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

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. YQ128 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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YQ128 Chemical Structure

YQ128 Chemical Structure

CAS No. : 2454246-18-3

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10 mM * 1 mL in DMSO
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Customer Review

Based on 1 publication(s) in Google Scholar

YQ128 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

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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]. YQ128 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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].

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

YQ128 Related Antibodies

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].

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

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
CAS No.
Appearance

Solid

Color

White to off-white

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 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (458.62 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8345 mL 9.1725 mL 18.3449 mL 45.8623 mL
5 mM 0.3669 mL 1.8345 mL 3.6690 mL 9.1725 mL
10 mM 0.1834 mL 0.9172 mL 1.8345 mL 4.5862 mL
15 mM 0.1223 mL 0.6115 mL 1.2230 mL 3.0575 mL
20 mM 0.0917 mL 0.4586 mL 0.9172 mL 2.2931 mL
25 mM 0.0734 mL 0.3669 mL 0.7338 mL 1.8345 mL
30 mM 0.0611 mL 0.3057 mL 0.6115 mL 1.5287 mL
40 mM 0.0459 mL 0.2293 mL 0.4586 mL 1.1466 mL
50 mM 0.0367 mL 0.1834 mL 0.3669 mL 0.9172 mL
60 mM 0.0306 mL 0.1529 mL 0.3057 mL 0.7644 mL
80 mM 0.0229 mL 0.1147 mL 0.2293 mL 0.5733 mL
100 mM 0.0183 mL 0.0917 mL 0.1834 mL 0.4586 mL
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YQ128 Related Classifications

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:

YQ1282454246-18-3YQ 128YQ-128NOD-like Receptor (NLR)Interleukin RelatedILInhibitorinhibitorinhibit

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