GW9662 - Moligand™, 10mM in DMSO , CAS No.22978-25-2

CAS: 22978-25-2 Cat. No.: G407990 Fórmula: C₁₃H₉ClN₂O₃ Peso molecular: 276.68 Número CE: 636-590-7

GRAU & PUREZA Moligand™, 10mM in DMSO

Synonyms

Benzamide, 2-chloro-5-nitro-N-phenyl-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Visão geral

Information

GW9662 is a selective PPAR antagonist forPPARγwithIC50of 3.3 nM in a cell-free assay, with at least 10- to 600-fold functional selectivity in cells with PPARγ versus PPARα and PPARδ.
In vitro

GW9662 binds to Cys(285) on PPARgamma which is conserved among all three PPARs. GW9662 acts as an antagonist of PPARgamma which is confirmed in an assay of adipocyte differentiation inhibition. GW9662 prevents activation of PPARγ and inhibits growth of human mammary tumour cell lines (MCF7, MDA-MB-468, MDA-MB-231) with IC50 of 20 μM-30 μM, suggesting either the existence of PPARγ agonistic properties of GW9662 or growth-inhibitory mechanisms independent of PPARγ. Co-treatment with both Rosiglitazone (50 μM) and GW9662 (10 μM) results in statistically lower viable cell numbers after 7 days in MDA-MB-231 cells. PPARγ1 ligands could suppress RANKL-induced osteoclast formation in primary murine myeloid (BMs) and RAW264.7 cells. Importantly, suppression by these ligands is reversed in a concentration-dependent fashion with GW 9662 (2 μM). GW 9662 (2 μM) blocks IL-4 suppression of osteoclast formation in BMs. GW 9662 (1 μM) blocks RANKL activation of NF-κB in RAW264.7 cells. GW9662 (10 μM) inhibits hormone- and agonist-induced adipogenesis of primary preadipocytes from patients with thyroid eye disease.

In vivo

Pretreatment with LPS (1 mg/kg i.p.) significantly attenuates all markers of renal injury and dysfunction caused by ischemia/reperfusion (I/R) injury in rats. Most notably, GW9662 (1 mg/kg i.p.) abolishes the protective effects of LPS.
Cell Data

cell lines：PHA-stimulated PBMC or PM-1 cells

Concentrations：10 μM

Incubation Time：10 days

Powder Purity:≥99%

Especificações

Sinónimos

Benzamide, 2-chloro-5-nitro-N-phenyl-

Especificações e pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos e fisiológicos

GW9662 is a selective PPAR antagonist for PPARγ with IC50 of 3.3 nM in a cell-free assay, with at least 10- to 600-fold functional selectivity in cells with PPARγ versus PPARα and PPARδ.

Condições de armazenamento de armazenamento

Store at -80°C

Enviado em

Dry ice packs + Cold packs

Este produto requer transporte de cadeia fria. Serviços terrestres e outros serviços econômicos não estão disponíveis.

Grau

Moligand™

Tipo de ação

ANTAGONIST

Nomes e identificadores

SMILES isoméricas

C1=CC=C(C=C1)NC(=O)C2=C(C=CC(=C2)[N+](=O)[O-])Cl

WGK Alemanha

3

Peso molecular

276.68

Reaxy-Rn

2749539

Reaxys-RN_link_address

https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=2749539&ln=

Alvos associados (humanos)

CYP1A2 Tchem Cytochrome P450 1A2 (1 Activities)

Discover Target: CYP1A2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CYP2C19 Tchem Cytochrome P450 2C19 (1 Activities)

Discover Target: CYP2C19

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

RORC Tchem Nuclear receptor ROR-gamma (1 Activities)

Discover Target: RORC

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PPARG Tclin Peroxisome proliferator-activated receptor gamma (2 Activities)

Discover Target: PPARG

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Propriedades químicas e físicas

• Solubilidade: Solubility (25°C) In vitro Water: 29 mg/mL (198.43 mM); DMSO: Insoluble

Perguntas frequentes

What is Moligand??

Moligand? is one of Aladdin Scientific's premium product lines, formulated for high-purity applications across multiple workflows. Compared to standard grades in the same workflow, Moligand? products typically offer tighter specifications, more rigorous QC, and stronger lot-to-lot consistency.

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 22978-25-2, the molecular formula is C13H9ClN2O3, and the molecular weight is 276.68 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.