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INE963

Cat. No. M10694
INE963  Structure
Size Price Availability Quantity
5mg USD 350  USD350 In stock
10mg USD 540  USD540 In stock
25mg USD 1080  USD1080 In stock
50mg USD 1500  USD1500 In stock
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Quality Control & Documentation
Biological Activity

INE963 is an oral, single-dose, fast-acting blood-stage antimalarial candidate with an EC50 value of 3-6 nM.

Chemical Information
Molecular Weight 402.51
Formula C19H26N6O2S
CAS Number 2640567-43-5
Form Solid
Storage 4°C, protect from light, 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] Rundan Duan, et al. Front Cardiovasc Med. Effects of the Btk-Inhibitors Remibrutinib (LOU064) and Rilzabrutinib (PRN1008) With Varying Btk Selectivity Over Tec on Platelet Aggregation and in vitro Bleeding Time

[2] Aikaterini Patsatsi, et al. Front Med (Lausanne). Bruton Tyrosine Kinase Inhibition and Its Role as an Emerging Treatment in Pemphigus

[3] D F Murrell, et al. Br J Dermatol. Proof of concept for the clinical effects of oral rilzabrutinib, the first Bruton tyrosine kinase inhibitor for pemphigus vulgaris: the phase II BELIEVE study

[4] Philipp von Hundelshausen, et al. Cancers (Basel). Bleeding by Bruton Tyrosine Kinase-Inhibitors: Dependency on Drug Type and Disease

[5] Claire L Langrish, et al. J Immunol. Preclinical Efficacy and Anti-Inflammatory Mechanisms of Action of the Bruton Tyrosine Kinase Inhibitor Rilzabrutinib for Immune-Mediated Disease

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