1. Immunology/Inflammation
  2. NOD-like Receptor (NLR)
    Interleukin Related
  3. YQ128

YQ128 

Cat. No.: HY-130252
Handling Instructions

YQ128 is a potent and selective second-generation NLRP3 (NOD-like receptor P3) inflammasome inhibitor with an IC50 of 0.30 µM. YQ128 significantly and selectively suppresses the production of IL-1β, but not TNF-α, and it can cross the BBB to reach the CNS. YQ128 has anti-inflammatory activity.

For research use only. We do not sell to patients.

YQ128 Chemical Structure

YQ128 Chemical Structure

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Description

YQ128 is a potent and selective second-generation NLRP3 (NOD-like receptor P3) inflammasome inhibitor with an IC50 of 0.30 µM. YQ128 significantly and selectively suppresses the production of IL-1β, but not TNF-α, and it can cross the BBB to reach the CNS. YQ128 has anti-inflammatory activity[1].

IC50 & Target[1]

NLRP3

0.30 μM (IC50)

IL-1β

 

In Vitro

YQ128 (0.3-100 µM; 30 mins) dose dependently suppressed the release of IL-1β from peritoneal macrophages upon LPS/ATP challenge with an IC50 of 1.59 µM[1].
YQ128 (20 µM; 2 hours) shows no significant toxic effects on hCMEC/D3 cells[1].

Cell Viability Assay[1]

Cell Line: Mouse peritoneal macrophages
Concentration: 0.3, 1.0, 3.0, 10, 30, 100 µM
Incubation Time: 30 mins
Result: Suppressed the release of IL-1β from peritoneal macrophages upon LPS/ATP challenge with an IC50 of 1.59 µM.
In Vivo

YQ128 (iv; 20 mg/kg) has an intermediate terminal plasma half-life (t1/2) of 6.6 hours after iv administration[1].
YQ128 (oral; 20 mg/kg) shows delayed gastrointestinal absorption with a tmax and cmax of 12 h and 73 ng/mL, respectively. Oral bioavailability (Foral) is estimated as 10%[1].
YQ128 exhibits extensive extravascular distribution with a large steady-state volume of distribution (Vdss) of 8.5 L/kg and rapid total clearance (CLtot) of 41 mL/min/kg[1].
YQ128 (10 mg/kg) has been shown to trigger IL-1β production in a NLRP3- dependent manner in C57BL/6 mice[1].

Animal Model: Sprague-Dawley rats (200-250 g)[1]
Dosage: 20 mg/kg (Pharmacokinetic Analysis)
Administration: Iv
Result: Had an intermediate terminal plasma half-life (t1/2) of 6.6 hours after iv administration.
Molecular Weight

545.11

Formula

C₂₇H₂₉ClN₂O₄S₂

SMILES

O=S(C1=CC=C(CCN(CC2=C(C=CC(Cl)=C2)OCCC)C(CC3=CSC=C3)=O)C=C1)(NCC#C)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
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YQ128
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HY-130252
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