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Art. -Nr.: HY-182943

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BTK-IN-49

BTK-IN-49 is a selective, orally active and brain-penetrant BTK inhibitor with an IC₅₀ of 0.14 nM. BTK-IN-49 binds to BTK and blocks B-cell receptor and Fcγ receptor signaling. BTK-IN-49 inhibits the proliferation of CNS-compartmentalized B-cells and FcγR-induced microglial proliferation in a BTK-dependent manner. BTK-IN-49 can be used for the study of multiple sclerosis.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Formel: C₂₆H₃₀N₈O₂
Molecular Weight:486.57

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

BTK-IN-49 Chemical Structure

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Preis

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

In Vitro

BTK-IN-49 (compound 13) inhibits recombinant active BTK enzyme with an IC₅₀ of 0.14 nM and suppresses CD69 expression on human CD19⁺ B-cells in whole blood with an IC₅₀ of 0.23 μM^[1].
BTK-IN-49 inhibits hERG channels with an IC₅₀ of 25 μM, suggesting moderate cardiovascular risk^[1].
BTK-IN-49 (1 μM) shows good kinome selectivity, inhibiting only BTK, KIT, and SRC by > 90% at 1 μM across a panel of 468 kinases^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Parmacokinetics

Species	Dose	Route	V	CL
Mice^[1]	50 mg/kg	p.o.	3866 mL/kg	261 mL/h/kg
Mice^[1]	125 mg/kg	p.o.	3866 mL/kg	261 mL/h/kg
Mice^[1]	250 mg/kg	p.o.	3866 mL/kg	261 mL/h/kg

In Vivo

BTK-IN-49 (compound 13) (50-250 mg/kg; p.o.; twice daily; 4-7 days) shows CNS exposures above the human WB anti-CD69 IC₇₀-IC₉₀ correlate with reduced tolerability, with the 50 mg/kg BID dose tolerated for 7 days in healthy C57BL/6 mice^[1].
BTK-IN-49 (5-50 mg/kg; p.o.; every 12 hours; 60 hours) robustly inhibits proliferation of CNS-compartmentalized B-cells in NOD.SCID mice, while peripherally restricted inhibitors show no activity^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Related Protocols :

Cell Viability Determination by MTT Colorimetric Assay

Chemical Information

Molecular Weight 486.57
Formel C₂₆H₃₀N₈O₂
SMILES

CC(C)(C)C1=NC(C(N[C@H]2C3=CC=C(C4=CC=NC(NC5=NN(C)C=C5)=N4)C=C3CCCC2)=O)=NO1
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Hopkins BT, et al. Leveraging Kinase Drugs for Neurosciences: Discovery of Selective, CNS-Penetrant Reversible Bruton's Tyrosine Kinase Inhibitors as Therapeutics for Neuroinflammation. J Med Chem. Published online April 7, 2026. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

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MOQ

Minimum order quantity

100 mg

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