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Lavendustin B

Cat. No. M20765
Lavendustin B Structure
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Biological Activity

Lavendustin B inhibits HIV-1 integrase (IN) interaction with its cognate cellular cofactor lens epithelium-derived growth factor (LEDGF/p75). Lavendustin B is an inhibitor of Tyrosine Kinase and also a competitive inhibitor of glucose transporter 1 (Glut1).

Chemical Information
Molecular Weight 365.38
Formula C21H19NO5
CAS Number 125697-91-8
Solubility (25°C) DMSO 73 mg/mL
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] Fatima E Agharbaoui, et al. Eur J Med Chem. Computational and synthetic approaches for developing Lavendustin B derivatives as allosteric inhibitors of HIV-1 integrase

[2] D Glahn, et al. Dev Biol. Tyrosine kinase inhibitors block sperm-induced egg activation in Xenopus laevis

[3] M Hisatomi, et al. Jpn J Pharmacol. Modulation of tyrosine kinase activity has multiple actions on insulin release from the pancreatic beta-cell: studies with lavendustin A

[4] S Meizel, et al. J Androl. Chloride efflux during the progesterone-initiated human sperm acrosome reaction is inhibited by lavendustin A, a tyrosine kinase inhibitor

[5] D E Hu, et al. Br J Pharmacol. Suppression of VEGF-induced angiogenesis by the protein tyrosine kinase inhibitor, lavendustin A

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Keywords: Lavendustin B supplier, Integrase, inhibitors, activators
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