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| 25mg |
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| 50mg |
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Purity: ≥98%
JSH-23 HCl is designed as an inhibitor of NF-κB transcriptional activity with IC50 of 7.1 μM in RAW 264.7 cell line. In LPS-stimulated macrophages RAW 264.7, JSH-23 inhibits NF-κB transcriptional activity in a dose-dependent fashion. Its cytotoxicity is not the cause of this outcome. JSH-23 is discovered to significantly reduce the LPS-induced DNA binding activity of NF-κB while reducing nuclear NF-κB p65 amounts in the same condition. JSH-23 performs these functions without affecting IκB degradation. Additionally, JSH-23 exhibits inhibition effects on the expression of pro-inflammatory transcripts and enzymes, such as IL-6, IL-1β, COX-2, and TNF-α. JSH-23 also prevents the chromatin condensation brought on by apoptosis that is induced by LPS.
| Targets |
NF-κB (IC50 = 7.1 μM)
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|---|---|
| ln Vitro |
JSH-2 (1-300 μM; 24 hours) at less than <100 μM has no discernible cytotoxic effects on RAW 264.7 cells[1].
After being exposed to LPS for 1 h, NF-B p65 nuclear amount is significantly increased. JSH-23 (30 μM; 1 hour) treatment reduces nuclear NF-κB p65 content in RAW 264.7 cells stimulated by LPS in a dose-dependent manner[1]. |
| ln Vivo |
JSH-23 (orally given at doses of 1 mg/kg or 3 mg/kg twice daily for two weeks) significantly improves nerve conduction and blood flow deficits in diabetic rats[2].
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| Animal Protocol |
Male Sprague Dawley diabetic rats (250-270 g)
1 mg/kg, 3 mg/kg Orally administered; daily; for 2 weeks |
| References |
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| Additional Infomation |
JSH-23 is a diamine that is 1,2-phenylenediamine carrying a methyl substituent at position 4 and a 3-phenylpropyl substituent at position N1. It has a role as a NF-kappaB inhibitor. It is a diamine and a substituted aniline. It is functionally related to a 1,2-phenylenediamine.
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| Molecular Formula |
C16H21N2
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|---|---|---|
| Molecular Weight |
276.81
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| Exact Mass |
240.162
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| CAS # |
749886-87-1
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| Related CAS # |
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| PubChem CID |
16760588
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| Appearance |
Pale purple to purple solid powder
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
418.7±40.0 °C at 760 mmHg
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| Melting Point |
104.4-105.0℃
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| Flash Point |
245.0±30.9 °C
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| Vapour Pressure |
0.0±1.0 mmHg at 25°C
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| Index of Refraction |
1.630
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| LogP |
3.66
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
18
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| Complexity |
223
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| Defined Atom Stereocenter Count |
0
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| Synonyms |
JSH-23 HCL
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.40 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 25.0 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: ≥ 2.5 mg/mL (10.40 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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 0.5% hydroxyethyl cellulose: 30 mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.6126 mL | 18.0629 mL | 36.1259 mL | |
| 5 mM | 0.7225 mL | 3.6126 mL | 7.2252 mL | |
| 10 mM | 0.3613 mL | 1.8063 mL | 3.6126 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.
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