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Remibrutinib (LOU064)

Cat. No. M10500
Remibrutinib (LOU064) Structure
Synonym:

LOU064

Size Price Availability Quantity
5mg USD 345  USD345 In stock
10mg USD 540  USD540 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Remibrutinib (LOU064) is a potent and highly selective covalent Inhibitor of Bruton's Tyrosine Kinase (BTK) with IC50 value of 1 nM. LOU064 (Remibrutinib) exhibits an exquisite kinase selectivity due to binding to an inactive conformation of BTK and has the potential for a best-in-class covalent BTK inhibitor for the treatment of autoimmune diseases. LOU064 (Remibrutinib) demonstrates potent in vivo target occupancy with an EC90 of 1.6 mg/kg and dose-dependent efficacy in rat collagen-induced arthritis.

Protocol
Cell Experiment
Cell lines human monocytic cell line THP1, Human Blood B cell and Basophil
Preparation method The effects of LOU064 on signaling from the activating FcγR are assessed in the human monocytic cell line THP1 (ATCC, TIB-202). The THP1 cell line expresses the two activating FcγRs CD32a (FcγRII2) and CD64 (FcγRI) that signal through BTK. Briefly, 384 well culture plates are coated with pooled non-specific human IgG fraction. Serial compound dilutions are dispensed into the IgG-coated plates containing a small volume of tissue culture medium. Then THP1 cells that are pre-differentiated by vitamin D3 treatment for 5 days are added to each well. Twenty-four hours later the secretion of IL-8 in the supernatant of these culture wells is assessed by a homogenous immunoassay.
Concentrations 3 nM, 10 nM, 30 nM, 100 nM, 300 nM
Incubation time 25 min, 50 min, 75 min, 100 min
Animal Experiment
Animal models Female Lewis rats, female C57BL/6 mice, male beagle dog
Formulation -
Dosages 1 mg/kg, 3 mg/kg
Administration i.v. or p.o. administration
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 507.53
Formula C27H27F2N5O3
CAS Number 1787294-07-8
Purity >99%
Solubility DMSO 100 mg/mL
Storage at -20°C
References

[1] Daniela Angst, et al. J Med Chem. Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Remibrutinib (LOU064), LOU064 supplier, BTK, inhibitors

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