| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| Targets |
IRAK1
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|---|---|
| ln Vitro |
When Jh-X-119-01 (10 μM) is added to LPS-treated macrophages in vitro, it reduces the phosphorylation of NF-κB and the levels of mRNA for IL-6 and TNFα. IRAK1 phosphorylation is specifically inhibited by Jh-X-119-01[1].
|
| ln Vivo |
LPS-challenged mice who receive Jh-X-119-01 have increased survival and decreased immunopathies. Mice's survival is increased by Jh-X-119-01 at a dose of 5 mg/kg body weight. Raising the dosage to 10 mg/kg considerably improves survival[1].
|
| Cell Assay |
Western Blot Analysis[1]
Cell Types: RAW 264.7 cells and THP-1 cells Tested Concentrations: 10 μM Incubation Duration: 15 minutes Experimental Results: diminished LPS (100 ng/mL)-induced phosphorylation of IκBα and NF-κB-P65. |
| Animal Protocol |
Animal/Disease Models: C57BL/6 (20-22 g, male) mice[1]
Doses: 5 mg/kg and 10 mg/kg Route of Administration: intraperitoneally (ip) injected; 5 days Experimental Results: Protected mice from LPS (20 mg/kg)-induced sepsis. Survival at day 5 was 13.3% in control group where septic mice were treated by vehicle, while the values were 37.5% and 56.3% for 5 mg/kg and 10 mg/kg. |
| References |
| Molecular Formula |
C25H21CLN6O3
|
|---|---|
| Molecular Weight |
488.9256
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| Exact Mass |
488.136
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| CAS # |
2591344-30-6
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| Related CAS # |
JH-X-119-01;2227368-54-7
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| PubChem CID |
131704491
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| Appearance |
Light yellow to yellow solid powder
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| Hydrogen Bond Donor Count |
5
|
| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
35
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| Complexity |
738
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Cl[H].O=C(C1C([H])=C([H])C([H])=C(C=1[H])N([H])C(C([H])=C([H])[H])=O)N([H])C1C([H])=C([H])C(=C([H])C=1[H])N([H])C(C1=C([H])C([H])=C([H])C(C2=C([H])C([H])=NN2[H])=N1)=O
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| InChi Key |
BUFHXMGSECIZAM-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H20N6O3.ClH/c1-2-23(32)27-19-6-3-5-16(15-19)24(33)28-17-9-11-18(12-10-17)29-25(34)22-8-4-7-20(30-22)21-13-14-26-31-21;/h2-15H,1H2,(H,26,31)(H,27,32)(H,28,33)(H,29,34);1H
|
| Chemical Name |
N-[4-[[3-(prop-2-enoylamino)benzoyl]amino]phenyl]-6-(1H-pyrazol-5-yl)pyridine-2-carboxamide;hydrochloride
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
DMSO: 50 mg/mL (102.26 mM)
H2O: < 0.1 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (5.11 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 sonication.
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 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 2: ≥ 2.5 mg/mL (5.11 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0453 mL | 10.2264 mL | 20.4528 mL | |
| 5 mM | 0.4091 mL | 2.0453 mL | 4.0906 mL | |
| 10 mM | 0.2045 mL | 1.0226 mL | 2.0453 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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