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Polyphemusin II-Derived Peptide

Cat. No. M41797
Polyphemusin II-Derived Peptide Structure
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Biological Activity

Polyphemusin II-Derived Peptide (T140), a CXCR4 inhibitor, shows high inhibitory activity against HIV-1 entry.

Chemical Information
Molecular Weight 2037.42
Formula C90H141N33O18S2
CAS Number 229030-20-0
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Zhi-Yong Gao et al. World Neurosurg. T140 Inhibits Apoptosis and Promotes Proliferation and Matrix Formation Through the SDF-1/CXC Receptor-4 Signaling Pathway in Endplate Chondrocytes of the Rat Intervertebral Discs

[2] Ryo Masuda et al. Bioconjug Chem. Paradoxical downregulation of CXC chemokine receptor 4 induced by polyphemusin II-derived antagonists

[3] Ryo Masuda et al. Bioorg Med Chem. Concise site-specific synthesis of DTPA-peptide conjugates: application to imaging probes for the chemokine receptor CXCR4

[4] Savita Tauro et al. Protein Pept Lett. An antiparallel beta-sheet and a beta-turn characterize the structure of antiviral HIV-1 peptide T140, as revealed by 2D NMR and MD Simulations

[5] J Juarez et al. Leukemia. Effects of inhibitors of the chemokine receptor CXCR4 on acute lymphoblastic leukemia cells in vitro

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Keywords: Polyphemusin II-Derived Peptide supplier, CXCR, inhibitors, activators

 
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