Rilzabrutinib is a next‑generation, reversible covalent BTK inhibitor being developed for immune‑mediated diseases. As a reversible covalent inhibitor, Rilzabrutinib combines the potency of covalent target engagement with the reversibility that may offer a more favorable safety profile compared to irreversible covalent inhibitors. Rilzabrutinib demonstrates an IC₅₀ of 1.3 ± 0.5 nM for BTK and is highly selective, with minimal off‑target activity against a panel of 251 other kinases. Rilzabrutinib is being investigated for chronic spontaneous urticaria, a condition characterized by persistent hives and itching that is often refractory to antihistamine therapy. The reversible covalent mechanism of Rilzabrutinib represents a novel approach to BTK inhibition that may offer advantages in both efficacy and safety for chronic autoimmune and inflammatory diseases.
Product Parameters
|
Parameter |
Specification |
|
Product Name |
Rilzabrutinib |
|
CAS Number |
1575596-29-0 |
|
Molecular Formula |
|
|
Molecular Weight |
|
|
Boiling Point |
882.5±65.0℃ |
|
Density |
1.39±0.1 |
|
pKa |
6.24±0.70 |
|
Storage Condition |
Store at -20℃ |
Why Cosperpharm?
Reversible covalent inhibition demands structural integrity. The reversible covalent binding mechanism of Rilzabrutinib depends on the integrity of the α,β‑unsaturated nitrile warhead—any degradation or impurity can alter binding kinetics and biological activity. Our analytical release protocol for Rilzabrutinib includes HPLC purity verification (98.97%), mass spectrometry identity confirmation, and comprehensive impurity profiling—because your research outcomes depend on the structural integrity of this novel BTK inhibitor.
Documentation that supports your research. Every shipment includes a Certificate of Analysis (COA) with batch‑specific HPLC purity, chromatographic traceability, and residual solvent data. Stability summaries and custom quality agreements are available upon request.
Flexible supply for all research stages. Cosperpharm supplies Rilzabrutinib from milligram quantities for in vitro studies to gram quantities for preclinical development. R&D samples ship within 5–7 business days.
Technical support for BTK inhibitor research. Our scientific team can advise on solubility optimization, formulation for in vivo studies, and analytical methods for detecting process‑related impurities—because we have extensive experience with this class of reversible covalent kinase inhibitors.
Global reach with transparent pricing. Cosperpharm ships to research institutions, CROs, and pharmaceutical companies worldwide, with full customs documentation included.
Product Advantages
Rilzabrutinib is a reversible covalent BTK inhibitor that combines the potency of covalent target engagement with the reversibility that may offer improved safety profiles. This differentiated mechanism represents a novel approach to BTK inhibition for chronic autoimmune and inflammatory diseases.
Potent Activity with IC₅₀ of 1.3 nM
Rilzabrutinib demonstrates an IC₅₀ of 1.3 ± 0.5 nM for BTK, making it one of the most potent reversible covalent BTK inhibitors in development. This exceptional potency supports robust inhibition of BTK‑mediated signaling pathways.
Exceptional Kinase Selectivity
Rilzabrutinib is highly selective when tested against a panel of 251 other kinases. This exceptional selectivity minimizes off‑target effects and supports a favorable safety profile in clinical development.
Orally Active with Convenient Dosing
Rilzabrutinib is orally active, supporting convenient oral administration in clinical development for chronic conditions such as chronic spontaneous urticaria.
Novel Therapeutic Approach for Chronic Spontaneous Urticaria
Rilzabrutinib is being developed for chronic spontaneous urticaria in patients who remain symptomatic despite H1 antihistamine use, representing a novel therapeutic approach for this debilitating condition with significant unmet medical need.
FAQ
A: Rilzabrutinib (PRN1008) is a reversible covalent, selective, and orally active inhibitor of Bruton‘s tyrosine kinase (BTK).
Q2: How does Rilzabrutinib differ from other BTK inhibitors?
A: Unlike irreversible covalent BTK inhibitors (e.g., ibrutinib), Rilzabrutinib is a reversible covalent inhibitor. This mechanism combines the potency of covalent target engagement with reversibility, potentially offering improved safety profiles.
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