PeptideDB

JC124 1638611-48-9

JC124 1638611-48-9

CAS No.: 1638611-48-9

JC124 is a specific NLRP3 inflammasome inhibitor. JC124 has anti~inflammatory and neuro-protective (neuro-protection) ef
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JC124 is a specific NLRP3 inflammasome inhibitor. JC124 has anti~inflammatory and neuro-protective (neuro-protection) effects.

Physicochemical Properties


Molecular Formula C17H19CLN2O4S
Molecular Weight 382.861762285233
Exact Mass 382.075
Elemental Analysis C, 53.33; H, 5.00; Cl, 9.26; N, 7.32; O, 16.72; S, 8.37
CAS # 1638611-48-9
Related CAS # 1638611-48-9;
PubChem CID 117715670
Appearance Light yellow to yellow solid powder
LogP 2.8
Hydrogen Bond Donor Count 2
Hydrogen Bond Acceptor Count 5
Rotatable Bond Count 7
Heavy Atom Count 25
Complexity 529
Defined Atom Stereocenter Count 0
InChi Key LXYPQRJNQPYTQW-UHFFFAOYSA-N
InChi Code

InChI=1S/C17H19ClN2O4S/c1-19-25(22,23)14-6-3-12(4-7-14)9-10-20-17(21)15-11-13(18)5-8-16(15)24-2/h3-8,11,19H,9-10H2,1-2H3,(H,20,21)
Chemical Name

5-chloro-2-methoxy-N-[2-[4-(methylsulfamoyl)phenyl]ethyl]benzamide
Synonyms

JC 124; JC-124; JC124
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)

Biological Activity


ln Vitro It has been demonstrated that JC124 can specifically prevent the production of NLRP3 inflammasomes, activate caspase-1, and lower IL-1β in vitro[1].
ln Vivo Injury-induced deteriorated neuronal numbers, inflammatory cell responses in injured brain, and cortical lesion volume were all significantly reduced by JC124 (100 mg/kg; i.p.; 4 doses; 30 minutes post-injury, 6, 24, and 30 hours post-TBI) treatment. The protein expression levels of NLRP3, ASC, IL-1 beta, TNFα, iNOS, and caspase-1 are similarly markedly decreased by JC124 [1].
Animal Protocol Animal/Disease Models: Adult male SD (SD (Sprague-Dawley)) rats (3-4 months old) with traumatic brain injury (TBI) [1]
Doses: 100 mg/kg
Route of Administration: intraperitoneal (ip) injection; 4 doses; 30 days after injury Minutes, 6, 24, and 30 hrs (hrs (hours)) after TBI
Experimental Results: Significant reduction in the number of injury-induced degenerated neurons, inflammatory cell responses in the injured brain, and cortical lesion volume.
References

[1]. A novel small molecular NLRP3 inflammasome inhibitor alleviates neuroinflammatory response following traumatic brain injury. J Neuroinflammation. 2019 Apr 11;16(1):81.


Solubility Data


Solubility (In Vitro) DMSO : ~250 mg/mL (~652.98 mM)
Solubility (In Vivo) Solubility in Formulation 1: ≥ 2.08 mg/mL (5.43 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 (5.43 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication.
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 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

Solubility in Formulation 3: ≥ 2.08 mg/mL (5.43 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 2.6119 mL 13.0596 mL 26.1192 mL
5 mM 0.5224 mL 2.6119 mL 5.2238 mL
10 mM 0.2612 mL 1.3060 mL 2.6119 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.