NP3-742
NP3-742 is an orally active NLRP3 inhibitor that binds to the NLRP3 NACHT domain. NP3-742 inhibits IL-1β release with IC50s of 6 nM and 47 nM in both the cellular and whole blood assays, respectively. NP3-742 is highly selective against a panel of more than 50 enzymes, receptors and sodium and calcium channels. NP3-742 can be used for the study of gout, cardiovascular disease or osteoarthritis.
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- Fòrmula: C19H24N6
- Peso molecular:336.43
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
NLRP3 |
IL-1β 6 nM (IC50) |
In Vitro
Parmacokinetics
| Species | Dose | Route | CL | Vss | T1/2 | F |
|---|---|---|---|---|---|---|
| Dog[1] | 0.1 mg/kg | i.v. | 10 mL/min/kg | 6.3 L/kg | 9.4 h | / |
| Dog[1] | 0.3 mg/kg | p.o. | 10 mL/min/kg | 6.3 L/kg | 9.4 h | 75 % |
| Mice[1] | 1 mg/kg | i.v. | 27 mL/min/kg | 2.9 L/kg | 2.0 h | / |
| Mice[1] | 3 mg/kg | p.o. | 27 mL/min/kg | 2.9 L/kg | 2.0 h | 54 % |
| Rat[1] | 0.3 mg/kg | i.v. | 29 mL/min/kg | 6.9 L/kg | 3.9 h | / |
| Rat[1] | 3 mg/kg | p.o. | / | 6.9 L/kg | 29 mL/min/kg | 93 % |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female C57BL6/JRj mice (7-13 weeks) were challenged with LPS (2.5 mg/kg) for 2 h[1]
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Dosage:0.3 mg/kg, 1 mg/kg, 3 mg/kg
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Administration:Oral; 1 h prior to LPS; once
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Result:Showed complete inhibition of IL-1β in the acute mouse peritonitis model when administered at 3 mg/kg p.o.
Lower doses of 1 and 0.3 mg/kg, resulted in 78 and 66% efficacy, respectively.
Chemical Information
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Peso molecular 336.43
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Fòrmula C19H24N6
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SMILES
CC1=CC2=C(N1)N=C(C=C2)C3=C(C=C(N=N3)N[C@@H]4CCCN(C4)C)C
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
NP3-742 Related Classifications
HY-179024 Related Classifications
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