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| Targets |
RIPK1-IN-9 targets receptor-interacting serine/threonine-protein kinase 1 (RIPK1), a key regulator of cell death and inflammation. It is a potent and selective inhibitor of RIPK1. The compound inhibits U937 cells with an IC₅₀ of 2 nM and L929 cells with an IC₅₀ of 1.3 nM.
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| ln Vitro |
In vitro, RIPK1-IN-9 is a potent and selective inhibitor of RIPK1. It demonstrates potent inhibitory activity in U937 cells with an IC₅₀ of 2 nM, and in L929 cells with an IC₅₀ of 1.3 nM. The compound is a dihydronaphthyridone compound with high selectivity for RIPK1.
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| ln Vivo |
In vivo data for RIPK1-IN-9 are limited in the available literature. The compound is primarily used as a research tool to study the role of RIPK1 in various biological processes, including necroptosis and inflammation. Further in vivo studies are needed to evaluate its therapeutic potential and pharmacokinetic properties.
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| Enzyme Assay |
RIPK1-IN-9's kinase inhibition activity can be characterized using biochemical kinase assays with purified RIPK1 enzyme. The compound inhibits RIPK1 activity with IC₅₀ values of 2 nM in U937 cells and 1.3 nM in L929 cells. Binding assays typically involve measuring the inhibition of RIPK1-mediated phosphorylation of substrates using standard kinase assays.
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| Cell Assay |
In vitro cell experiments with RIPK1-IN-9 use U937 and L929 cell lines to assess its inhibitory activity. Cells are treated with the compound at various concentrations, and cell viability or RIPK1 activity is assessed. The compound's effects on necroptosis and inflammatory signaling pathways can be evaluated.
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| Animal Protocol |
In vivo animal studies with RIPK1-IN-9 have not been extensively reported in the available literature. The compound is primarily used for in vitro research. Further studies are needed to evaluate its in vivo efficacy, pharmacokinetics, and safety in animal models.
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| ADME/Pharmacokinetics |
Pharmacokinetic data specific to RIPK1-IN-9 are limited in the available literature. As a small molecule with a molecular weight of 472.51, the compound is expected to have reasonable bioavailability. The compound is stored as powder at -20°C for 3 years or in solvent at -80°C for 1 year.
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| Toxicity/Toxicokinetics |
RIPK1-IN-9 is considered safe for research use at typical concentrations. As a research compound, it is intended for laboratory use only and not for human consumption. The compound should be handled under standard laboratory safety practices with appropriate precautions.
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| References | |
| Additional Infomation |
RIPK1-IN-9 (example 45) is a potent and selective RIPK1 inhibitor. It inhibits U937 cells (IC₅₀=2 nM) and L929 cells (IC₅₀=1.3 nM). The compound has a CAS number of 2682889-57-0 and is stored as a powder at -20°C for 3 years.
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| Molecular Formula |
C26H25FN6O2
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|---|---|
| Molecular Weight |
472.514108419418
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| Exact Mass |
472.202
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| CAS # |
2682889-57-0
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| PubChem CID |
156825492
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
3.3
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
35
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| Complexity |
753
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1CCC(C1)OC2=C(C=C(C=C2)F)CN3CCC4=C(C3=O)C=C(C=N4)C5=CC6=NC(=NN6C=C5)N
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| InChi Key |
NFZIVWWKQSSLRB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C26H25FN6O2/c27-19-5-6-23(35-20-3-1-2-4-20)18(11-19)15-32-9-8-22-21(25(32)34)12-17(14-29-22)16-7-10-33-24(13-16)30-26(28)31-33/h5-7,10-14,20H,1-4,8-9,15H2,(H2,28,31)
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| Chemical Name |
3-(2-amino-[1,2,4]triazolo[1,5-a]pyridin-7-yl)-6-[(2-cyclopentyloxy-5-fluorophenyl)methyl]-7,8-dihydro-1,6-naphthyridin-5-one
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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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1164 mL | 10.5818 mL | 21.1636 mL | |
| 5 mM | 0.4233 mL | 2.1164 mL | 4.2327 mL | |
| 10 mM | 0.2116 mL | 1.0582 mL | 2.1164 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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