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| 25mg |
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Purity: ≥98%
GW9662 (GW-9662; GW 9662) is an irreversible and selective inhibitor of PPAR (peroxisome proliferator-activated receptor) with potential anticancer activity. It inhibits PPARγ with an IC50 of 3.3 nM in a cell-free assay, and shows >100-fold selectivity for PPARγ over PPARα and PPARδ. GW9662 prevented activation of PPARgamma and inhibited growth of human mammary tumour cell lines. GW9662 may permit use of anti-ER strategies to inhibit breast cancer in ER- patients. GW9662 suppresses the cell viability with IC50 values ranging from 20-30μM.
| ln Vitro |
GW9662 has the ability to suppress radioligand binding to PPARγ, PPARα, and PPARδ, with corresponding pIC50 values of 8.48±0.27 (IC50=3.3 nM; n = 10), 7.49±0.17 (IC50=32 nM; n = 9), and 5.69±0.17 (IC50=2000 nM; n = 3). The binding studies with PPARα and PPARδ show that GW9662 is 10- and 600-fold less effective, respectively, with a nanomolar IC50 against PPARγ. GW9662 effectively and selectively blocks full-length PPARγ in cell-based reporter assays[1]. When paired with either 50 μM BRL 49653 (P=0.001) or 10 μM GW9662 (P=0.01) alone, co-treatment with both 50 μM BRL 49653 and 10 μM GW9662 leaves a significantly less number of viable cells after 7 days[2].
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| ln Vivo |
Both BADGE- and GW9662(1 mg/kg, ip)-treated mice had significantly greater bone marrow (BM) nucleated cell counts than the aplastic anemia (AA) group[3]. In rats, GW9662 (1 mg/kg, ip) significantly reduces the renoprotective benefits of lipopolysaccharide (LPS)[4].
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| References |
[1]. Leesnitzer LM, et al. Functional consequences of cysteine modification in the ligand binding sites of peroxisome proliferator activated receptors by GW9662. Biochemistry. 2002 May 28;41(21):6640-50.
[2]. Seargent JM, et al. GW9662, a potent antagonist of PPARgamma, inhibits growth of breast tumor cells and promotes the anticancer effects of the PPARgamma agonist BRL 49653, independently of PPARgamma activation. Br J Pharmacol. 2004 Dec;143(8):933-7. [3]. Sato K, et al. PPARγ antagonist attenuates mouse immune-mediated bone marrow failure by inhibition of T cell function.Haematologica. 2016 Jan;101(1):57-67. [4]. Collino M, et al. The selective PPARgamma antagonist GW9662 reverses the protection of LPS in a model of renal ischemia-reperfusion. Kidney Int. 2005 Aug;68(2):529-36 |
| Molecular Formula |
C13H9CLN2O3
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|---|---|
| Molecular Weight |
276.68
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| CAS # |
22978-25-2
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| Related CAS # |
GW9662-d5;2117730-84-2
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| SMILES |
O=C(NC1=CC=CC=C1)C2=CC([N+]([O-])=O)=CC=C2Cl
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| InChi Key |
DNTSIBUQMRRYIU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H9ClN2O3/c14-12-7-6-10(16(18)19)8-11(12)13(17)15-9-4-2-1-3-5-9/h1-8H,(H,15,17)
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| Chemical Name |
2-Chloro-5-nitro- N -phenylbenzamide
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| Synonyms |
GW-9662; GW 9662; GW9662;
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.04 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (9.04 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: ≥ 0.5 mg/mL (1.81 mM) (saturation unknown) in 1% DMSO 99% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 1% DMSO+30% polyethylene glycol+1% Tween 80: 30mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.6143 mL | 18.0714 mL | 36.1428 mL | |
| 5 mM | 0.7229 mL | 3.6143 mL | 7.2286 mL | |
| 10 mM | 0.3614 mL | 1.8071 mL | 3.6143 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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Effect of GW9662 on urine flow subsequent to I/R in rats pretreated with lipopolysaccharide.Kidney Int.2005 Aug;68(2):529-36. |
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