SML4164
ATN-161 trifluoroacetate salt
≥95% (HPLC), (Powder or Lyophilized powder or film), integrin α5β1receptor antagonist
Synonym(s):
1-Acetyl-L-prolyl-L-histidyl-L-seryl-L-cysteinyl-L-aspartamide trifluoroacetate salt, Ac-PHSCN-NH2 trifluoroacetate salt, Ac-Pro-His-Ser-Cys-Asn-NH2, PHSCN trifluoroacetate salt
Quality Level
Assay
≥95% (HPLC)
form
(Powder or Lyophilized powder or film)
storage condition
desiccated
color
white to off-white
storage temp.
-10 to -25°C
SMILES string
O=C([C@H]1N(C(C)=O)CCC1)N[C@@H](CC2=CN=CN2)C(N[C@@H](CO)C(N[C@@H](CS)C(N[C@@H](CC(N)=O)C(N)=O)=O)=O)=O
General description
ATN-161, an antagonist of the integrin α5β1receptor, is a non-RGD-based integrin binding peptide derived from the synergy region of fibronectin that inhibits the receptors for integrins alpha-vbeta-3 and integrin alpha-5 beta-1. Integrin alpha-5 beta-1 is expressed on endothelial cells and plays a key role in endothelial cell adhesion and migration and may also play a key role in cancer cell invasion and metastasis. ATN-161 exhibits antiangiogenic and antitumor activity.
This noncompetitive inhibitor of the fibronectin PHSRN sequence has the potential to disrupt the function of various integrins involved in tumor angiogenesis and metastasis. It can inhibit the interaction between the SARS-CoV-2 spike protein and its host binding partners.
This noncompetitive inhibitor of the fibronectin PHSRN sequence has the potential to disrupt the function of various integrins involved in tumor angiogenesis and metastasis. It can inhibit the interaction between the SARS-CoV-2 spike protein and its host binding partners.
Application
ATN-161trifluoroacetate salt may be used in studies focusing on angiogenesis andcancer research, particularly in the development of models assessing tumorgrowth and metastasis. It may also be used as a fluorescent probe inresearch to study cellular processes and interactions due to its ability tobind to integrins.
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Brandon J Beddingfield et al.
JACC. Basic to translational science, 6(1), 1-8 (2020-10-27)
Many efforts to design and screen therapeutics for the current severe acute respiratory syndrome-coronavirus-2 (SARS-CoV-2) pandemic have focused on inhibiting viral host cell entry by disrupting angiotensin-converting enzyme-2 (ACE2) binding with the SARS-CoV-2 spike protein. This work focuses on the
M E Cianfrocca et al.
British journal of cancer, 94(11), 1621-1626 (2006-05-18)
To evaluate the toxicity, pharmacological and biological properties of ATN-161, a five -amino-acid peptide derived from the synergy region of fibronectin, adult patients with advanced solid tumours were enrolled in eight sequential dose cohorts (0.1-16 mg kg(-1)), receiving ATN-161 administered
Jie Chen et al.
The American journal of pathology, 185(9), 2575-2589 (2015-07-28)
Endothelial cell interactions with transitional matrix proteins, such as fibronectin, occur early during atherogenesis and regulate shear stress-induced endothelial cell activation. Multiple endothelial cell integrins bind transitional matrix proteins, including α5β1, αvβ3, and αvβ5. However, the role these integrins play
Wen-Qiu Wang et al.
Molecular pharmaceutics, 13(9), 2881-2890 (2016-04-19)
The wet form of age-related macular degeneration (AMD) is a leading cause of blindness among elderly Americans and is characterized by abnormal vessel growth, termed choroidal neovascularization (CNV). Integrin α5β1 is a transmembrane receptor that binds matrix macromolecules and proteinases
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