| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg | |||
| Other Sizes |
| Targets |
BPH-652 potassium specifically targets the enzyme CrtM (dehydrosqualene synthase) in Staphylococcus aureus. It acts as an inhibitor (blocker/antagonist) of CrtM with a Ki of 1.5 nM. The IC50 for inhibition of S. aureus pigment formation is 100-300 nM. By inhibiting this enzyme, it blocks the production of the virulence factor staphyloxanthin.
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| ln Vitro |
In vitro, BPH-652 potassium is a potent inhibitor of CrtM with a Ki of 1.5 nM. It inhibits S. aureus pigment formation with an IC50 of 100-300 nM. This activity demonstrates its ability to block the biosynthesis of staphyloxanthin, a key virulence factor.
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| ln Vivo |
Treatment with BPH-652 (0.5 mg twice day, i.p., days -1, 0, 1, and 2) significantly decreased S. When mouse kidney aureus bacterial counts were compared to controls (P < 0.001), 8 out of 13 samples fell below the detection threshold, whereas only 2 out of 14 samples in the control group did so. This means that, on average, the treatment group's viable bacteria were reduced by 98% [1].
In vivo, BPH-652 potassium has been shown to significantly decrease S. aureus bacterial counts in a mouse model of systemic infection. Treatment with BPH-652 (0.5 mg twice daily, i.p.) resulted in an average reduction of 98% in viable bacteria in the kidneys. This demonstrates its efficacy in impairing bacterial virulence in vivo. |
| Enzyme Assay |
Cell-free assays for BPH-652 potassium focus on its ability to inhibit the enzymatic activity of CrtM. In these assays, the recombinant CrtM enzyme is incubated with its substrate and varying concentrations of the inhibitor. The production of the enzymatic product is measured, and the IC50 is calculated.
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| Cell Assay |
In vitro cell-based assays for BPH-652 potassium are performed to measure its effect on S. aureus pigment formation. Bacteria are cultured in the presence of varying concentrations of the compound, and the amount of staphyloxanthin pigment produced is measured spectrophotometrically. The IC50 for pigment inhibition is then calculated.
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| Animal Protocol |
Animal/Disease Models: Mouse systemic Staphylococcus aureus infection model [1].
Doses: 0.5 mg twice (two times) daily (days -1, 0, 1 and 2). Route of Administration: intraperitoneal (ip) injection. Experimental Results: The number of Staphylococcus aureus in the kidneys of mice in the BPH-652 treatment group was Dramatically lower than that in the control group. In vivo animal experiments for BPH-652 potassium are conducted in mouse models of systemic S. aureus infection. Mice are treated with the compound (e.g., 0.5 mg twice daily, i.p.), and the bacterial load in organs such as the kidneys is measured. The reduction in bacterial counts compared to controls indicates the compound's efficacy. |
| ADME/Pharmacokinetics |
Pharmacokinetic (PK) data for BPH-652 potassium is not detailed in the available literature. It is typically administered via intraperitoneal (i.p.) injection in animal studies. For storage, it is recommended to keep the powder at -20°C.
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| Toxicity/Toxicokinetics |
Toxicological data for BPH-652 potassium is not available in the public literature. As a research compound, its safety profile has not been extensively characterized. Its use is strictly for research purposes.
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| References |
[1]. Liu CI, et al. A cholesterol biosynthesis inhibitor blocks Staphylococcus aureus virulence. Science. 2008 Mar 7;319(5868):1391-4.
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| Additional Infomation |
BPH-652 potassium is a research-grade compound used to study the role of staphyloxanthin in S. aureus virulence. It is a potent inhibitor of CrtM with a Ki of 1.5 nM. It has not been approved for clinical use. All information is for research reference only.
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| Molecular Formula |
C16H16K3O7PS
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|---|---|
| Molecular Weight |
500.6277
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| Exact Mass |
499.926
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| CAS # |
157124-84-0
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| Related CAS # |
188526-11-6 (acid);157124-84-0 (potassium);
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| PubChem CID |
16730264
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| Appearance |
Typically exists as solid at room temperature
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
28
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| Complexity |
523
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
DRADVLDMPYYQDB-UHFFFAOYSA-K
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| InChi Code |
InChI=1S/C16H19O7PS.3K/c17-24(18,19)16(25(20,21)22)11-5-7-13-6-4-10-15(12-13)23-14-8-2-1-3-9-14;;;/h1-4,6,8-10,12,16H,5,7,11H2,(H2,17,18,19)(H,20,21,22);;;/q;3*+1/p-3
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| Chemical Name |
tripotassium;4-(3-phenoxyphenyl)-1-phosphonatobutane-1-sulfonate
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
H2O : ~25 mg/mL (~49.94 mM)
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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 | 1.9975 mL | 9.9874 mL | 19.9748 mL | |
| 5 mM | 0.3995 mL | 1.9975 mL | 3.9950 mL | |
| 10 mM | 0.1997 mL | 0.9987 mL | 1.9975 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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