| ln Vitro |
RIPK1-IN-33 (compound 23a) (30-60 min) exhibited significant free radical scavenging ability (IC50 = 123.3 μM) and antioxidant activity (IC50 = 9.72 μM) [1]. RIPK1-IN-33 (0.0076-50 μM, 17 h) dose-dependently reduced the mRNA expression level of PTGS2 in HT-1080 cells (IC50 = 0.156 μM) [1].
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| ln Vivo |
RIPK1-IN-33 (compound 23a) (33 mg/kg (68.8 μmol/kg), intravenously, twice, 24 hours) has a protective effect in a rat model of cerebral ischemia-reperfusion injury[1]. RIPK1-IN-33 (compound 23a) (100-200 mg/kg, intravenously, once or once daily for 7 days) did not result in death or significant adverse events in a rat model of cerebral ischemia-reperfusion injury[1].
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| Cell Assay |
Real-time quantitative PCR[1]
Cell Types: HT-1080 cells Tested Concentrations: 0.0076, 0.0227, 0.0686, 0.206, 0.617, 1.9, 5.6, 16.7, 50 μM Incubation Duration: 17 hours Experimental Results: Reduced the mRNA expression level of PTGS2 in HT-1080 cells (IC50 = 0.156 μM). Compared with edaravone (IC50 = 4.92 μM), it showed significantly stronger anti-ferroptosis activity. |
| Animal Protocol |
Animal/Disease Models:Adult male Sprague-Dawley rats (200-230 g) were subjected to transient middle cerebral artery occlusion (tMCAO) [1]
Dose: 33 mg/kg (68.8 μmol/kg) Route of Administration:Intravenous injection twice, with the second administration 6 hours apart Experimental Results:Compared with the vector control group, the infarct volume of tMCAO rats was reduced. Neurological function of tMCAO rats was improved. MDA levels were downregulated. Protein expression of necroptosis-associated caspase-3 in the ischemic penumbra was reduced. Protein expression of cyclooxygenase-2 (COX-2, encoded by PTGS2) was downregulated. Glutathione peroxidase 4 (GPX4) was upregulated in the ferroptosis pathway. Animal/Disease Models:Adult male Sprague-Dawley rats (200-230 g) were subjected to transient middle cerebral artery occlusion (tMCAO) [1] Doses: 100, 200 mg/kg Route of Administration: Single intravenous injection or once daily intravenous injection for 7 days Experimental Results: No abnormalities were found in body weight, food consumption, organ-to-body weight ratio, blood biochemical parameters or autopsy results. |
| References |
| Appearance |
Typically exists as solids at room temperature
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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.) |
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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