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CH 5450

Cat. No. M29691
CH 5450 Structure
Synonym:

Z-Ile-Glu-Pro-Phe-Ome

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Quality Control & Documentation
Biological Activity

CH 5450 (Z-Ile-Glu-Pro-Phe-Ome) is a selective short peptide human cardiac chymase inhibitor. CH-5450 inhibits the action of rat MAB elastase 2 on substrate Ang I with an IC50 value of 49 µM and N-succinyl-Ala-Ala-Pro-Phe-p-nitroanilide with an IC50 value of 4.8 µM.

Chemical Information
Molecular Weight 652.73
Formula C34H44N4O9
CAS Number 252557-97-4
Form Solid
Solubility (25°C) DMSO ≥ 43 mg/mL
Storage Store at ≤ -20°C, dry, sealed
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] Shao-heng He, et al. Acta Pharmacol Sin. Inhibition of tryptase and chymase induced nucleated cell infiltration by proteinase inhibitors

[2] Carlos F Santos, et al. Can J Physiol Pharmacol. Kinetic characterization and inhibition of the rat MAB elastase-2, an angiotensin I-converting serine protease

[3] S He, et al. J Pharmacol Exp Ther. Inhibitors of chymase as mast cell-stabilizing agents: contribution of chymase in the activation of human mast cells

[4] K Waldeck, et al. Br J Pharmacol. Characterization of angiotensin II formation in human isolated bladder by selective inhibitors of ACE and human chymase: a functional and biochemical study

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Keywords: CH 5450, Z-Ile-Glu-Pro-Phe-Ome supplier, Peptides, inhibitors, activators


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