FPTQ

SKU: orb1301734

Description

FPTQ is a potent and selective mGluR1 antagonist with IC50 values of 6 nM (human) and 1.4 nM (mouse). It is a valuable research tool for studying neurological disorders and inflammation, demonstrating significant antioxidant and anti-inflammatory activity in both cellular and animal models.

Research Area

Neuroscience

Key Properties

• CAS Number: 864863-72-9
• MW: 305.31
• Purity: 99.88%
• Formula: C₁₇H₁₂FN₅
• SMILES: Cc1c(nnn1-c1cccnc1F)-c1ccc2ncccc2c1
• Target: GluR
• Solubility: DMSO:4.4 mg/mL (14.41 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (3.28 mM)

Bioactivity

• Target IC50:
  mGluR1(mouse):1.4 nM|mGluR1(human):6 nM
• In Vivo:
  Neutrophils translocation in the zebrafish tail-transected model was inhibited by FPTQ. Neutrophil aggregation was also inhibited by FPTQ in the LPS-stimulated zebrafish model. FPTQ (5-20 μM) decreases the number of neutrophils migrating to the amputation site in zebrafish larvae by tail amputation. In the tailfin wound method, the number of neutrophils collecting at the wound site also decreases in a dose-dependent manner in zebrafish .In a LPS-induced inflammation zebrafish model, LPS solution is injected into the yolks of Tg(mpx:EGFP) i114 zebrafish larvae and exposed the zebrafish larvae immediately to FPTQ treatment.FPTQ (20 μM; 4 hours) significantly decreases the fluorescent neutrophils after yolk injection and has an anti-inflammatory effect during the early phase of inflammation .
• In Vitro:
  FPTQ, at concentrations ranging from 0.5 to 10 μM, exhibited no cytotoxic effects in RAW264.7 macrophage cells . Furthermore, when administered at doses between 1 and 20 μM for a duration of 24 hours, FPTQ significantly inhibited LPS-induced NO production starting from concentrations above 1 μM. Specifically, a 10 μM dose of FPTQ resulted in a 31% reduction in oxidative stress . Additionally, this compound markedly suppressed LPS-stimulated upregulation of pro-inflammatory cytokines IL-1β and IL-6 in a concentration-dependent manner. At 10 μM, FPTQ was found to decrease the mRNA levels of IL-1β and IL-6 by 27% and 44%, respectively, illustrating its potent anti-inflammatory properties in RAW264.7 macrophage cells . This was further supported by RT-PCR analysis, confirming the downregulation of these cytokines .

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

mGluR1, FPTQ

Compound Identifiers

PubChem CID

11301185