Physicochemical Properties
| Molecular Formula | C28H29NO6 |
| Molecular Weight | 475.53 |
| Appearance | Typically exists as solid at room temperature |
| HS Tariff Code | 2934.99.9001 |
| 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) |
Biological Activity
| Targets | Caspase 3 23.4 nM (EC50) |
| ln Vitro | M109S (0.1–10,000 nM, 24–48 h) can prevent Bax and Bak-induced apoptosis [1]. M109S (0-10μM, 4 h) prevents MEF cell apoptosis caused by staurosporine[1]. Neuro2a cell apoptosis induced by etoposide (HY-13629 Etoposide) is inhibited by M109S (0-10μM, 24 h) [1]. ARPE19 cells' apoptosis caused by Obatoclax (HY-10969A) is inhibited by M109S (500 nM, 24 h) [1]. N-terminal exposure to conformational changes is inhibited by M109S (500 nM, 48 h) [1]. Bax's translocation into the mitochondria is inhibited by M109S (500 nM, 48 h) [1]. M109S (1.0 μM, 4h) decreases reactive oxygen species and mitochondrial oxygen consumption, whereas M109S (0.1-1 mM) boosts glycolysis [1]. |
| ln Vivo | M109S (10 mg/kg gavage, three injections within 48 hours) can prevent intense light-induced photoreceptor loss in the retina [1]. An oral bioactive cell death inhibitor that crosses the blood-brain/retina barrier is M109S (ip, 1 mg/kg, intravenous, 5 mg/kg, or oral gavage, 10 mg/kg) [1]. |
| Cell Assay |
Apoptosis Analysis[1] Cell Types: MEF(Wt, Bax only, Bak only) Tested Concentrations: 0.1 nM, 1 nM, 10 nM, 100 nM, 10000 nM Incubation Duration: 24 h((WT and Bax-only), 48 h (Bak-only) Experimental Results: demonstrated a dose-dependent suppression of caspase activation in all three types of MEFs. Apoptosis Analysis[1] Cell Types: demonstrated a dose-dependent suppression of caspase activation in all three types of MEFs. Tested Concentrations: 0 nM, 1.6 nM, 8 nM, 40 nM, 200 nM, 10 μM Incubation Duration: 4 h Experimental Results: Suppressed STS-induced caspase activation in a dose-dependent manner. Apoptosis Analysis[1] Cell Types: Neuro2a Tested Concentrations: 0 nM, 40 nM, 200 nM, 10 μM Incubation Duration: 24 h Experimental Results: Suppressed Etoposide -induced caspase activation in a dose-dependent manner. Western Blot Analysis[1] Cell Types: ARPE19 Tested Concentrations: 500 nM Incubation Duration: 24 h Experimental Results: Dramatically inhibited Obatoclax-induced apoptosis in ARPE19 cells comparing to control. Immunofluorescence[1] Cell Types: iBax cells Tested Concentrations: 500 nM Incubation Duration: 48 |
| Animal Protocol |
Animal/Disease Models: Abca4-/-Rdh8-/- mice Doses: 10mg/kg Route of Administration: po (oral gavage) Experimental Results: Comparing to micewith M109S, the number of AF spots was similar to that detected in the dark-adapted mice Animal/Disease Models: Mice and Rat Doses: intraperitoneal (ip)injection (IP, 1 mg/kg), intravenous (iv) injection (IV, 5 mg/kg), or po (oral gavage) (OP, 10 mg/kg). Route of Administration: intraperitoneal (ip)injection (IP, 1 mg/kg ), intravenous (iv) injection (IV, 5 mg/kg), or po (oral gavage) (OP, 10 mg/kg). Experimental Results: In mice, M109S reached 1.0 mg/mL (2.6 mM) plasma concentration within 30 min from administration, and it remained at 596± 134 ng/mL (1.6± 0.36 mM) 24 h after the po (oral gavage) administration, the same as in rat. At 24 h after the po (oral gavage) administration, the level of M109S in the plasma was 565.3± 188.3 nM in rats.The level of M109S in the rat retina and brain reached 171.0± 52.0 nM and 222.7± 74.7 nM, respectively, 24 h after its oral administration. |
| References | [1]. Singh CP, et al. Semisynthesis of Novel Dispiro-pyrrolizidino/thiopyrrolizidino-oxindolo/indanedione Natural Product Hybrids of Parthenin Followed by Their Cytotoxicity Evaluation. ACS Omega. 2023 Sep 14;8(38):35283-35294. |
Solubility Data
| 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 (e.g. IP/IV/IM/SC) Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline) *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). 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)] *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. Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline) Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline) Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline) Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil) Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL 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). Oral Formulation 3: Dissolved in PEG400 Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose Oral Formulation 6: Mixing with food powders Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1029 mL | 10.5146 mL | 21.0292 mL | |
| 5 mM | 0.4206 mL | 2.1029 mL | 4.2058 mL | |
| 10 mM | 0.2103 mL | 1.0515 mL | 2.1029 mL |