| Size | Price | Stock | Qty |
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| 5mg |
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| 50mg |
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| Targets |
SIRT1[1].
SIRT1 (Sirtuin 1). BML-278 is a SIRT1 activator with an EC150 (or EC50) of 1 μM. It displays selectivity over SIRT2 (EC50 = 25 μM) and SIRT3 (EC50 = 50 μM). SIRT1 is a NAD+-dependent deacetylase involved in aging, metabolism, and cell survival. Activation of SIRT1 has implications for longevity and metabolic health. |
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| ln Vitro |
BML-278 activates SIRT1 deacetylase activity with an EC150 of 1 μM. It increases H3K9 methylation and inhibits H3K9 acetylation in paternal and maternal pronuclei. The compound arrests primary human mesenchymal cells in G1/S phase and reduces senescence. BML-278 reduces tubulin acetylation in U937 cells. These activities demonstrate its cellular effects as a SIRT1 activator.
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| ln Vivo |
BML-278 improves early embryonic development in model systems. It arrests the cell cycle of primary human mesenchymal cells in G1/S phase and reduces senescence. The compound increases H3K9 methylation and inhibits H3K9 acetylation in paternal and maternal pronuclei. These in vivo-like effects support its utility in developmental and aging research.
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| Enzyme Assay |
In vitro enzyme assays for SIRT1 activation are performed using recombinant SIRT1 enzyme, a fluorogenic acetylated peptide substrate, and NAD+. BML-278 is incubated at varying concentrations (typically 0.1–100 μM) with the enzyme and substrate. Deacetylation is detected by fluorescence. EC50 values are calculated from dose-response curves. Selectivity against SIRT2 and SIRT3 is determined using the same assay format with the respective enzymes.
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| Cell Assay |
Cells (e.g., primary human mesenchymal cells, U937 cells, or embryonic cells) are cultured and treated with BML-278 at concentrations ranging from 0.1–10 μM for 24–72 hours. SIRT1 activation is assessed by measuring acetylation of SIRT1 substrates (e.g., H3K9, tubulin) by Western blot. Cell cycle analysis is performed by flow cytometry. Senescence is evaluated by beta-galactosidase staining. Embryonic development is assessed by morphological criteria.
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| Animal Protocol |
In vivo animal studies for BML-278 have been conducted in embryonic development models. For cell cycle and senescence studies, primary human mesenchymal cells are used as an ex vivo model. Detailed in vivo protocols in animal models have not been extensively reported. Standard protocols for SIRT1 activator studies could be adapted for future in vivo experiments.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for BML-278 are limited. The compound is cell-permeable, indicating favorable membrane penetration. It has a molecular weight of 391.46 and formula C24H25NO4. In vivo PK parameters such as half-life, bioavailability, and tissue distribution have not been extensively characterized. For in vivo use, formulation would need to be developed.
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| Toxicity/Toxicokinetics |
Toxicology data for BML-278 have not been published. The compound is for research use only and not approved for human therapeutic applications. No systematic toxicological evaluation has been performed. Standard safety precautions for handling chemical activators should be observed.
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| References |
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| Additional Infomation |
4-Phenylacetyl-1-(benzyl)-4H-pyridine-3,5-dicarboxylic acid diethyl ester is a dihydropyridine.
BML-278 (CAS: 120533-76-8, molecular formula C24H25NO4, molecular weight 391.46) is a SIRT1 activator with selectivity over SIRT2 and SIRT3. It is not in clinical trials and has no regulatory approval. The compound is supplied as a research-grade activator for laboratory use only. References include studies on embryonic development and cellular senescence. |
| Molecular Formula |
C24H25NO4
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|---|---|
| Molecular Weight |
391.46
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| Exact Mass |
391.178
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| Elemental Analysis |
C, 73.64; H, 6.44; N, 3.58; O, 16.35
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| CAS # |
120533-76-8
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| PubChem CID |
10620479
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
4.117
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
29
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| Complexity |
591
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCOC(=O)C1=CN(C=C(C1C2=CC=CC=C2)C(=O)OCC)CC3=CC=CC=C3
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| InChi Key |
JOHFECBOWRGWJZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H25NO4/c1-3-28-23(26)20-16-25(15-18-11-7-5-8-12-18)17-21(24(27)29-4-2)22(20)19-13-9-6-10-14-19/h5-14,16-17,22H,3-4,15H2,1-2H3
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| Chemical Name |
diethyl 1-benzyl-4-phenyl-1,4-dihydropyridine-3,5-dicarboxylate
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| Synonyms |
BML-278; BML 278; BML278; diethyl 1-benzyl-4-phenyl-1,4-dihydropyridine-3,5-dicarboxylate; Diethyl 1-benzyl-4-phenyl-4H-pyridine-3,5-dicarboxylate
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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 | 2.5545 mL | 12.7727 mL | 25.5454 mL | |
| 5 mM | 0.5109 mL | 2.5545 mL | 5.1091 mL | |
| 10 mM | 0.2555 mL | 1.2773 mL | 2.5545 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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