| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg | |||
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| Other Sizes |
| Targets |
BI-0115 targets LOX-1, a scavenger receptor that mediates the uptake of oxidized low-density lipoprotein (oxLDL) into cells. LOX-1 plays a critical role in the pathogenesis of atherosclerosis by promoting foam cell formation, endothelial dysfunction, and inflammation. By inhibiting LOX-1, BI-0115 prevents oxLDL uptake and may reduce atherosclerotic plaque formation.
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|---|---|
| ln Vitro |
BI-0115 effectively decreases the uptake of oxLDL inside the cellular environment. The obtained Kd values in SPR (4.3 µM) and ITC (6.99 µM) are in good agreement with the cellular assay's IC50 values (5.4 µM)[1].
In vitro, BI-0115 inhibits oxidized LDL uptake in CHO cells expressing human Ox-LDL receptor 1 with an IC50 of 5.4 µM. Its binding triggers receptor inhibition by forming dimers of the homodimeric ligand binding domain. Detailed in vitro activity data are not provided. |
| ln Vivo |
In vivo activity data for BI-0115 are not detailed in the available references. As a LOX-1 inhibitor, it would be expected to have effects in models of atherosclerosis, where it could reduce foam cell formation, inflammation, and plaque progression. Further studies would be needed to confirm in vivo efficacy.
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| Enzyme Assay |
LOX-1 binding inhibition is assessed using cell-free binding assays with recombinant LOX-1 protein and labeled oxidized LDL. Competitive displacement of labeled oxLDL is measured to determine binding affinity and inhibitory potency. Surface plasmon resonance or ELISA-based assays can also be used.
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| Cell Assay |
Cellular assays for BI-0115 use CHO cells expressing human Ox-LDL receptor 1. Cells are treated with BI-0115 and exposed to labeled oxLDL. Cellular uptake of oxLDL is measured, and IC50 values are calculated from dose-response curves.
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| Animal Protocol |
In vivo animal studies for BI-0115 would be conducted in mouse or rabbit models of atherosclerosis. The compound would be administered orally or intraperitoneally, and endpoints would include aortic plaque area, lipid deposition, and inflammatory markers. Detailed protocols are not provided in the available references.
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| ADME/Pharmacokinetics |
BI-0115 has the molecular formula C₁₅H₁₄ClN₃O with a molecular weight of 287.74. It is a selective small molecule inhibitor of LOX-1. Detailed pharmacokinetic parameters such as half-life, bioavailability, and tissue distribution are not disclosed in the available references.
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| Toxicity/Toxicokinetics |
No specific toxicity data are detailed in the available references. As a LOX-1 inhibitor, potential toxicities would depend on the role of LOX-1 in normal physiology. The compound's selectivity would be important for minimizing off-target effects. Safety studies would be required for clinical development.
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| References | |
| Additional Infomation |
BI-0115 is a research compound not yet approved for clinical use. It is a selective small molecule inhibitor of LOX-1, a key receptor involved in the uptake of oxidized LDL and the pathogenesis of atherosclerosis. It serves as a valuable pharmacological tool for studying LOX-1 function and exploring therapeutic strategies for atherosclerosis and other cardiovascular diseases.
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| Molecular Formula |
C15H14CLN3O
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|---|---|
| Molecular Weight |
287.747
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| Exact Mass |
287.082
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| CAS # |
4929-23-1
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| Related CAS # |
4929-23-1;
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| PubChem CID |
146676953
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
489.2±45.0 °C at 760 mmHg
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| Flash Point |
249.7±28.7 °C
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| Vapour Pressure |
0.0±1.2 mmHg at 25°C
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| Index of Refraction |
1.602
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| LogP |
3.08
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
20
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| Complexity |
365
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCCN1C2=C(NC3=C(C1=O)C=CC(=C3)Cl)N=CC=C2
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| InChi Key |
QTCZUCSALXBZQR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H14ClN3O/c1-2-8-19-13-4-3-7-17-14(13)18-12-9-10(16)5-6-11(12)15(19)20/h3-7,9H,2,8H2,1H3,(H,17,18)
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| Chemical Name |
9-chloro-5-propyl-11H-pyrido[2,3-b][1,4]benzodiazepin-6-one
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| Synonyms |
BI-0115BI 0115BI0115
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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 (~347.54 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.69 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.4752 mL | 17.3762 mL | 34.7524 mL | |
| 5 mM | 0.6950 mL | 3.4752 mL | 6.9505 mL | |
| 10 mM | 0.3475 mL | 1.7376 mL | 3.4752 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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