Home Angiogenesis BTK inhibitor - Interleukins inhibitor Remibrutinib For research use only.

Remibrutinib

Synonyms: LOU064

Remibrutinib 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 Chemical Structure

Remibrutinib Chemical Structure

CAS No. 1787294-07-8

Purity & Quality Control

Batch: S966001 DMSO]100 mg/mL]false]Ethanol]4 mg/mL]false]Water]Insoluble]false Purity: 99.14%
99.14

Remibrutinib Related Products

Signaling Pathway

BTK Signaling Pathways

BTK Signaling Pathway

Biological Activity

Description Remibrutinib 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
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]
Cell Research 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.
In Vivo
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]
Animal Research Animal Models Female Lewis rats, female C57BL/6 mice, male beagle dog.
Dosages 1 mg/kg, 3 mg/kg
Administration IV, Oral gavage
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05677451 Recruiting
Chronic Spontaneous Urticaria
Novartis Pharmaceuticals|Novartis
 July 11 2023 Phase 3
NCT05432388 Recruiting
Allergy Peanut
Novartis Pharmaceuticals|Novartis
 October 12 2022 Phase 2
NCT05156281 Recruiting
Relapsing Multiple Sclerosis
Novartis Pharmaceuticals|Novartis
 December 13 2021 Phase 3
NCT05147220 Recruiting
Relapsing Multiple Sclerosis
Novartis Pharmaceuticals|Novartis
 December 16 2021 Phase 3
NCT04035668 Terminated
Sjögren Syndrome
Novartis Pharmaceuticals|Novartis
 July 12 2019 Phase 2

Chemical Information & Solubility

Molecular Weight 507.53 Formula

C27H27F2N5O3
CAS No. 1787294-07-8 SDF --
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
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (197.03 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 4 mg/mL

Water : Insoluble


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