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Berotralstat dihydrochloride

Cat. No. M28905
Berotralstat dihydrochloride Structure
Synonym:

BCX7353 dihydrochloride

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Quality Control & Documentation
Biological Activity

Berotralstat dihydrochloride is a low toxicity, effective, highly specific, second-generation, synthetic and orally active plasma kallikrein inhibitor used for the research of hereditary angioedema (HAE) attacks. Berotralstat dihydrochloride works by blocking the enzymatic activity of plasma kallikrein in releasing bradykinin, the major biologic peptide that promotes swelling and pain associated with attacks of HAE.

Chemical Information
Molecular Weight 635.48
Formula C30H28Cl2F4N6O
CAS Number 1809010-52-3
Form Solid
Solubility (25°C) DMSO 120 mg/mL (ultrasonic)
Storage 4°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.

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Keywords: Berotralstat dihydrochloride, BCX7353 dihydrochloride supplier, Serine/Threonine Protease, inhibitors, activators


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