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-BTKY223 and p-PLCγ2Y1217. BTK-IN-17 shows anti-inflammatory effects.
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- Formule: C26H23N7O2
- Masse moléculaire:465.51
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Activité biologique
Description
IC50 & Target
IC50: 13.7 nM (BTK)[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| PBMC | IC50 |
53.1 nM
Compound: 36R
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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
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[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-BTKY223 and p-PLCγ2Y1217 in Ramos cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Ramos cells
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Concentration:0-10000 nM
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Incubation Time:
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Result:Inhibited phosphorylation of downstream BTK (p-BTKY223) and phosphorylation of PLCγ2 (p-PLCγ2Y1217).
In Vivo
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 |
| T1/2 (h) | 0.73±0.05 | 1.67±0.27 |
| Tmax (h) | - | 1.00±0.5 |
| AUC(ng·h·mL-1) | 454±25 | 164±18 |
| CL (mL·kg-1·min-1) | 36.8±2.0 | - |
| Vdss (L·kg-1) | 1.67±0.04 | - |
| F (%) | - | 3.6±0.4 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Masse moléculaire 465.51
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Formule C26H23N7O2
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SMILES
C=CC(N1CC[C@H](C1)N2N=C(C3=CNC4=NC=NC2=C34)NC5=CC=C(C=C5)OC6=CC=CC=C6)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
BTK-IN-17 Related Classifications
HY-151920 Related Classifications
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