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Sebetralstat

Cat. No. M21530
Sebetralstat Structure
Synonym:

KVD900

Size Price Availability Quantity
5mg USD 160  USD160 In stock
10mg USD 250  USD250 In stock
25mg USD 460  USD460 In stock
50mg USD 750  USD750 In stock
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Quality Control & Documentation
Biological Activity

Sebetralstat is an orally active plasma kininase (KLKB1) inhibitor for studies related to hereditary angioedema (HAE).

Chemical Information
Molecular Weight 491.51
Formula C26H26FN5O4
CAS Number 1933514-13-6
Solubility (25°C) DMSO ≥ 100 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] Emel Aygren-Prsn, et al. Lancet. An investigational oral plasma kallikrein inhibitor for on-demand treatment of hereditary angioedema: a two-part, randomised, double-blind, placebo-controlled, crossover phase 2 trial

[2] Rebecca L Davie, et al. J Med Chem. Sebetralstat (KVD900): A Potent and Selective Small Molecule Plasma Kallikrein Inhibitor Featuring a Novel P1 Group as a Potential Oral On-Demand Treatment for Hereditary Angioedema

[3] Peter Mutch, et al. Xenobiotica. Absorption, metabolism, and excretion of [14C]-sebetralstat (KVD900) following a single oral dose in healthy male participants

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  Catalog
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Keywords: Sebetralstat, KVD900 supplier, Serine/Threonine Protease, inhibitors, activators


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