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

YQ128 

Cat. No.: HY-130252 Purity: 99.65%
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

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 420 In-stock
Estimated Time of Arrival: December 31
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 550 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1650 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2250 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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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
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (458.62 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8345 mL 9.1725 mL 18.3449 mL
5 mM 0.3669 mL 1.8345 mL 3.6690 mL
10 mM 0.1834 mL 0.9172 mL 1.8345 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (3.82 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (3.82 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

YQ128YQ 128YQ-128NOD-like Receptor (NLR)Interleukin RelatedILInhibitorinhibitorinhibit

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YQ128
Cat. No.:
HY-130252
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