Remibrutinib (LOU064)

Catalog No.S9660

For research use only.

Remibrutinib (LOU064) is a potent, highly selective covalent inhibitor of bruton tyrosine kinase (BTK) with IC50 of 1.3 nM, 2.5 nM and 18 nM for BTK, FcγR-induced IL8 and anti-IgM/IL4-induced CD69, respectively. Remibrutinib (LOU064) exhibits an exquisite kinase selectivity due to binding to an inactive conformation of BTK and has the potential for the treatment of autoimmune diseases.

Remibrutinib (LOU064) Chemical Structure

CAS No. 1787294-07-8

Purity & Quality Control

Choose Selective BTK Inhibitors

Biological Activity

Description Remibrutinib (LOU064) is a potent, highly selective covalent inhibitor of bruton tyrosine kinase (BTK) with IC50 of 1.3 nM, 2.5 nM and 18 nM for BTK, FcγR-induced IL8 and anti-IgM/IL4-induced CD69, respectively. Remibrutinib (LOU064) exhibits an exquisite kinase selectivity due to binding to an inactive conformation of BTK and has the potential for the treatment of autoimmune diseases.
Targets
BTK [1]
(Cell-free assay)
IL-8 [1]
(Cell-free assay)
CD69 [1]
(Cell-free assay)
1.3 nM 2.5 nM 18 nM
In vitro

LOU064 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.[1]

In vivo

LOU064 demonstrates potent in vivo target occupancy with an EC90 of 1.6 mg/kg and dose-dependent efficacy in rat collagen-induced arthritis.[1]

Protocol (from reference)

Cell Research:

[1]

  • Cell lines: human monocytic cell line THP1, Human Blood B cell and Basophil.
  • Concentrations: 3 nM, 10 nM, 30 nM, 100 nM, 300 nM
  • Incubation Time: 25 min, 50 min, 75 min, 100 min
  • 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.

Animal Research:

[1]

  • Animal Models: Female Lewis rats, female C57BL/6 mice, male beagle dog.
  • Dosages: 1 mg/kg, 3 mg/kg
  • Administration: IV, Oral gavage

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 507.53
Formula

C27H27F2N5O3

CAS No. 1787294-07-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=C(C=C(C=C1NC(=O)C2=C(C=C(C=C2)C3CC3)F)F)C4=C(C(=NC=N4)N)OCCN(C)C(=O)C=C

In vivo Formulation Calculator (Clear solution)

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05432388 Not yet recruiting Drug: remibrutinib|Drug: placebo Allergy Peanut Novartis Pharmaceuticals|Novartis August 12 2022 Phase 2
NCT05156281 Recruiting Drug: Remibrutinib|Drug: Teriflunomide Relapsing Multiple Sclerosis Novartis Pharmaceuticals|Novartis December 13 2021 Phase 3
NCT05147220 Recruiting Drug: Remibrutinib|Drug: Teriflunomide Relapsing Multiple Sclerosis Novartis Pharmaceuticals|Novartis December 16 2021 Phase 3
NCT04109313 Active not recruiting Drug: LOU064 Chronic Spontaneous Urticaria Novartis Pharmaceuticals|Novartis October 24 2019 Phase 2
NCT03944707 Terminated Drug: LOU064 100 mg|Drug: Placebo Asthma Novartis Pharmaceuticals|Novartis July 18 2019 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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