NLRP3-IN-42
NLRP3-IN-42 (compound H28) is a potent NLRP3 inhibitor with an KD value of 1.15 µM. NLRP3-IN-42 decreases the LPS (HY-D1056) induced protein expression of cleaved-caspase-1 (p20). NLRP3-IN-42 selectively inhibits IL-1β release.
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- CAS No.: 3040024-62-9
- 화학식: C29H27F3N2O3S2
- 분자량:572.66
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
IC50 & Target
[1]|
NLRP3 1.15 μM (Kd) |
IL-1β |
In Vitro
NLRP3-IN-42 (compound H28) (0-30 µM) decreases the LPS (HY-D1056) induced protein expression of cleaved-caspase-1 (p20) in a dose-dependent manner[1].
NLRP3-IN-42 can stably bind to the ADP active site of the NLRP3 NACHT domain[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:J774A.1 cells
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Concentration:0, 3, 10, 30 µM
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Incubation Time:2.5 h + 30 min
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Result:Decreased the LPS (1 μg/mL) induced protein expression of cleaved-caspase-1 (p20) in culture supernatants (SN) and whole cell lysates (WCL) in a dose-dependent manner.
In Vivo
Pharmacokinetic Parameters (ICR mice)[1].
| PK parameters | H28 |
| Administered dose (mg/kg) | iv at 2.5 mg/kg |
| AUC0-∞ (h*ng/mL) | 1189 ± 137 |
| t1/2 (h) | 1.69 ± 0.38 |
| CL (mL/h/kg) | 35.36 ± 4.12 |
| Cmax (ng/mL) | 2987 ± 281 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:4-8 weeks, Male C57BL/6 mice[1]
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Dosage:10 mg/kg
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Administration:I.p; 1 h before injection of LPS (35 mg/kg, ip) for 2.5 h
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Result:Significantly inhibited IL-1β production in the treatment mice. It is noteworthy that the treatment with these compounds do not result in significant inhibition of TNF-α levels.
Chemical Information
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CAS No. 3040024-62-9
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분자량 572.66
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화학식 C29H27F3N2O3S2
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SMILES
CCCNS(=O)(C1=CC=C(C2=CC=CC=C2N(CC3=CC=C(C(F)(F)F)C=C3)C(CC4=CSC=C4)=O)C=C1)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
NLRP3-IN-42 Related Classifications
HY-163744 Related Classifications
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