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BLT-1

Alias: BLT-1 BLT 1 BLT1
Cat No.:V12868 Purity: ≥98%
BLT-1 is a sulfur semicarbocopper chelator and selective scavenger receptor type B1 (SR-BI) inhibitor.
BLT-1
BLT-1 Chemical Structure CAS No.: 321673-30-7
Product category: New1
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
50mg
Other Sizes
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Product Description
BLT-1 is a sulfur semicarbocopper chelator and selective scavenger receptor type B1 (SR-BI) inhibitor. BLT-1 inhibits SR-BI-mediated lipid transfer between high-density lipoprotein (HDL) and cells. BLT-1 is a potent HCV (hepatitis C virus) entry inhibitor.
Biological Activity I Assay Protocols (From Reference)
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].
References

[1]. Discovery of chemical inhibitors of the selective transfer of lipids mediated by the HDL receptorSR-BI. Proc Natl Acad Sci U S A. 2002 Nov 26;99(24):15422-7.

[2]. Identification of the molecular target of small molecule inhibitors of HDL receptor SR-BI activity. Biochemistry. 2008 Jan 8;47(1):460-72.

[3]. BLT-1, a specific inhibitor of the HDL receptor SR-BI, induces a copper-dependent phenotype during zebrafish development. Toxicol Lett. 2007 Dec 10;175(1-3):1-7. Epub 2007 Aug 22.

[4]. Reply to Padmanabhan and Dixit: Hepatitis C virus entry inhibitors for optimally boosting direct-acting antiviral-based treatments. Proc Natl Acad Sci U S A. 2017 Jun 6;114(23):E4527-E4529.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C12H23N3S
Molecular Weight
241.397
Exact Mass
241.161
CAS #
321673-30-7
PubChem CID
9585336
Appearance
White to light yellow solid powder
Density
1.14±0.1 g/cm3
Boiling Point
359.6±25.0 °C
LogP
4.057
Hydrogen Bond Donor Count
2
Hydrogen Bond Acceptor Count
2
Rotatable Bond Count
6
Heavy Atom Count
16
Complexity
251
Defined Atom Stereocenter Count
0
SMILES
CCCCCCC\1CCC/C1=N\NC(=S)N
InChi Key
OWGUSBISUVLUJF-KAMYIIQDSA-N
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-
Chemical Name
2-Hexyl-1-cyclopentanone thiosemicarbazone
Synonyms
BLT-1 BLT 1 BLT1
HS Tariff Code
2934.99.9001
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)
Solubility Data
Solubility (In Vitro)
DMSO : ~41.67 mg/mL (~172.62 mM)
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.

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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.
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 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 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.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
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  • Enter 5 in the Volume box and choose the correct unit (mL)
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
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  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

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  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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.

Biological Data
  • High-throughput screen for inhibitors of SR-BI-mediated DiI uptake from DiI-HDL. Example of a fluorescent readout obtained from a single 384-well plate during the first round of the high-throughput screen. SR-BI-expressing ldlA[mSR-BI] cells were plated into 384-well plates, and the effect of compounds (≈10 μM) on the uptake of DiI from DiI-HDL (10 μg of protein per ml) was determined by using a high-speed fluorescence plate reader. Columns 1–20 show results (fluorescence in arbitrary units) from 16 independent wells per column (different colored symbols) from a single plate, representing a total of 320 compounds. Controls without compounds are wells containing ldlA[mSR-BI] cells in the absence or presence of a 40-fold excess of unlabeled HDL, or containing untransfected ldlA-7 cells (very low SR-BI expression). Wells containing an inhibitory compound named BLT-1 and wells with compounds that quenched DiI-HDL fluorescence (Q) are indicated.[1].Discovery of chemical inhibitors of the selective transfer of lipids mediated by the HDL receptorSR-BI. Proc Natl Acad Sci U S A. 2002 Nov 26;99(24):15422-7.
  • Cell surface expression of SR-BI. ldlA[mSR-BI] and ldlA-7 cells were treated for 3 h with or without BLTs at their corresponding IC95CE concentrations (1 μM for BLT-1 and BLT-2 and 50 μM for BLT-3–BLT-5) followed by determination of surface expression levels of SR-BI by flow cytometry. A–C show histograms of the surface expression for ldlA[mSR-BI] cells without BLTs, ldlA[mSR-BI] cells with 1 μM BLT-1, and ldlA-7 cells without BLTs, respectively. D summarizes the results in ldlA[mSR-BI] cells for all five BLTs, with the value determined without compounds set to 100%. n, number of independent determinations.[1].Discovery of chemical inhibitors of the selective transfer of lipids mediated by the HDL receptorSR-BI. Proc Natl Acad Sci U S A. 2002 Nov 26;99(24):15422-7.
  • Effects of BLT-1 on the concentration dependence of 125I-HDL binding to ldlA[mSR-BI] cells. The binding of 125I-HDL to ldlA[mSR-BI] cells was determined in duplicate at the indicated concentrations of HDL in the presence (blue) or absence (black) of 1 μM BLT-1 (IC95CE). Each value was corrected for binding of 125I-HDL in the presence of 40-fold excess of unlabeled HDL to ldlA [mSR-BI] cells in the presence of BLT-1.[1].Discovery of chemical inhibitors of the selective transfer of lipids mediated by the HDL receptorSR-BI. Proc Natl Acad Sci U S A. 2002 Nov 26;99(24):15422-7.
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