2. Immunology/Inflammation
  3. NOD-like Receptor (NLR) Interleukin Related
  4. 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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NP3-742

NP3-742 Estructura química

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NP3-742 Related Antibodies

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Descripciòn

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[1].

IC50 & Target[1]

NLRP3

 

IL-1β

6 nM (IC50)

In Vitro

NP3-742 has reduces hERG inhibition[1].
NP3-742 is metabolically stable (<25 μL/min/mg) in mouse, rat, dog and human liver microsomes[1].

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

NP3-742 Related Antibodies
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

NP3-742 (0.3-3 mg/kg; Oral; 1 h prior to LPS) exhibits full inhibition of IL-1β production at 3 mg/kg in te acute mouse peritonitis model[1].

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

Animal Model: Female C57BL6/JRj mice (7-13 weeks) were challenged with LPS (2.5 mg/kg) for 2 h[1]
Dosage: 0.3 mg/kg, 1 mg/kg, 3 mg/kg
Administration: Oral; 1 h prior to LPS; once
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.
Peso molecular

336.43

Fòrmula

C19H24N6
SMILES

CC1=CC2=C(N1)N=C(C=C2)C3=C(C=C(N=N3)N[C@@H]4CCCN(C4)C)C
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
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NP3-742 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

NP3-742NOD-like Receptor (NLR)Interleukin RelatedILinflammasomein vivo efficacyIL-1βNLRP3Inhibitorinhibitorinhibit

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Nombre del producto:
NP3-742
Cat. No.:
HY-179024
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