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MLCK inhibitor peptide 18

Cat. No. M13758
MLCK inhibitor peptide 18 Structure
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Biological Activity

MLCK inhibitor peptide 18 is a myosin light chain kinase (MLCK) inhibitor with an IC50 of 50 nM, and inhibits CaM kinase II only at 4000-fold higher concentrations.

Chemical Information
Molecular Weight 1324.62
Formula C60H105N23O11
CAS Number 224579-74-2
Solubility (25°C) Water 90 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] Ossama Allam, et al. PLoS One. HIV induces production of IL-18 from intestinal epithelial cells that increases intestinal permeability and microbial translocation

[2] Younggeon Jin, et al. Am J Physiol Cell Physiol. Myosin light chain kinase mediates intestinal barrier dysfunction via occludin endocytosis during anoxia/reoxygenation injury

[3] Tamia K Lapointe, et al. Am J Physiol Gastrointest Liver Physiol. Interleukin-18 facilitates neutrophil transmigration via myosin light chain kinase-dependent disruption of occludin, without altering epithelial permeability

[4] Eikichi Ihara, et al. Can J Physiol Pharmacol. The regulation of smooth muscle contractility by zipper-interacting protein kinase

[5] H Yoshida, et al. Biochim Biophys Acta. A possible role for Ca(2+)/calmodulin-dependent protein kinase IV during pancreatic acinar stimulus-secretion coupling

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