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  • Product Name: GW-9662
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  • Purity: 98.0%
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Related CAS#:
22978-25-2 2117730-84-2

22978-25-2

22978-25-2 structure
22978-25-2 structure
  • Name: GW9662
  • Chemical Name: 2-Chloro-5-nitro-N-4-phenylbenzamide
  • CAS Number: 22978-25-2
  • Molecular Formula: C13H9ClN2O3
  • Molecular Weight: 276.675
  • Catalog: Biochemical Inhibitor Metabolism PPAR antagonist
  • Create Date: 2019-01-02 19:36:51
  • Modify Date: 2024-01-05 18:40:13
  • GW9662 is a potent and selective PPARγ antagonist with an IC50 of 3.3 nM, showing 10 and 1000-fold selectivity over PPARα and PPARδ, respectively.
Name 2-Chloro-5-nitro-N-4-phenylbenzamide
Synonyms MFCD01215270
Benzamide, 2-chloro-5-nitro-N-phenyl-
2-Chloro-5-nitro-N-phenylbenzamide
GW-9662
GW9662
Description GW9662 is a potent and selective PPARγ antagonist with an IC50 of 3.3 nM, showing 10 and 1000-fold selectivity over PPARα and PPARδ, respectively.
Related Catalog
Target

PPARγ:3.3 nM (IC50)

PPARα:32 nM (IC50)

PPARδ:2000 nM (IC50)
In Vitro GW9662 inhibits radioligand binding to PPARγ, PPARα, and PPARδ with pIC50s 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), respectively. GW9662 has nanomolar IC50 versus PPARγ and is 10- and 600-fold less potent in binding experiments using PPARα and PPARδ, respectively. In cell-based reporter assays, GW9662 is a potent and selective antagonist of full-length PPARγ[1]. Co-treatment with both 50 μM Rosiglitazone and 10 μM GW9662 results in statistically lower viable cell numbers after 7 days when compared to treatment with either 50 μM rosiglitazone (P=0.001) or 10 μM GW9662 (P=0.01) alone[2].
In Vivo Bone marrow (BM) nucleated cell counts in both BADGE- and GW9662(1 mg/kg, i.p.)-treated mice are significantly higher than counts in the aplastic anemia (AA) group[3]. GW9662 (1 mg/kg, i.p.) largely attenuates the renoprotective effects of Lipopolysaccharide (LPS) in the rat[4].
Cell Assay Cells (MCF7, MDA-MB-231, MDA-MB-468) are plated in 96-well plates at a density of 1×103 cells per well in RPMI medium. After overnight incubation to allow for cell attachment, the medium is removed and replaced with fresh medium containing varying concentrations of Rosiglitazone (1-100 μM), GW9662 (100 nM-50 μM) or solvent (DMSO) alone. MDA-MB-231 cells are also subjected to combinations of Rosiglitazone (10, 50 μM) and GW9662 (1, 10 μM) added simultaneously. The final concentration of DMSO in all cases does not exceed 0.1% and is not found to be cytotoxic in any of the cell lines tested at this concentration. Chemosensitivity is assessed following a continuous 72 h exposure using a standard MTT assay.
Animal Admin Mice[3] Inbred C57BL/6 (B6, H2b/b), DBA/1J (DBA/1, H2q/q), FVB/NJ (FVB, H2q/q) mice and congenic C.B10-H2b/b/LilMcd (CB10, H2b/b) mice are used. BADGE or GW9662, are administrated by daily intraperitoneal injection at 30 mg/kg for BADGE, or at 1 mg/kg for GW9662, from one day prior to the experiment and continued for up to 2 weeks. In the FVB AA model, some mice are injected with cyclosporine A (CsA, 50 mg/kg/day) starting 1 hour after the LN injection, and continued for 5 days as immunosuppression. At the end of the experiments, the mice are euthanized by CO2 inhalation. Rats[4] Sixty-two male Wistar rats weighing 215 to 315 g are used in this study. Animals are randomly allocated into 6 groups as follows: (1) I/R group: control, rats are administered 10% (v/v) DMSO (vehicle for GW9662, 1 mL /kg, IP) 24 and 12 hours prior to renal I/R, and saline (vehicle for LPS, 1 mL /kg, IP) 24 hours prior to renal I/R (N=12); (2) I/R LPS group: rats are administered 10% (v/v) DMSO (vehicle for GW9662, 1 mL /kg, IP) 24 and 12 hours prior to renal I/R, and LPS (1 mg/kg, IP) 24 hours prior to renal I/R (N=11); (3) I/R GW9662 group: rats are administered GW9662 (1 mg/kg, IP) 24 and 12 hours prior to renal I/R, and saline (vehicle for LPS, 1 mL /kg, IP) 24 hours prior to renal I/R (N=9); (4) I/R LPS+GW9662 group: rats are administered GW9662 (1 mg/kg, IP) 24 and 12 hours prior to renal I/R, and LPS (1 mg/kg, IP) 24 hours prior to renal I/R (N=11); (5) Sham group: rats are subjected to the same surgical procedures as above, except for renal I/R. Rats are administered 10% (v/v) DMSO (vehicle for GW9662, 1 mL /kg, IP) and saline (vehicle for LPS, 1 mL /kg, IP) at times equivalent to those described above (N=12); (6) Sham GW9662 group: rats are subjected to the same surgical procedures as above, except for renal I/R. Rats are administered GW9662 (1 mg/kg, IP) and saline (vehicle for LPS, 1 mL /kg, IP) at times equivalent to those described above (N=7).
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 tumour cells and promotes the anticancer effects of the PPARgamma agonist rosiglitazone, 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.
Density 1.4±0.1 g/cm3
Boiling Point 360.9±32.0 °C at 760 mmHg
Melting Point 171-175 °C(lit.)
Molecular Formula C13H9ClN2O3
Molecular Weight 276.675
Flash Point 172.0±25.1 °C
Exact Mass 276.030182
PSA 74.92000
LogP 2.76
Appearance solid | white
Vapour Pressure 0.0±0.8 mmHg at 25°C
Index of Refraction 1.676
Storage condition 2-8°C
Water Solubility DMSO: 26 mg/mL, soluble
Symbol GHS07
GHS07
Signal Word Warning
Hazard Statements H317-H319
Precautionary Statements P280-P305 + P351 + P338
Hazard Codes Xi
Risk Phrases R36;R43
Safety Phrases S26-S36/37-S24/25-S22
RIDADR NONH for all modes of transport
WGK Germany 3
HS Code 2924299090
HS Code 2924299090
Summary 2924299090. other cyclic amides (including cyclic carbamates) and their derivatives; salts thereof. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%

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