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| 50mg |
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| Other Sizes |
| Targets |
BLT-1 primarily targets scavenger receptor B, type 1 (SR-BI), a cell surface receptor that mediates the selective uptake of cholesteryl esters from HDL. By inhibiting SR-BI, BLT-1 blocks the transfer of lipids between HDL and cells. This inhibition affects both the cellular uptake of HDL cholesteryl ether and the efflux of cellular cholesterol to HDL. SR-BI also plays a role in HCV entry, and BLT-1 inhibits HCV entry by blocking SR-BI function.
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| ln Vitro |
In ldlA[mSR-BI] cells, the IC50 of BLT-1 for DiI-HDL and [3H]CE-HDL was 60 and 110 nM, respectively [1]. The contribution of BLT-1 to HCV in Huh 7.5.1 cells BLT-1 (50 μM; 3 hr) does not cause broad abnormalities in the intracellular membrane trafficking of HeLa and BSC-1 cells that are reliant and independent of amyloid [1]. 0.96 μM is the IC50[4]. mSR-BI-t1's [3H]CE-cell-contained modulator (IC50=0.057 μM) and modulator (IC50=0.098 μM) can both be inhibited by BLT-1 on [3H]CE-HDL [2].
In vitro, BLT-1 is a potent inhibitor of SR-BI-mediated lipid transfer. It inhibits the uptake of DiI-HDL and [³H]CE-HDL in ldlA[mSR-BI] cells with IC50s of 60 and 110 nM, respectively. It also inhibits SR-BI-dependent selective uptake of [³H]CE from HDL in liposomes with an IC50 of 0.098 µM. BLT-1 inhibits HCV entry in Huh 7.5.1 cells with an IC50 of 0.96 μM. At 50 µM, it does not induce general defects in intracellular membrane trafficking. |
| ln Vivo |
Specific in vivo activity data for BLT-1 is not detailed in the provided search results. As an SR-BI inhibitor and HCV entry inhibitor, it is being investigated for its potential in treating HCV infection and studying lipid metabolism. SR-BI is a key receptor for HCV entry, and its inhibition represents a potential therapeutic strategy for preventing HCV infection. Further studies are needed to characterize its in vivo efficacy and safety.
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| Enzyme Assay |
The in vitro activity of BLT-1 is assessed using cell-based lipid uptake and efflux assays. Cells expressing SR-BI (e.g., ldlA[mSR-BI] cells) are incubated with fluorescently labeled or radiolabeled HDL (e.g., DiI-HDL, [³H]CE-HDL) in the presence of varying concentrations of BLT-1. The uptake of lipids into cells or the efflux of cholesterol from cells is measured. The IC50 is determined from dose-response curves. For HCV entry assays, Huh 7.5.1 cells are infected with HCV in the presence of BLT-1.
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| Cell Assay |
For cellular assays, ldlA[mSR-BI] cells or Huh 7.5.1 hepatoma cells are cultured in appropriate media. Cells are treated with various concentrations of BLT-1 (typically 0.01-100 µM) for defined periods. For lipid uptake assays, cells are incubated with labeled HDL, and the fluorescence or radioactivity is measured. For HCV entry assays, cells are infected with HCV, and viral replication is assessed by measuring HCV RNA or protein levels. Cell viability is assessed using standard assays.
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| Animal Protocol |
In vivo, BLT-1 would be administered to animal models of HCV infection or dyslipidemia. The compound is formulated in a suitable vehicle (e.g., 10% DMSO, 40% PEG300, 5% Tween-80, and 45% saline) and administered at various doses via intraperitoneal or oral routes. In HCV models, viral load is measured. In dyslipidemia models, lipid profiles are assessed. Pharmacodynamic studies involve measuring SR-BI activity in tissues.
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| ADME/Pharmacokinetics |
BLT-1 has a molecular weight of 241.40 g/mol and a molecular formula of C12H23N3S. It is soluble in DMSO at 41.67 mg/mL. The compound should be stored as a powder at -20°C for up to 3 years or at 4°C for up to 2 years. For in vivo administration, it can be formulated in 10% DMSO, 40% PEG300, 5% Tween-80, and 45% saline. The compound has a logP of 3.3.
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| Toxicity/Toxicokinetics |
Specific toxicity data for BLT-1 is not available in the provided search results. As an SR-BI inhibitor, it may affect cholesterol metabolism and potentially impact cardiovascular health. The compound is intended for research purposes only and is not approved for human or veterinary use. Standard laboratory safety precautions should be followed when handling the compound. Comprehensive toxicological studies are required to establish its full safety profile.
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| References |
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| Additional Infomation |
BLT-1 (Block lipid transport-1) is a research compound that selectively inhibits SR-BI-mediated lipid transfer. It is also a potent HCV entry inhibitor. SR-BI is a key receptor for HCV entry, and its inhibition is a potential therapeutic strategy for preventing HCV infection. BLT-1 is a valuable tool for studying lipid metabolism, cholesterol transport, and viral entry mechanisms. The compound is not approved for clinical use and is intended for research purposes only.
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| Molecular Formula |
C12H23N3S
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| Molecular Weight |
241.397
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| Exact Mass |
241.161
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| CAS # |
321673-30-7
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| PubChem CID |
9585336
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| Appearance |
White to light yellow solid powder
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| Density |
1.14±0.1 g/cm3
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| Boiling Point |
359.6±25.0 °C
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| LogP |
4.057
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
16
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| Complexity |
251
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCCCCCC\1CCC/C1=N\NC(=S)N
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| InChi Key |
OWGUSBISUVLUJF-KAMYIIQDSA-N
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| InChi Code |
InChI=1S/C12H23N3S/c1-2-3-4-5-7-10-8-6-9-11(10)14-15-12(13)16/h10H,2-9H2,1H3,(H3,13,15,16)/b14-11-
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| Chemical Name |
2-Hexyl-1-cyclopentanone thiosemicarbazone
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| Synonyms |
BLT-1 BLT 1 BLT1
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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 : ~41.67 mg/mL (~172.62 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (8.62 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 20.8 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: 2.08 mg/mL (8.62 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 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: ≥ 2.08 mg/mL (8.62 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 | 4.1425 mL | 20.7125 mL | 41.4250 mL | |
| 5 mM | 0.8285 mL | 4.1425 mL | 8.2850 mL | |
| 10 mM | 0.4143 mL | 2.0713 mL | 4.1425 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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