An integrin receptor antagonist
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ATN-161 (trifluoroacetate salt)

Item No. 34056

Technical Information
Formal Name
1-acetyl-L-prolyl-L-histidyl-L-seryl-L-cysteinyl-L-aspartamide, monotrifluoroacetate salt
CAS Number
904763-27-5
Synonyms
  • Ac-PHSCN-NH2
  • PHSCN Peptide
Molecular Formula
C23H35N9O8S • CF3COOH
Formula Weight
Purity
≥95%
A crystalline solid
PBS (pH 7.2): 1 mg/ml
SMILES
OC(C(F)(F)F)=O.NC(C[C@@H](C(N)=O)NC([C@H](CS)NC([C@H](CO)NC([C@H](CC1=CN=CN1)NC([C@H]2N(C(C)=O)CCC2)=O)=O)=O)=O)=O
InChi Code
InChI=1S/C23H35N9O8S.C2HF3O2/c1-11(34)32-4-2-3-17(32)23(40)29-14(5-12-7-26-10-27-12)20(37)30-15(8-33)21(38)31-16(9-41)22(39)28-13(19(25)36)6-18(24)35;3-2(4,5)1(6)7/h7,10,13-17,33,41H,2-6,8-9H2,1H3,(H2,24,35)(H2,25,36)(H,26,27)(H,28,39)(H,29,40)(H,30,37)(H,31,38);(H,6,7)/t13-,14-,15-,16-,17-;/m0./s1
InChi Key
MCVJOWHOEOLJGI-LQCLSJOXSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    ATN-161 is a peptide derived from fibronectin and an integrin αVβ3 and αVβ5 antagonist.1 It binds to αVβ3 and αVβ5 receptors (Kds = 0.69 and 1 µM, respectively) in MDA-MB-231 breast cancer cells, as well as inhibits the interaction between αVβ5 and human angiotensin-converting enzyme 2 (ACE2) or severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) spike protein in a concentration-dependent manner in cell-free assays.1,2 ATN-161 reduces viral titers in Vero E6 cells infected with SARS-CoV-2 (EC50 = 3.16 µM).2 It inhibits VEGF-induced migration and capillary tube formation of primary human choroidal endothelial cells when used at a concentration of 0.1 µM.3 ATN-161 (1 mg/kg) reduces tumor growth and metastasis in an MDA-MB-231 mouse xenograft model and infarct volume and edema in a mouse model of ischemic stroke induced by middle cerebral artery occlusion (MCAO).1,4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Khalili, P., Arakelian, A., Chen, G., et alA non-RGD-based integrin binding peptide (ATN-161) blocks breast cancer growth and metastasis in vivo. Mol. Cancer Ther. 5(9), 2271-2280 (2006).

    2. Beddingfield, B.J., Iwanaga, N., Chapagain, P.P., et alThe integrin binding peptide, ATN-161, as a novel therapy for SARS-CoV-2 infection. JACC Basic Transl. Sci. 6(1), 1-8 (2021).

    3. Wang, W., Wang, F., Lu, F., et alThe antiangiogenic effects of integrin α5β1 inhibitor (ATN-161) in vitro and in vivo. Invest. Ophthalmol. Vis. Sci. 52(10), 7213-7220 (2011).

    4. Edwards, D.N., Salmeron, K., Lukins, D.E., et alIntegrin α5β1 inhibition by ATN-161 reduces neuroinflammation and is neuroprotective in ischemic stroke. J. Cereb. Blood Flow Metab. 40(8), 1695-1708 (2020).