| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| Targets |
RIPK1
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|---|---|
| ln Vitro |
Necrostatin-34 (Nec-34) in FADD def-Jurkat cells and L939 cells had IC50 values for TNFα of 667 nM and 134 nM, respectively[1]. The phosphorylation of RIPK1's Ser166 (p-S166), a biomarker for RIPK1 activation, indicates that necrostatin-34 (Nec-34, 10 μM) suppresses the dimerization-induced RIPK1 activation[1]. Necrostatin-34 (Nec-34) has the potential to prevent TNFα-induced complex II formation by impeding RIPK1 kinase activation[1].
|
| Cell Assay |
Western Blot Analysis[1]
Cell Types: RIPK1 knockout L929 cells transfected with an expressing vector encoding an inducible and dimerizable RIPK1 fused with FKBP at the C-terminus. Tested Concentrations: 10 μM. Incubation Duration: 30 min (and then 100 ng/mL TNFα was added for indicated periods of time). Experimental Results: Downregulated p-S166 levels. |
| References |
| Molecular Formula |
C18H16N4O2S2
|
|---|---|
| Molecular Weight |
384.48
|
| Exact Mass |
384.071
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| CAS # |
375835-43-1
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| PubChem CID |
3841655
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Index of Refraction |
1.675
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| LogP |
0.968
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
26
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| Complexity |
634
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
LOQIRQHGJVGIEL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H16N4O2S2/c1-11-2-4-12(5-3-11)13-8-15(23)21-17(14(13)9-19)26-10-16(24)22-18-20-6-7-25-18/h2-7,13H,8,10H2,1H3,(H,21,23)(H,20,22,24)
|
| Chemical Name |
2-[[5-cyano-4-(4-methylphenyl)-2-oxo-3,4-dihydro-1H-pyridin-6-yl]sulfanyl]-N-(1,3-thiazol-2-yl)acetamide
|
| 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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : 125 mg/mL (325.11 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.41 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 (5.41 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 | 2.6009 mL | 13.0046 mL | 26.0092 mL | |
| 5 mM | 0.5202 mL | 2.6009 mL | 5.2018 mL | |
| 10 mM | 0.2601 mL | 1.3005 mL | 2.6009 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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