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Cat. No. Name Size Price Add Cart
KI0792Ivermectin50 mg$154

Chemical Characteristic

Product NameIvermectin
SynonymsStromectol, Ivomec, Mectizan, Ivexterm, MK-933
CAS No.70288-86-7
Molecular Weight 875.09
FormulaC48H74O14
Chemical Structure

Biological activities

Ivermectin is a broad-spectrum antiparasitic avermectin agent. The IC50 of ivermectin is 1 and 2.5 µM against the induction of calcein and BCECF retention in A549 cells, respectively. Ivermectin prevents calcein efflux in HL60-MRP1 with an IC50 of 3.8 µM. Ivermectin blocks the Pgp (P-glycoprotein), MRP1 (multidrug resistance proteins), 2 and 3 ATPase activities.[1] Ivermectin inhibits helical swimming and body reversal behaviors in a time- and concentration-dependent manner. Ivermectin at 0.3 nM also significantly decreases the frequency of helical swimming waves.[2] In mammalian membrane vesicles specifically overexpressing human ABCG2 (ATP-binding cassette G2), ivermectin inhibits E3S transport with an IC50 of 1.5µM. Ivermectin blocks the basal vanadate sensitive activity of ABCG2 with the same efficacy as Kο134, the reference inhibitor. Ivermectin interacts with human ABCG2 with a Kι of 1.4µM.[3] In addition, ivermectin is a competitive inhibitor of specific [3H]-GABA binding activity with a Kι of 3.39nM.[4] Ivermectin acts by binding selectively to specific neurotransmitter receptors that function in the peripheral motor synapses of parasites. Ivermectin blocks chemical transmission across the nerve synapses that use glutamate-gated anion channels or γ-aminobutyric acid-gated chloride channels.[5]

Protocols

In vitro: Ivermectin is dissolved in a solution with 5% DMSO.[4]

References

[1] Lespine A, et al. Interaction of ivermectin with multidrug resistance proteins (MRP1, 2 and 3). Chem Biol Interact. 2006, 159(3): 169-179. 閵嗏偓閵嗏偓
[2] Ding J, et al. Behavioral effects of ivermectin in a freshwater oligochaete, Lumbriculus variegatus. Environ Toxicol Chem. 2001, 20(7): 1584-1590. 閵嗏偓閵嗏偓
[3] Jani M, et al. Ivermectin interacts with human ABCG2. J Pharm Sci. 2011, 100(1): 94-97. 閵嗏偓閵嗏偓
[4] Ros-Moreno RM, et al. Interaction of ivermectin with gamma-aminobutyric acid receptors in Trichinella spiralis muscle larvae.Parasitol Res. 1999, 85(4): 320-323. 閵嗏偓閵嗏偓
[5] Dourmishev AL, et al. Ivermectin: pharmacology and application in dermatology. Int J Dermatol. 2005, 44(12): 981-988. 閵嗏偓閵嗏偓

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