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Art. -Nr.: HY-151920

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BTK-IN-17

BTK-IN-17 (compound 36R) is a selective and orally activeBTK inhibitor with an IC₅₀ value of 13.7 nM. BTK-IN-17 decreases the expression of p-BTK^Y223 and p-PLCγ2^Y1217. BTK-IN-17 shows anti-inflammatory effects.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Formel: C₂₆H₂₃N₇O₂
Molecular Weight:465.51

Speicherung:

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

Data Sheet (276 KB)

BTK-IN-17 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
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC₅₀: 13.7 nM (BTK)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
PBMC	IC₅₀	53.1 nM Compound: 36R	Antiinflammatory activity in human PBMC assessed as inhibition of anti-IgM induced CD69 expression incubated for 2 hrs followed by goat F(ab') 2 anti-human IgM addition measured after 18 hrs by flow cytometry analysis Antiinflammatory activity in human PBMC assessed as inhibition of anti-IgM induced CD69 expression incubated for 2 hrs followed by goat F(ab') 2 anti-human IgM addition measured after 18 hrs by flow cytometry analysis	[PMID: 36462441]

In Vitro

BTK-IN-17 (compound 36R) shows hERG channel inhibition with an IC₅₀ value of 8.6 µM^[1].
BTK-IN-17 (0-10000 nM) decreases the expression of p-BTK^Y223 and p-PLCγ2^Y1217 in Ramos cells^[1].

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

Western Blot Analysis^[1]

Cell Line:

Ramos cells
Concentration:

0-10000 nM
Incubation Time:
Result:

Inhibited phosphorylation of downstream BTK (p-BTKY223) and phosphorylation of PLCγ2 (p-PLCγ2Y1217).

In Vivo

BTK-IN-17 (1 mg/kg for i.v.; 10 mg/kg for p.o.) shows the plasma concentrations rapidly reached 125 nM and BTK occupancy reached 79%one hour after oral administration, target occupancy of roughly 62% was maintained after 24 h in rats^[1].
BTK-IN-17 (10, 30, 50 mg/kg; p.o.; once daily for 10 days) shows good anti-inflammatory effects in rats^[1].
Pharmacokinetic Parameters of BTK-IN-17 in Male Sprague-Dawley rats^[1].

	iv (1 mg/kg)	po (10 mg/kg)
C₀ (ng·mL^-1)	786±121	-
C _max (ng·mL^-1)	-	52.5±11.3
T_1/2 (h)	0.73±0.05	1.67±0.27
T_max (h)	-	1.00±0.5
AUC(ng·h·mL^-1)	454±25	164±18
CL (mL·kg^-1·min^-1)	36.8±2.0	-
Vd_ss (L·kg^-1)	1.67±0.04	-
F (%)	-	3.6±0.4

Sprague-Dawley rats, 1 mg/kg for i.v.; 10 mg/kg p.o.^[1].

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

Chemical Information

Molecular Weight 465.51
Formel C₂₆H₂₃N₇O₂
SMILES

C=CC(N1CC[C@H](C1)N2N=C(C3=CNC4=NC=NC2=C34)NC5=CC=C(C=C5)OC6=CC=CC=C6)=O
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

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Fang X, et al. Discovery of orally active 1,4,5,6,8-pentaazaacenaphthylens as novel, selective, and potent covalent BTK inhibitors for the treatment of rheumatoid arthritis. Eur J Med Chem. 2022 Nov 25;246:114940. [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

Keywords

MOQ

Minimum order quantity

100 mg

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