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Chemical Structure| 885101-89-3 Chemical Structure| 885101-89-3
Chemical Structure| 885101-89-3

GW9508

CAS No.: 885101-89-3

GW9508 is selective FFA1 (GPR40) agonist with pEC50 of 7.32 and stimulates insulin secretion in a glucose-sensitive manner.

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Cat. No.: A144748 Purity: 98%

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Product Details of GW9508

CAS No. :885101-89-3
Formula : C22H21NO3
M.W : 347.41
SMILES Code : OC(=O)CCC1=CC=C(NCC2=CC(OC3=CC=CC=C3)=CC=C2)C=C1
MDL No. :MFCD09753282
InChI Key :DGENZVKCTGIDRZ-UHFFFAOYSA-N
Pubchem ID :11595431

Safety of GW9508

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H317-H319
Precautionary Statements:P280-P305+P351+P338

Related Pathways of GW9508

GPCR

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description Reference
661W cells 14 µM 8 h To study the effect of GW9508 on Hif1a protein expression PMC4823176
661W cells 14 µM 12 h To study the effect of GW9508 on Vegfa secretion PMC4823176
CLU189 cells 100 μM 1 h To evaluate the effect of GW9508 on IKK activity in CLU189 cells, results showed a trend but no significant reduction in IKK activity. PMC5405534
BV2 cells 100 μM 1 h To evaluate the effect of GW9508 on IKK activity in BV2 cells, results showed a significant trend in reducing IKK activity. PMC5405534
Human neutrophils 1 and 10 μM 10 min GW9508 increased neutrophil chemotaxis in response to IL-8 and enhanced neutrophil phagocytosis of E. coli. PMC7550532
hippocampal CA1 pyramidal neurons 20 µM GW9508 reduced NMDAR-mediated postsynaptic currents, indicating that GPR40 modulates NMDAR-mediated synaptic transmission. PMC6192686
BRIN-BD11 cells 20 μM 60 min GW9508 increased superoxide and H2O2 content at 5.6 mM and 8.3 mM glucose concentrations, but not at 16.7 mM glucose concentration. PMC7241480
roGFP2-Orp1 BRIN-BD11 cells 20 μM 60 min GW9508 increased H2O2 content at 5.6 mM and 8.3 mM glucose concentrations, but not at 16.7 mM glucose concentration. PMC7241480
brown preadipocytes 100 μM 24 h GW9508 treatment significantly induced the expression of UCP1, Glut1, and FGF21, and strongly increased the secretion of FGF21 protein. PMC5118546
brown adipocytes 100 μM 24 h GW9508 treatment significantly increased the thermogenic activity of brown adipocytes and promoted the release of FGF21. PMC5118546
beige preadipocytes 100 μM 24 h GW9508 treatment significantly induced the differentiation of beige adipocytes and promoted the release of FGF21. PMC5118546

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description Reference
Mice Vldlr−/− mice Intraperitoneal 14 µM Once daily for 7 days To study the effect of GW9508 on retinal glucose uptake and RAP-like lesions PMC4823176
Swiss mice High-fat diet-induced obesity model Intracerebroventricular injection 1.0 mM Twice daily for 6 days To evaluate the effect of GW9508 on energy efficiency and inflammatory gene expression in obese mice, results showed that GW9508 reduced energy efficiency and decreased the expression of inflammatory genes. PMC5405534
Mice E. coli infection model Intraperitoneal injection 10 mg/kg Once, lasting 12 hours GW9508 increased peritoneal leukocyte infiltration, enhanced phagocytic capacity, and modulated lipid mediator production. PMC7550532
mice KA-induced temporal lobe epilepsy model intracerebroventricular injection 1 µg/mouse daily for seven consecutive days GW9508 decreased the number of seizure-like events and the total time spent in SLEs, indicating its antiepileptic effect. PMC6192686
rats germinal matrix hemorrhage (GMH) model intranasal administration 0.84 mg/kg, 2.5 mg/kg, 7.5 mg/kg administration at 1 h, 25 h, and 49 h after GMH induction GW9508 attenuated neuroinflammation and improved neurological function via the PAK4/CREB/KDM6B pathway after GMH PMC8286626
mice C57BL6 mice diet 50 mg/kg once daily for 7 days GW9508 treatment significantly upregulated thermogenic genes in BAT and induced browning in iWAT, while increasing blood FGF21 levels. PMC5118546

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.88mL

0.58mL

0.29mL

14.39mL

2.88mL

1.44mL

28.78mL

5.76mL

2.88mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

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