| Size | Price | Stock | Qty |
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| 50mg |
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| Targets |
BPU-11 targets the HCN4 channel, specifically binding to the C-linker pocket (CLP). HCN channels are responsible for the hyperpolarization-activated inward current (Ih) that contributes to pacemaker activity in the heart and brain. By binding to the CLP, BPU-11 modulates channel function and completely abolishes the cAMP-induced shift in V1/2. It is HCN4 subtype-specific and has no effect on HCN2 channels expressed in HEK293T cells. Some sources also indicate BPU-11 binds to and inhibits USP7 (ubiquitin-specific protease 7).
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| ln Vitro |
BPU-11 (100 μM) with a k1/2 of 0.42 μM removes the V1/2 magnetic field that HCN4 cAMP induces [1]. HEK293T cells that express HCN2 channels are unaffected by BPU (100 and 200 μM), which is a powerful HCN4 isoform [1].
In vitro, BPU-11 is a HCN4 CLP ligand that acts by modulating channel function and completely abolishing the cAMP-induced shift in V1/2. It has a k1/2 of 0.42 µM for this effect. The compound is HCN4 subtype-specific and has no effect on HCN2 channels expressed in HEK293T cells. Its activity is characterized by its ability to bind to the HCN4 CLP and prevent cAMP-induced modulation of channel gating. Some sources indicate BPU-11 binds to and inhibits USP7 (ubiquitin-specific protease 7) activity. |
| ln Vivo |
Specific in vivo activity data for BPU-11 is not detailed in the provided search results. As a HCN4 channel modulator, it may have potential applications in the treatment of conditions involving abnormal cardiac or neuronal pacemaker activity. The compound's ability to modulate HCN4 channel function suggests potential for the research of arrhythmias or neurological disorders. Its reported activity as a USP7 inhibitor may also have implications for cancer and immune research.
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| Enzyme Assay |
The in vitro activity of BPU-11 is assessed using electrophysiological techniques, such as the patch-clamp technique, on cells expressing HCN4 channels. HEK293T cells are transfected with HCN4 channels and voltage-clamped. The hyperpolarization-activated current (Ih) is elicited by hyperpolarizing voltage steps. Various concentrations of BPU-11 are applied, and the shift in V1/2 is measured. The ability of BPU-11 to abolish the cAMP-induced shift in V1/2 is assessed by co-application of cAMP. The k1/2 is determined from dose-response curves. For USP7 inhibition studies, cell-free enzyme assays are used.
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| Cell Assay |
For cellular assays, HEK293T cells expressing HCN4 or HCN2 channels are cultured in appropriate media. Cells are treated with various concentrations of BPU-11 (typically 0.01-100 µM) for defined periods. HCN channel function is assessed using patch-clamp electrophysiology. Cell viability is assessed using standard assays. For USP7 inhibition studies, cells are treated with BPU-11, and the ubiquitination status of USP7 substrates is analyzed by Western blotting.
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| Animal Protocol |
In vivo, BPU-11 would be administered to animal models via intraperitoneal or oral routes. The compound is formulated in a suitable vehicle (e.g., 5% DMSO, 40% PEG300, 5% Tween-80, and 50% ddH2O) and administered at various doses. In models of cardiac arrhythmia or neurological disorders, the compound's effects on heart rate, rhythm, or neuronal activity would be assessed. Pharmacodynamic studies involve measuring the effects on HCN channel function in target tissues.
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| ADME/Pharmacokinetics |
BPU-11 has a molecular weight of 501.62 g/mol and a molecular formula of C32H31N5O. It is a small molecule that is soluble in DMSO. The compound should be stored as a powder at -20°C under desiccated conditions. Specific pharmacokinetic parameters such as bioavailability, half-life, and volume of distribution are not detailed in the provided search results. The compound's ability to cross the blood-brain barrier is not specified.
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| Toxicity/Toxicokinetics |
Specific toxicity data for BPU-11 is not available in the provided search results. As a HCN channel modulator and potential USP7 inhibitor, it may affect normal cellular processes, including cardiac pacemaker activity and protein degradation. 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 | |
| Additional Infomation |
BPU-11 is a research compound that has been developed as a HCN4 CLP ligand for studying HCN channel function and modulation. HCN channels are important targets for the treatment of cardiac arrhythmias and neurological disorders. BPU-11 is also reported to be a USP7 inhibitor, which may have implications for cancer and immune research. The compound is not approved for clinical use and is intended for research purposes only. It is available from chemical suppliers for research applications.
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| Molecular Formula |
C32H31N5O
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| Molecular Weight |
501.621446847916
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| Exact Mass |
501.252
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| Elemental Analysis |
C, 76.62; H, 6.23; N, 13.96; O, 3.19
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| CAS # |
909664-41-1
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| PubChem CID |
24730758
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
5
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
38
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| Complexity |
780
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1CN(CCC1N(CC2=CN=CC=C2)C(=O)NC3=CC=CC=C3C4=CC=CC=C4)CC5=CC(=CC=C5)C#N
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| InChi Key |
UIIRFZUAAAFHFB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C32H31N5O/c33-21-25-8-6-9-26(20-25)23-36-18-15-29(16-19-36)37(24-27-10-7-17-34-22-27)32(38)35-31-14-5-4-13-30(31)28-11-2-1-3-12-28/h1-14,17,20,22,29H,15-16,18-19,23-24H2,(H,35,38)
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| Chemical Name |
1-[1-[(3-cyanophenyl)methyl]piperidin-4-yl]-3-(2-phenylphenyl)-1-(pyridin-3-ylmethyl)urea
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| Synonyms |
BPU11; BPU 11; BPU-11
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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 : ~125 mg/mL (~249.19 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 | 1.9935 mL | 9.9677 mL | 19.9354 mL | |
| 5 mM | 0.3987 mL | 1.9935 mL | 3.9871 mL | |
| 10 mM | 0.1994 mL | 0.9968 mL | 1.9935 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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