| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 100mg | |||
| Other Sizes |
| Targets |
NLRP3 inflammasome. JC-171 selectively inhibits NLRP3 inflammasome activation. The compound prevents the assembly of the inflammasome complex, thereby blocking the activation of caspase-1 and the subsequent release of pro-inflammatory cytokines such as interleukin-1β and interleukin-18.
|
|---|---|
| ln Vitro |
In primary macrophages, JC-171 (0-100 μM) dose-dependently inhibits the activation of the NLRP3 inflammasome and the generation of IL-1β [1].
JC-171 inhibits LPS/ATP-induced IL-1β release from J774A.1 macrophages with an IC₅₀ of 8.45 μM. JC-171 (0-100 μM) inhibits NLRP3 inflammasome activation and IL-1β production in primary macrophages in a dose-dependent manner. Cell viability is assessed using J774A.1 murine macrophage cells. |
| ln Vivo |
JC-171 therapy delays the course and lowers the severity of experimental autoimmune encephalomyelitis (EAE) in mice [1].
JC-171 treatment delays progression and reduces the severity of experimental autoimmune encephalomyelitis (EAE) in mice. The compound effectively reduces inflammatory signaling and pyroptotic cell death in vivo. JC-171 is used in immunology and inflammation research, particularly in autoimmune and neurodegenerative diseases. |
| Enzyme Assay |
NLRP3 inflammasome activation assay: J774A.1 murine macrophages are primed with LPS and then treated with JC-171 at varying concentrations (0-100 μM) before ATP stimulation. Culture supernatants are collected, and IL-1β levels are measured by ELISA. The inhibition of IL-1β release is calculated, and IC₅₀ values are determined.
|
| Cell Assay |
Cell viability assay[1]
Cell Types: J774A.1 mouse macrophage Tested Concentrations: 0-100 μM. Incubation Duration: 0.5 hrs (hours) (4.5 hrs (hours) before LPS (1 μg/mL) treatment). Experimental Results: Inhibited the release of IL-1β in J774A.1 cells after LPS/ATP stimulation. Cytokine production assay: Primary macrophages are treated with JC-171 at varying concentrations (0-100 μM) in a dose-dependent manner. Cells are stimulated with LPS/ATP. IL-1β and IL-18 levels in culture supernatants are measured by ELISA. Caspase-1 activation is assessed by Western blot or fluorogenic substrate cleavage. |
| Animal Protocol |
Animal/Disease Models: On day 0, mice were immunized subcutaneously (sc) (sc) with 200 μg of myelin oligodendrocyte glycoprotein (MOG) 35-55 peptide emulsified in Freund's complete adjuvant (CFA), followed by injection of 200 ng of pertussis toxin .
Doses: 100 mg/kg, 10 mg/kg. Route of Administration: IP on days 0, 1, and 2; every other day thereafter (100 mg/kg). Dosing (10 mg/kg) was started every other day starting when an individual mouse's clinical score reached 1 (flaggy tail). Experimental Results: Compared with vehicle treatment, EAE progression was effectively inhibited. Resulting in a substantial decrease in the frequency of MOG35-55-specific Th17 cells in the spleen and spinal cord of EAE mice. EAE mouse model: Mice are immunized subcutaneously with 200 μg MOG₃₅₋₅₅ peptide emulsified in CFA on day 0, followed by pertussis toxin injection. JC-171 is administered at various doses. Disease progression is monitored by clinical scoring, and severity is assessed by histological analysis of spinal cords. |
| ADME/Pharmacokinetics |
JC-171 has a molecular weight of 384.83 g/mol and molecular formula C₁₆H₁₇ClN₂O₅S. Solubility: DMSO 250 mg/mL (649.64 mM). In vivo formulation: 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline. Storage: powder at -20°C for 3 years.
|
| Toxicity/Toxicokinetics |
No detailed toxicity data has been published. JC-171 is for research use only. Standard laboratory safety practices should be followed when handling this compound. As an NLRP3 inhibitor, potential effects on immune function should be considered.
|
| References | |
| Additional Infomation |
JC-171 is a selective NLRP3 inflammasome inhibitor with an IC₅₀ of 8.45 μM for inhibiting LPS/ATP-induced IL-1β release. It blocks inflammasome assembly, caspase-1 activation, and pro-inflammatory cytokine release. JC-171 delays EAE progression in mice and is used in autoimmune and inflammation research. No clinical trials or approved上市 status have been reported.
|
| Molecular Formula |
C16H17CLN2O5S
|
|---|---|
| Molecular Weight |
384.834582090378
|
| Exact Mass |
384.054
|
| CAS # |
2112809-98-8
|
| PubChem CID |
134600183
|
| Appearance |
White to off-white solid powder
|
| LogP |
2.3
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
25
|
| Complexity |
531
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
ClC1C=CC(=C(C=1)C(NCCC1C=CC(=CC=1)S(NO)(=O)=O)=O)OC
|
| InChi Key |
KQRQPMUPYDOTCA-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C16H17ClN2O5S/c1-24-15-7-4-12(17)10-14(15)16(20)18-9-8-11-2-5-13(6-3-11)25(22,23)19-21/h2-7,10,19,21H,8-9H2,1H3,(H,18,20)
|
| Chemical Name |
5-chloro-N-[2-[4-(hydroxysulfamoyl)phenyl]ethyl]-2-methoxybenzamide
|
| Synonyms |
JC-171; JC 171; JC171
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~649.64 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.40 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.40 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5986 mL | 12.9928 mL | 25.9855 mL | |
| 5 mM | 0.5197 mL | 2.5986 mL | 5.1971 mL | |
| 10 mM | 0.2599 mL | 1.2993 mL | 2.5986 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
