Remibrutinib (LOU064)

Modify Date: 2025-08-23 20:52:41

Remibrutinib (LOU064) Structure
Remibrutinib (LOU064) structure
Common Name Remibrutinib (LOU064)
CAS Number 1787294-07-8 Molecular Weight 507.53
Density N/A Boiling Point N/A
Molecular Formula C27H27F2N5O3 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Remibrutinib (LOU064)


Remibrutinib, is a potent and orally active bruton tyrosine kinase (BTK) inhibitor with an IC50 value of 1 nM. Remibrutinib inhibits BTK activity with an IC50 value of 0.023 μM in blood[1]. Remibrutinib has the potential for Chronic urticaria (CU) treatment[2].

 Names

Name Remibrutinib

 Remibrutinib (LOU064) Biological Activity

Description Remibrutinib, is a potent and orally active bruton tyrosine kinase (BTK) inhibitor with an IC50 value of 1 nM. Remibrutinib inhibits BTK activity with an IC50 value of 0.023 μM in blood[1]. Remibrutinib has the potential for Chronic urticaria (CU) treatment[2].
Related Catalog
Target

IC50: 1 nM (BTK)[1]

In Vitro In a biochemical enzyme assay,Remibrutinib (example 6) inhibits Btk enzymatic activity with an IC50 value of 1 nM[1]. In vitro B cell activation assay, Remibrutinib inhibits Btk enzymatic activity in blood with an IC50 value of 0.023 μM, the whole blood is collected from the abdominal aorta of anaesthetized adult male Lewis rats[1].
References

[1]. Daniela Angst, et al. Novel amino pyrimidine derivatives. Patent WO2015079417A1.

[2]. Kolkhir P, et al. New treatments for chronic urticaria. Ann Allergy Asthma Immunol. 2019 Aug 23.

 Chemical & Physical Properties

Molecular Formula C27H27F2N5O3
Molecular Weight 507.53
InChIKey CUABMPOJOBCXJI-UHFFFAOYSA-N
SMILES C=CC(=O)N(C)CCOc1c(N)ncnc1-c1cc(F)cc(NC(=O)c2ccc(C3CC3)cc2F)c1C

 Remibrutinib (LOU064)Bioassay

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Name: Inhibition of Btk Enzymatic Activity Assay from US Patent US11673868: "Amino pyrimidi...
Source: BindingDB
Target: N/A
External Id: BindingDB_11294_1
Name: Inhibition of CD69 expression on CD19 positive B cells in anti-IgD stimulated human w...
Source: ChEMBL
Target: N/A
External Id: CHEMBL5133804
Name: Metabolic stability in human liver microsomes assessed as intrinsic clearance
Source: ChEMBL
Target: N/A
External Id: CHEMBL5133805
Name: Metabolic stability in rat liver microsomes assessed as intrinsic clearance
Source: ChEMBL
Target: N/A
External Id: CHEMBL5133806
Name: Inhibition of BTK (unknown origin) assessed as log ratio of Kinact/Ki
Source: ChEMBL
Target: Tyrosine-protein kinase BTK
External Id: CHEMBL5133802
Name: Clearance in iv dosed Sprague-Dawley rat
Source: ChEMBL
Target: N/A
External Id: CHEMBL5133803
Name: Inhibition of BTK (unknown origin)
Source: ChEMBL
Target: Tyrosine-protein kinase BTK
External Id: CHEMBL5133797
Name: Inhibition of Btk Enzymatic Activity from US Patent US10457647: "Amino pyrimidine der...
Source: BindingDB
Target: N/A
External Id: BindingDB_8763_1
Name: Intrinsic clearance in rat liver microsomes
Source: ChEMBL
Target: N/A
External Id: CHEMBL4358490
Name: Inhibition of BTK in human B cells assessed as reduction in anti-IgM/IL4-stimulated C...
Source: ChEMBL
Target: Tyrosine-protein kinase BTK
External Id: CHEMBL4358489
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