| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
DKI5 specifically targets the lectin-like oxidized low-density lipoprotein receptor-1 (LOX-1), also known as OLR1. LOX-1 is a type II transmembrane glycoprotein that functions as a scavenger receptor for oxidized low-density lipoprotein (oxLDL). LOX-1 is expressed on endothelial cells, macrophages, smooth muscle cells, and platelets, and plays a critical role in the pathogenesis of atherosclerosis by mediating the uptake of oxLDL and promoting endothelial dysfunction, inflammation, and foam cell formation. LOX-1 is also involved in the development of hypertension, diabetes, and other cardiovascular diseases. DKI5 inhibits LOX-1 with an IC50 of 22.5 μM. The compound strongly inhibits lipid peroxidation and may possess anti-inflammatory and antioxidant activities.
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| ln Vitro |
In vitro, DKI5 inhibits LOX-1 with an IC50 of 22.5 μM. The compound strongly inhibits lipid peroxidation, as demonstrated in in vitro bioassays. DKI5 may possess anti-inflammatory and antioxidant activities, making it a potential tool for studying the role of oxidative stress and inflammation in cardiovascular disease. By inhibiting LOX-1, the compound blocks the uptake of oxidized LDL, reducing foam cell formation and the progression of atherosclerosis. Specific details of the compound's in vitro activity are described in the primary literature. DKI5 is used as a research tool for studying LOX-1 biology and for validating LOX-1 as a therapeutic target.
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| ln Vivo |
In vivo activity of DKI5 has been investigated in preclinical models of atherosclerosis and inflammation. As a LOX-1 inhibitor, the compound is expected to reduce the uptake of oxidized LDL, inhibit foam cell formation, and attenuate the progression of atherosclerosis. The compound's anti-inflammatory and antioxidant activities may also contribute to its in vivo effects. Specific in vivo efficacy data is available from the primary literature describing the compound. The compound is typically administered via intraperitoneal (i.p.) injection or oral gavage in these studies.
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| Enzyme Assay |
The inhibitory activity of DKI5 against LOX-1 is assessed using binding or functional assays. For binding assays, recombinant LOX-1 or LOX-1-expressing cells are incubated with a labeled ligand (such as fluorescently labeled oxidized LDL) in the presence of varying concentrations of the test compound. The amount of ligand bound is quantified. For functional assays, the uptake of oxidized LDL by LOX-1-expressing cells is measured in the presence of the compound. IC50 values are calculated from dose-response curves. Lipid peroxidation inhibition is assessed using standard biochemical assays.
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| Cell Assay |
Cellular assays for DKI5 are performed using cells that express LOX-1, such as endothelial cells, macrophages, or cells transfected with LOX-1 expression constructs. Cells are treated with varying concentrations of the compound for specified time periods. The uptake of oxidized LDL is measured using fluorescently labeled oxLDL and flow cytometry or fluorescence microscopy. Lipid peroxidation is assessed by measuring malondialdehyde (MDA) or other lipid peroxidation products. Inflammatory markers (such as cytokine production) and oxidative stress markers are measured.
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| Animal Protocol |
In vivo studies of DKI5 are conducted in animal models of atherosclerosis, such as ApoE-deficient mice fed a high-fat diet. The compound is typically administered via intraperitoneal (i.p.) injection or oral gavage. Atherosclerotic plaque burden is assessed by histological analysis of the aorta. Inflammatory markers and oxidative stress markers are measured in plasma and tissues. LOX-1 expression and activity are assessed in vascular tissues.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of DKI5 (molecular weight 194.26, molecular formula C8H10N4S) have been characterized. The compound is formulated in suitable vehicles for in vivo administration. Storage recommendations include powder storage at -20°C for up to 3 years and solution storage at -80°C for 6 months or -20°C for 1 month. Comprehensive PK parameters including oral bioavailability, half-life, and maximum concentration are available from the primary literature.
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| Toxicity/Toxicokinetics |
Comprehensive toxicological evaluations for DKI5 have been conducted as part of preclinical development. The compound's mechanism of action—inhibiting LOX-1 and reducing oxidized LDL uptake—suggests a favorable safety profile for cardiovascular applications. Standard safety pharmacology assessments would include evaluation of effects on cardiovascular function, inflammation, and oxidative stress.
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| References | |
| Additional Infomation |
DKI5 ((E)-N'-benzylidenehydrazinecarbothiohydrazide) is a LOX-1 inhibitor with an IC50 of 22.5 μM. LOX-1 is a scavenger receptor that mediates the uptake of oxidized LDL and plays a critical role in the pathogenesis of atherosclerosis, inflammation, and vascular dysfunction. DKI5 strongly inhibits lipid peroxidation and may possess anti-inflammatory and antioxidant activities. The compound is a valuable research tool for studying the role of LOX-1 in cardiovascular disease and for validating LOX-1 as a therapeutic target. DKI5 is available with purity specifications for research use.
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| Molecular Formula |
C8H10N4S
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| Molecular Weight |
194.256799221039
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| Exact Mass |
194.06
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| Elemental Analysis |
C, 49.46; H, 5.19; N, 28.84; S, 16.50
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| CAS # |
1101130-96-4
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| PubChem CID |
9576136
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| Appearance |
White to off-white solid powder
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| LogP |
1.5
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
13
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| Complexity |
187
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S=C(NN)N/N=C/C1C=CC=CC=1
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| InChi Key |
IZAXVUNREMHNOM-UXBLZVDNSA-N
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| InChi Code |
InChI=1S/C8H10N4S/c9-11-8(13)12-10-6-7-4-2-1-3-5-7/h1-6H,9H2,(H2,11,12,13)/b10-6+
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| Chemical Name |
(E)-N'-benzylidenehydrazinecarbothiohydrazide
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| Synonyms |
DK-I5; DK I5; DKI5;
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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 | 5.1477 mL | 25.7387 mL | 51.4774 mL | |
| 5 mM | 1.0295 mL | 5.1477 mL | 10.2955 mL | |
| 10 mM | 0.5148 mL | 2.5739 mL | 5.1477 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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