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| Size | Price | Stock |
|---|---|---|
| 250mg | $3200 | Check With Us |
| 500mg | $5000 | Check With Us |
| 1g | $7500 | Check With Us |
: Cat #: V32253 CAS #: 1787294-07-8 Purity ≥ 99%
Description: Remibrutinib (LOU-064) is a potent, highly selective and orally bioavailable covalent inhibitor of bruton tyrosine kinase (BTK) with an IC50 of 0.023μM. It has the potential for Chronic urticaria (CU) treatment. 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. It demonstrates potent in vivo target occupancy with an EC90 of 1.6 mg/kg and dose-dependent efficacy in rat collagen-induced arthritis. LOU064 is currently being tested in phase 2 clinical studies for chronic spontaneous urticaria and Sjoegren's syndrome. Bruton's tyrosine kinase (BTK), a cytoplasmic tyrosine kinase, plays a central role in immunity and is considered an attractive target for treating autoimmune diseases. The use of currently marketed covalent BTK inhibitors is limited to oncology indications based on their suboptimal kinase selectivity.
References: [1]. Daniela Angst, et al. Novel amino pyrimidine derivatives. Patent WO2015079417A1.
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| Molecular Weight (MW) | 507.5418 |
|---|---|
| Molecular Formula | C₂₇H₂₇F₂N₅O₃ |
| CAS No. | 1787294-07-8 |
| SMILES Code | O=C(NC1=CC(F)=CC(C2=NC=NC(N)=C2OCCN(C)C(C=C)=O)=C1C)C3=CC=C(C4CC4)C=C3F |
| Synonyms | LOU064; LOU-064; LOU 064; Remibrutinib; |
| Protocol | In Vitro | In a biochemical enzyme assay,Remibrutinib (example 6) inhibits Btk enzymatic activity with an IC50 value of 1 nM. 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. |
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| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 1.9703 mL | 9.8514 mL | 19.7028 mL | 39.4056 mL |
| 5mM | 0.3941 mL | 1.9703 mL | 3.9406 mL | 7.8811 mL |
| 10mM | 0.1970 mL | 0.9851 mL | 1.9703 mL | 3.9406 mL |
| 20mM | 0.0985 mL | 0.4926 mL | 0.9851 mL | 1.9703 mL |
This equation is commonly abbreviated as: C1 V1 = C2 V2
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.