| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
ROCK2-IN-14 (compound 10d) (10 nM-1 μM; 24 h) significantly inhibited the protein expression levels of S100A9, p-MYPT1 and p-NM2 in HaCaT cells [1]. ROCK2-IN-14 (10 nM-1 μM; 48 h) reduced the mRNA expression levels of IL-6 and TSLP in HaCaT cells in a concentration-dependent manner [1]. Immunofluorescence analysis showed that ROCK2-IN-14 (10 nM-1 μM; 24 h) significantly improved the abnormal polymerization of the cytoskeleton F-actin in HaCaT cells [1]. ROCK2-IN-14 (1 nM-1 μM; 72 h) had no significant effect on the viability of HaCaT cells, and the cell survival rate in each group was higher than 90% [1]. ROCK2-IN-14 (1 μM; 24 h) significantly reduced the migration ability of HaCaT cells and reduced the wound healing rate of scratches by approximately 45% compared with the control group [1].
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| ln Vivo |
ROCK2-IN-14 (compound 10d) (dose: 10 mg/kg, 30 mg/kg, 100 mg/kg; route of administration: gavage; frequency of administration: once daily; duration of administration: 14 consecutive days) significantly reduced the auricular thickening in the BALB/c atopic dermatitis (AD) mouse model and downregulated the levels of serum IgE, TNF-α, IL-6 and TSLP [1]. ROCK2-IN-14 (compound 10d) (dose: 500 mg/kg; route of administration: gavage; frequency of administration: single dose; duration of administration: once) did not show significant toxicity in the acute toxicity model of ICR mice, with a survival rate of 100% and a maximum tolerated dose exceeding 500 mg/kg [1].
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| Cell Assay |
Cell viability assay [1]
Cell Types: HaCaT Concentration: 0.001 μM, 0.01 μM, 0.1 μM, 1 μM Incubation Duration: 72 hours Experimental Results: No significant effect on HaCaT cell viability; cell survival rate was above 90% at all tested concentrations. Real-time quantitative PCR[1] Cell Types: HaCaT Tested Concentrations: 10 nM, 100 nM, 1 μM Incubation Duration: 48 hours Experimental Results: The mRNA expression levels of inflammatory factors IL-6 and TSLP were reduced in a concentration-dependent manner, with the most significant reduction at 1 μM (68% and 72%, respectively). Western Blot analysis [1] Cell Types: HaCaT Concentration tested: 48 h Incubation Duration: 24 h Experimental Results: Concentration significantly downregulated the protein expression levels of S100A9, p-MYPT1 (Thr853) and p-NM2 in HaCaT cells. |
| Animal Protocol |
Animal/Disease Models:BALB/c mice (female, 18-22 g, 6-8 weeks old) + atopic dermatitis (AD) model [1]
Doses: 10 mg/kg (0.5% CMC-Na), 30 mg/kg (0.5% CMC-Na), 100 mg/kg (0.5% CMC-Na) Route of Administration: Once daily by gavage for 14 consecutive days Experimental Experimental Results: Compared with the model group, the thickening of the ears of AD model mice was significantly reduced, with a reduction of 35% in the 10 mg/kg group, 58% in the 30 mg/kg group, and 72% in the 100 mg/kg group; at a dose of 30 mg/kg, the serum levels of IgE, TNF-α, IL-6 and TSLP decreased by 28%, 42%, 51% and 48%, respectively. Animal/Disease Models:ICR mice (male and female, 20-24 g, 7-9 weeks old) + acute toxicity model [1] Doses: 500 mg/kg Route of Administration: Single gavage administration Experimental Results: No obvious toxic symptoms (such as weight loss, abnormal behavior, organ damage) were observed in the mice during the 14-day observation period. The survival rate of the mice was 100%, indicating that the maximum tolerated dose (MTD) was greater than 500 mg/kg. |
| References |
| Molecular Formula |
C24H26N4O2S
|
|---|---|
| Molecular Weight |
434.55
|
| CAS # |
3115784-59-0
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| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
CN(C)CCCOC1=CC(CNC(C2=CC3=CC=C(C4=CNN=C4)C=C3S2)=O)=CC=C1
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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 | 2.3012 mL | 11.5062 mL | 23.0123 mL | |
| 5 mM | 0.4602 mL | 2.3012 mL | 4.6025 mL | |
| 10 mM | 0.2301 mL | 1.1506 mL | 2.3012 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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