Size | Price | |
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100mg | ||
250mg | ||
500mg | ||
Other Sizes |
Targets |
caspase-3 23.4 nM (EC50) Caspase 3 23.4 nM (EC50)
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ln Vitro |
M109S (0.1-10000 nM, 24-48 h) prevents apoptosis mediated by Bak and Bax [1]. Staurosporine (HY-15141 STS)-induced apoptosis in MEF cells is inhibited by M109S (0-10 μM, 4 h). In Neuro2a cells, Etoposide (HY-13629)-induced apoptosis is inhibited by M109S (0-10μM, 24 h) [1]. M109S (500 nM, 24 h) prevents the apoptosis that Obatoclax (HY-10969A) causes in ARPE19 cells [1]. Bax's conformational shift (N-terminal exposure) and mitochondrial translocation are inhibited by M109S (500 nM, 48 h) [1]. M109S (1.0 μM, 4 h) decreases reactive oxygen species and mitochondrial oxygen consumption, but M109S (0.1–1 nM, 4 h) boosts glycolysis[1].
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ln Vivo |
M109S (10 mg/kg, gavaged three times in a 48-hour period) guards against intense light-induced photoreceptor loss in the retina [1]. Orally administered bioactive cell death agent M109S can be injected intraperitoneally at a dose of 1 mg/kg, intravenous at a dose of 5 mg/kg, orally at a dose of 10 mg/kg. It has the ability to cross the blood-brain/retina barrier. inhibitors [1].
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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: MEF Tested Concentrations: 0 nM, 1.6 nM, 8 nM, 40 nM, 200 nM, 10000 nM 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, 10000 nM 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. Western Blot Analysis[1] Cell Types: iBax cells Tested Concentrations: 500 nM Incubation Duration: 48 h Experimental Results: Dramatically suppressed the amount of immunoprecipitated Bax w |
Animal Protocol |
Animal/Disease Models: Abca4-/-Rdh8-/- mice
Doses: 10 mg/kg Route of Administration: po (oral gavage) Experimental Results: Comparing to mice with 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) (po, 10 mg/kg) Route of Administration: intraperitoneal (ip)injection, intravenous (iv)injection, or po (oral gavage). Experimental Results: demonstrated plasma concentration reached 1.0 mg/mL (2.6 mM) within 30 min from po in mice , and it remained at 596± 134 ng/mL (1.6±0.36 mM) after 24 h, the same as in rat. Plasmic M109S was 565.3±188.3 nM in rats, and 171.0±52.0 nM in retina, 222.7±74.7 nM in brain, respectively. |
References |
[1]. Mieko Matsuyama, et al. Development of novel cytoprotective small compounds inhibiting mitochondria-dependent cell death. Science 26, 107916, October 20, 2023
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Molecular Formula |
C21H21N5O2
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Molecular Weight |
375.42
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CAS # |
2578300-07-7
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Appearance |
Typically exists as solids (or liquids in special cases) 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.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.6637 mL | 13.3184 mL | 26.6368 mL | |
5 mM | 0.5327 mL | 2.6637 mL | 5.3274 mL | |
10 mM | 0.2664 mL | 1.3318 mL | 2.6637 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.