2. Immunology/Inflammation
  3. NOD-like Receptor (NLR)
  4. NLRP3-IN-10

NLRP3-IN-10 is a potent NLRP3 inhibitor, inhibits IL-1β release with an IC50 value of 251.1 nM. NLRP3-IN-10 suppresses NLRP3 inflammasome activation by attenuating ASC speck formation.

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NLRP3-IN-10 Chemical Structure

NLRP3-IN-10 Chemical Structure

CAS No. : 2641826-39-1

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Based on 1 publication(s) in Google Scholar

NLRP3-IN-10 Related Antibodies

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Description

NLRP3-IN-10 is a potent NLRP3 inhibitor, inhibits IL-1β release with an IC50 value of 251.1 nM. NLRP3-IN-10 suppresses NLRP3 inflammasome activation by attenuating ASC speck formation[1].

IC50 & Target

NLRP3

251.1 nM (IC50)

In Vitro

NLRP3-IN-10 (compound 14c) (0.4, 1.6, 6.4 μM; 40 min) exerts remarkable inhibitory activity on NLRP3 inflammasome activation induced by LPS-MSU (12 h) in THP-1 cells in a dose-dependent manner[1].
NLRP3-IN-10 (0.1-6.4 μM; 1.5 h) shows no cytotoxicity against THP-1 cells and (0.1, and 0.4 μM; 40 min) avoids Nigericin (HY-127019)-induced pyroptosis[1].
NLRP3-IN-10 (0.1, 0.2, and 0.4 μM; 40 min) reduces the processing of caspase-1 p20 and IL-1β, in supernatants in THP-1 cells in a dose-dependent manner[1].
NLRP3-IN-10 (3 μM and 5 μM; 40 min) decreases LPS-induced THF-α, and (0.2 μM and 0.8 μM; 40 min) reduces the rate of THP-1 cells with ASC specks, indicating ASC oligomerization interruptionsup>[1].
NLRP3 inflammasome is regarded as a two-step process, including priming and action. NLRP3-IN-10 (1, 10, and 100 μM; 40 min) suppresses LPS-induced NLRP3 priming through directly interacting with NLRP3[1].

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

NLRP3-IN-10 Related Antibodies
In Vivo

NLRP3-IN-10 (compound 14c) (10 mg/kg; i.v.; single dose) reduces peritoneal neutrophil influx in mice and IL-1β in the spleen in the MSU-induced peritonitis in LPS-primed mouse model[1].
NLRP3-IN-10 (10, 30, 90 mg/kg; p.o.; single dose) exhibits extremely low exposure (14.6−23.53 μg·h/L), poor bioavailability (2.47−13.79%), and high plasma clearance (2201.58−5551.12 L/h/kg) after different doses for oral administration[1].
Pharmacokinetics of NLRP3-IN-10 in mouse[1]

Route Dose (mg/kg) AUC0-t (μg·h/L) CL (L/h/kg) Cmax (μg/L) T1/2 (h) Tmax (h) F (%)
IV 10 105.88 133.75 81.97 3.13 0.11
PO 10 14.60 2201.58 3.35 7.43 2.11 13.79
PO 30 15.84 2583.27 16.42 7.92 1.26 4.99
PO 90 23.53 5551.12 13.59 6.08 4.21 2.47

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

Animal Model: MSU-induced peritonitis in a LPS-primed mouse model (C57BL/6J mice, 7-week-old, male)[1]
LPS: 1 mg/kg, i.p.; MSU: 100 mg/kg, i.v.
Dosage: 10 mg/kg
Administration: Intravenous injection; single dose
Result: Significantly reduced IL-1β release in the spleen of mice after 6 h treatment.
Significantly reduced the increase of peritoneal neutrophil influx compared with the control group.
Molecular Weight

365.19

Formula

C17H14BrFO3
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

BrC(C=C1OC)=C(C=C1/C=C/C(C2=CC=C(C=C2)F)=O)OC
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 : 100 mg/mL (273.83 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 2.7383 mL 13.6915 mL 27.3830 mL
5 mM 0.5477 mL 2.7383 mL 5.4766 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7383 mL 13.6915 mL 27.3830 mL 68.4575 mL
5 mM 0.5477 mL 2.7383 mL 5.4766 mL 13.6915 mL
10 mM 0.2738 mL 1.3692 mL 2.7383 mL 6.8458 mL
15 mM 0.1826 mL 0.9128 mL 1.8255 mL 4.5638 mL
20 mM 0.1369 mL 0.6846 mL 1.3692 mL 3.4229 mL
25 mM 0.1095 mL 0.5477 mL 1.0953 mL 2.7383 mL
30 mM 0.0913 mL 0.4564 mL 0.9128 mL 2.2819 mL
40 mM 0.0685 mL 0.3423 mL 0.6846 mL 1.7114 mL
50 mM 0.0548 mL 0.2738 mL 0.5477 mL 1.3692 mL
60 mM 0.0456 mL 0.2282 mL 0.4564 mL 1.1410 mL
80 mM 0.0342 mL 0.1711 mL 0.3423 mL 0.8557 mL
100 mM 0.0274 mL 0.1369 mL 0.2738 mL 0.6846 mL
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NLRP3-IN-10 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:

NLRP3-IN-102641826-39-1NOD-like Receptor (NLR)inflammasome activationASC speck formationnanomolar rangechalcone analoguesSARanti-inflammationselectivityInhibitorinhibitorinhibit

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