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PKSI-527

Cat. No. M42611
PKSI-527 Structure
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Biological Activity

PKSI-527 is a new, highly selective plasma kallikrein inhibitor.

Chemical Information
Molecular Weight 473.99
Formula C25H32ClN3O4
CAS Number 128837-71-8
Form Solid
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] Masaru Hashimoto et al. Thromb Haemost. Suppression of argatroban-induced endogenous thrombolysis by PKSI-527, and antibodies to TPA and UPA, evaluated in a rat arterial thrombolysis model

[2] K Tomoo et al. J Biochem. Binding diversity of a noncovalent-type low-molecular-weight serine protease inhibitor and function of a catalytic water molecule: X-ray crystal structure of PKSI-527--inhibited trypsin

[3] A Fukumizu et al. Chem Pharm Bull (Tokyo). Amino acids and peptides. LIII. Synthesis and biological activities of some pseudo-peptide analogs of PKSI-527, a plasma kallikrein selective inhibitor: the importance of the peptide backbone

[4] Y Fujimori et al. Agents Actions. Effects of a highly selective plasma kallikrein inhibitor on collagen-induced arthritis in mice

[5] K Wanaka et al. Thromb Res. Effect of a highly selective plasma-kallikrein synthetic inhibitor on contact activation relating to kinin generation, coagulation and fibrinolysis

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Keywords: PKSI-527 supplier, Serine/Threonine Protease, inhibitors, activators

 
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