| Size | Price | Stock | Qty |
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| Targets |
BML-111 targets FPR2 (formyl peptide receptor 2), also known as the lipoxin A4 receptor. FPR2 is a G protein-coupled receptor that mediates the anti-inflammatory and pro-resolving effects of lipoxin A4. BML-111 is a lipoxin A4 analog and a potent FPR2 agonist, with an IC50 of 70 nM. By activating FPR2, BML-111 mimics the effects of lipoxin A4, including the inhibition of neutrophil recruitment, the promotion of macrophage phagocytosis of apoptotic cells, and the suppression of pro-inflammatory cytokine production. BML-111 also represses the activity of angiotensin-converting enzyme (ACE) and increases the activity of ACE2. These actions contribute to its anti-angiogenic, antitumorigenic, and anti-inflammatory properties.
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| ln Vitro |
BML-111 lowers the levels of hypoxia-inducible factor-1α and prevents the synthesis of vascular endothelial growth factor in H22 cells [1]. With an IC50 of 5 nM, BML-111 blocks leukotriene B4-induced cell migration[3].
In vitro studies have characterized BML-111 as a potent FPR2 agonist with an IC50 of 70 nM. It suppresses tumor-related angiogenesis in vitro and reduces tumor growth. BML-111 has anti-angiogenic effects, likely through the inhibition of endothelial cell proliferation and migration. It also exhibits anti-inflammatory properties by modulating immune cell function and reducing the production of pro-inflammatory cytokines. BML-111's ability to repress ACE activity and increase ACE2 activity contributes to its protective effects in models of acute lung injury. These in vitro findings establish BML-111 as a potent agonist of FPR2 with diverse biological activities. |
| ln Vivo |
Male imprinted control mice treated with BML-111 (1 mg/kg; i.p.; 15 days) showed reduced tumor-associated angiogenesis and tumor growth in vivo. Additionally, BML-111 can promote in situ cell death while preventing tumor tissue macrophage invasion [1]. LPS-induced acute lung injury and LPS/D-GalN-induced acute liver injury are prevented by BML-111. While ACE activity is inhibited by BML-111, ACE2 activity is increased. ACE, AngII, and AngII type 1 receptor (AT1R) expression levels are all decreased by BML-111, although ACE2, angiotensin-(1-7) (Ang-1-7), and Mas are all increased [2].
In vivo studies have demonstrated that BML-111 has significant therapeutic effects in animal models. In hepatoma H22 cell-bearing mice, BML-111 suppresses tumor-related angiogenesis and reduces tumor growth. In rats, BML-111 protects against hemorrhagic shock-induced acute lung injury. These effects are attributed to its anti-inflammatory and pro-resolving actions, which are mediated through FPR2 activation. BML-111's ability to modulate ACE and ACE2 activity may also contribute to its protective effects in acute lung injury. These in vivo studies confirm that BML-111 is a potent agonist of FPR2 with therapeutic potential in cancer and inflammatory diseases. |
| Enzyme Assay |
The in vitro assays for BML-111 measure its binding to FPR2 and its ability to activate FPR2-mediated signaling. Receptor binding assays are performed using membranes from cells expressing FPR2 and a radiolabeled ligand. Functional assays measure the activation of downstream signaling pathways, such as calcium mobilization or the inhibition of cAMP accumulation. BML-111 has an IC50 of 70 nM for FPR2 activation. The compound's effects on ACE and ACE2 activity can also be measured in vitro using enzyme activity assays. These assays confirm that BML-111 is a potent agonist of FPR2 with additional effects on the renin-angiotensin system.
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| Cell Assay |
In vitro cell-based assays for BML-111 are used to study its effects on immune cell function, angiogenesis, and tumor cell biology. For anti-angiogenic assays, endothelial cells are treated with BML-111, and their proliferation, migration, and tube formation are assessed. For anti-inflammatory assays, immune cells (e.g., macrophages, neutrophils) are treated with BML-111, and the production of pro-inflammatory cytokines is measured. For anti-tumor assays, cancer cells are treated with BML-111, and cell proliferation and apoptosis are assessed. These cell-based assays confirm that BML-111 has anti-angiogenic, anti-inflammatory, and anti-tumor properties.
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| Animal Protocol |
Animal/Disease Models: Male imprinted control area mice (5-6 weeks old, 18-22 g) were injected with H22 cells [1]
Doses: 1 mg/kg Route of Administration: intraperitoneal (ip) injection; intraperitoneal (ip) injection. H22 cells were injected 5 minutes before and 4 hrs (hrs (hours)) after inoculation, then every 12 hrs (hrs (hours)) for 2 days, then one time/day for the next 3 days, and every other day for the last 10 days. Experimental Results: Inhibition of tumors in vivo Related angiogenesis and tumor growth. In vivo animal experiments for BML-111 are conducted in models of cancer and inflammation. In the hepatoma H22 mouse model, mice are injected with H22 cells to establish tumors, and then treated with BML-111. Tumor growth and angiogenesis are monitored. In the hemorrhagic shock-induced acute lung injury model, rats are subjected to hemorrhagic shock and then treated with BML-111. Lung injury is assessed by measuring lung edema, inflammation, and histopathological changes. These studies provide evidence for the in vivo efficacy of BML-111 in cancer and inflammatory diseases. |
| ADME/Pharmacokinetics |
BML-111 has a molecular weight of 192.21 g/mol and a molecular formula of C8H16O5. It is a solid compound with a purity of >99%. BML-111 is soluble in water and DMSO at 100 mM. For storage, it is recommended to keep the compound at -20°C. The compound is stable under recommended storage conditions. Pharmacokinetic properties such as absorption, distribution, metabolism, and excretion (ADME) have not been extensively characterized. BML-111 is a research compound and is not intended for human or veterinary use.
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| Toxicity/Toxicokinetics |
Detailed toxicity data for BML-111 is not provided in standard product descriptions. As a research compound, its toxicity profile has not been extensively characterized. In vivo studies have used BML-111 in animal models without reported overt toxicity. However, comprehensive toxicological studies, including acute and chronic toxicity studies, have not been reported. As with all research chemicals, standard laboratory safety precautions should be followed when handling BML-111. Its use is limited to research applications and it is not intended for human or veterinary use.
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| References |
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| Additional Infomation |
BML-111 is a research compound and is not approved for any clinical or therapeutic use. It is a lipoxin A4 analog and a potent FPR2 (lipoxin A4 receptor) agonist with an IC50 of 70 nM. BML-111 suppresses tumor-related angiogenesis and reduces tumor growth in hepatoma H22 cell-bearing mice. It also protects against hemorrhagic shock-induced acute lung injury in rats. BML-111 represses ACE activity and increases ACE2 activity. It has anti-angiogenic, antitumorigenic, and anti-inflammatory properties. BML-111 is used to study lipoxin A4 receptor signaling and its role in inflammation, cancer, and other diseases. Its mechanism of action involves activating FPR2 and modulating the renin-angiotensin system.
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| Molecular Formula |
C8H16O5
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| Molecular Weight |
192.211
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| Exact Mass |
192.099
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| CAS # |
78606-80-1
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| PubChem CID |
10899465
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| Appearance |
Colorless to light yellow solid-liquid Mixture
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
360.8±42.0 °C at 760 mmHg
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| Flash Point |
143.5±21.4 °C
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| Vapour Pressure |
0.0±1.8 mmHg at 25°C
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| Index of Refraction |
1.489
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| LogP |
-1.72
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
13
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| Complexity |
148
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| Defined Atom Stereocenter Count |
2
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| SMILES |
OC(C(O)CO)CCCC(OC)=O
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| InChi Key |
RNMFWAFZUNVQOR-NKWVEPMBSA-N
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| InChi Code |
InChI=1S/C8H16O5/c1-13-8(12)4-2-3-6(10)7(11)5-9/h6-7,9-11H,2-5H2,1H3/t6-,7+/m0/s1
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| Chemical Name |
methyl (5S,6R)-5,6,7-trihydroxyheptanoate
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| Synonyms |
BML-111 BML111 BML 111
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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) |
DMSO : ~100 mg/mL (~520.26 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (13.01 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (13.01 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (13.01 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 5.2026 mL | 26.0132 mL | 52.0264 mL | |
| 5 mM | 1.0405 mL | 5.2026 mL | 10.4053 mL | |
| 10 mM | 0.5203 mL | 2.6013 mL | 5.2026 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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