274150 phosphate suppresses intracellular iNOS in J774 cells in a time-coupled manner with an IC50 value of 0.2 μM [1]. The selectivity of GW274150 phosphate for eNOS and nNOS in tissues is >260-fold and 219-fold, respectively. demonstrates selectivity for human eNOS and nNOS of >100- and >80-fold, respectively [1]
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| ln Vivo |
GW274150 Phosphate is an iNOS dye with a long half-life of five hours that can inhibit the increase in sodium NO2- and NO3- levels caused by LPS 14 hours after a single intraperitoneal dye (ED50=3 mg/kg) was administered. GW274150 Phosphate Salt (intraperitoneal injection; 2.5, 5 and 10 mg/kg; prior to carrageenan injection) decreased the degree of lung injury caused by carrageenan in a dose-related manner. Additionally, there was a considerable disruption in PMN respiration and formation that was dose-related [2]. In Parkinson's disease (PD), GW274150 phosphate (oral; 30 mg/kg; twice daily; 7 days) had a bell-shaped neuroprotective effect but yet produced notable neuroprotection. Ineffective in the 6-OHDA dosing model at large doses[3].
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| Animal Protocol |
Animal/Disease Models: SD rat[2]
Doses: 2.5, 5 and 10 mg/kg intraperitoneal (ip) injection of carrageenan injection 5 minutes before administration Experimental Results: Yes Carrageenan is protective against lung injury in an acute inflammatory model. |
| 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.
[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 [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. |
| Molecular Formula |
C₈H₂₀N₃O₆PS
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|---|---|
| Molecular Weight |
317.30
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| CAS # |
438542-15-5
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| Related CAS # |
GW274150;210354-22-6;GW274150 dihydrochloride;438542-17-7
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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| SMILES |
P(O)(O)(O)=O.C(CSCCNC(=N)C)[C@H](N)C(=O)O
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| Synonyms |
GW274150 phosphate; GW274150 phosphate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ~100 mg/mL (~315.16 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 12.5 mg/mL (39.39 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication (<60°C).
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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