GW274150 |
| Catalog No.GC31673 |
GW274150 es un inhibidor potente, selectivo, activo por vÍa oral y dependiente de NADPH de la Óxido nÍtrico sintasa inducible humana (iNOS) (IC50 = 2,19 μM; Kd = 40 nM) y de iNOS de rata (ED50 = 1,15 μM).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 210354-22-6
Sample solution is provided at 25 µL, 10mM.
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GW274150 is a novel arginine-competitive, NADPH-dependent iNOS inhibitor that has been identified from a series of acetamide amino acids that have a high selectivity for iNOS vs both eNOS (> 260-fold) and nNOS (> 219-fold) and high bioavailability (> 90%) after oral administration.Target: iNOSin vivo: GW274150 demonstrates a narrow neuroprotective therapeutic window against the toxic actions of 6-OHDA. GW274150 administration leads to a dose-dependent decrease in the number of iNOS-positive cells in the SNc of the 6-OHDA-lesioned animals. The iNOS inhibitor GW274150 fails to produce long-term neuroprotection after its withdrawal in the 6-OHDA-lesioned rat. [1]
[1]. 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. [2]. Seymour M, et al. Ultrasonographic measures of synovitis in an early phase clinical trial: a double-blind, randomised, placebo and comparator controlled phase IIa trial of GW274150 (a selective inducible nitric oxide synthase inhibitor) in rheumatoid arthritis. Clin Exp Rheumatol. 2012 Mar-Apr;30(2):254-61.
| Cas No. | 210354-22-6 | SDF | |
| Canonical SMILES | N[C@@H](CCSCCNC(C)=N)C(O)=O | ||
| Formula | C8H17N3O2S | M.Wt | 219.3 |
| Solubility | Water : ≥ 62 mg/mL (282.72 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 4.56 mL | 22.7998 mL | 45.5996 mL |
| 5 mM | 0.912 mL | 4.56 mL | 9.1199 mL |
| 10 mM | 0.456 mL | 2.28 mL | 4.56 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 29 reference(s) in Google Scholar.)
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