A 779 TFA(159432-28-7 free base)

SKU: orb1299656

Description

A 779 TFA is a selective and potent antagonist of the Mas receptor (Mas1/GPER), which mediates the effects of angiotensin-(1-7). This compound is a valuable research tool for investigating the renin-angiotensin system in both in vitro and in vivo models, helping to elucidate the physiological roles of the Ang-(1-7)/Mas axis.

Research Area

Immunology & Inflammation, Metabolism Research

Key Properties

• MW: 987.01
• Purity: >99.99% (May vary between batches)
• Formula: C₄₁H₆₁F₃N₁₂O₁₃
• SMILES: OC(=O)C(F)(F)F.CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@@H](N)CC(O)=O)C(C)C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](C)C(O)=O
• Target: RAAS
• Solubility: DMSO:11.78 mg/mL (11.94 mM)

Bioactivity

• In Vivo:
  Inhibition of Ang1-7 cascade by A 779significantly eradicated captopril protective effects on bone metabolism, mineralization and micro-structure.A 779also restored OVX effects on RANKL expression and ACE-1/AngII/AT1R cascade and down-regulated OPG expression and ACE-2/Ang1-7/Mas pathway.In line with the clinical observations of the bone-preservative properties following ACE-1 inhibition, local activation of ACE-2/Ang1-7/Mas signaling and suppressed osteoclastogenesis seem responsible for the osteo-preservative effect of captopril, which could offers a potential therapeutic value in treatment of disabling bone and skeletal muscular diseases.
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• In Vitro:
  A 779suppresses the proliferating cell nuclear antigen (PCNA) protein expression up-regulated by Ang II, but A 779alone has no effect to induce proliferation and migration of VSMCs.Pretreatment with Ang-(1-7) significantly retards Ang II-induced inflammatory responses of VSMCs associated with up-regulated MCP-1, VCAM-1 and IL-1β expressions, and this effect of Ang-(1-7) is blocked by A-779.But A 779alone has no effect to induce inflammatory response of VSMCs.
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• Cell Research:
  HUVECs were cultured in vitro and divided into six groups: the control group (normal medium), the ox-LDL group(treated with 75 mg/L ox-LDL), the ox-LDL+ Ang-(1-7) group (1 μmol/L Ang-(1-7) pretreated for 30 minutes, then intervened with 75 mg/L ox-LDL), the ox-LDL+ Ang-(1-7)+ A-779 group(1 μmol/L A-779 (Mas receptor) pretreated for 30 minutes, 1 μmol/L Ang-(1-7) pretreated for 30 minutes, then intervened with 75 mg/L ox-LDL), the ox-LDL+ A-779 group (1 μmol/L A-779 pretreated for 30 minutes, then intervened with 75 mg/L ox-LDL), the ox-LDL+ HTA125 group (10 μg/L HTA125 (TLR4-blocking antibody) pretreated for 30 minutes, then intervened with 75 mg/L ox-LDL ). The corresponding index was detected after 24 hours after intervention. Apoptosis of cells were detected by Annexin V-FITC/PI double staining flow cytometry and transferase-mediated deoxyuridine triphosphate-biotin nick end labeling (TUNEL). The generation of reactive oxygen species (ROS), products in oxidative stress, were detected by DCFH-DA staining. The mRNA and protein expression levels of NADPH oxidase 4(NOX4) and TLR4 were detected by real-time reverse transcription-polymerase chain reaction (RT-PCR) and Western blotting analysis respectively.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Angiotensin Receptor, A 779 3TFA(159432-28-7(free base)), A 779 TFA(159432 28 7 free base), A 779 TFA(159432287 free base), A 779 TFA(159432-28-7 free base)

Compound Identifiers

PubChem CID

145707593