| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
| Targets |
Leishmania
bpV(phen) trihydrate targets protein tyrosine phosphatases (PTPs) and the tumor suppressor PTEN (phosphatase and tensin homolog), with selectivity for PTEN over other PTP family members. The compound also exhibits inhibitory activity against Leishmania parasites. |
|---|---|
| ln Vitro |
In H/R-damaged H9c2 cells, treatment with bpV (phen) (5 μM; 24.5 hours; H9c2 cells) further reduced cell viability [1]. H/R-damaged H9c2 cells undergo increased apoptosis upon treatment with bpV (phen) (5 μM; 24.5 hours) [1]. H/R-damaged H9c2 cells' cytoplasmic cytochrome c accumulation was markedly enhanced by bpV (phen) (5 μM; 24.5 hours; H9c2 cells) treatment [1]. Stimulation with bpV (phen) inhibits PTEN-induced putative kinase protein 1 (PINK1)/Parkin-mediated mitophagy [1]. The insulin receptor tyrosine kinase is hyperphosphorylated and activated, resulting in the insulin mimic bpV (phen) [4].
In vitro, bpV(phen) trihydrate effectively inhibits PTEN and PTPs, leading to enhanced insulin signaling and activation of the Th1-type immune response characterized by IL-12 and IFNgamma production. The compound promotes apoptosis in certain cell types and possesses anti-angiogenic and anti-tumor properties. It also inhibits the proliferation of Leishmania parasites in vitro. |
| ln Vivo |
The mean tumor volume was significantly reduced in male BALB/c nude (nu/nu) athymic mice treated with bpV (phen) (5 mg/kg; intraperitoneal injection; daily; for 38 days) [1].
In vivo, bpV(phen) trihydrate has demonstrated anti-tumor activity through its inhibition of PTEN and PTPs, which activates downstream signaling pathways involved in cell survival and proliferation. The compound's insulin-mimetic properties suggest potential applications in diabetes research, though detailed in vivo pharmacokinetic and efficacy data are limited. |
| Enzyme Assay |
For in vitro enzyme/receptor binding assays, bpV(phen) trihydrate is typically evaluated using recombinant PTEN, PTP-beta, and PTP-1B enzymes in phosphatase activity assays. The compound is incubated with the enzyme and a suitable substrate (e.g., p-nitrophenyl phosphate), and the inhibitory activity is determined by measuring the reduction in phosphatase activity. IC₅0 values are calculated from dose-response curves.
|
| Cell Assay |
Cell Viability Assay[1]
Cell Types: Hypoxia/reoxygenation (H/R)-injured H9c2 cells Tested Concentrations: 5 μM Incubation Duration: 24.5 hrs (hours) (hypoxia for 24 h; reoxygenation for 30 minutes) Experimental Results: Caused a further decrease of cell viability. Apoptosis Analysis[1] Cell Types: Hypoxia/reoxygenation (H/R)-injured H9c2 cells Tested Concentrations: 5 μM Incubation Duration: 24.5 hrs (hours) (hypoxia for 24 h; reoxygenation for 30 minutes) Experimental Results: Increased the apoptosis of H/R-injured H9c2 cells. Western Blot Analysis[1] Cell Types: Hypoxia/reoxygenation (H/R)-injured H9c2 cells Tested Concentrations: 5 μM Incubation Duration: 24.5 hrs (hours) (hypoxia for 24 h; reoxygenation for 30 minutes) Experimental Results: demonstrated an increased release of Cytochrome C. For in vitro cellular assays, bpV(phen) trihydrate is dissolved in an appropriate solvent (e.g., DMSO) and applied to cultured cells at varying concentrations. Cellular effects such as apoptosis, cytokine secretion, and signaling pathway activation (e.g., AKT phosphorylation) are assessed using flow cytometry, ELISA, or Western blotting. The compound is typically used at concentrations ranging from nanomolar to low micromolar. |
| Animal Protocol |
Animal/Disease Models: Male BALB/c nude (nu/nu) athymic mice (6-7 weeks old) injected with PC-3 cells[2]
Doses: 5 mg/kg Route of Administration: intraperitoneal (ip)injection; daily; for 38 days Experimental Results: Caused a significant reduction in average tumor volume. In vivo animal studies with bpV(phen) trihydrate typically involve oral or intraperitoneal administration in rodent models of cancer or metabolic disease. Dosing regimens, routes of administration, and efficacy endpoints (e.g., tumor volume reduction, blood glucose levels) are determined based on the specific research model. Detailed protocols are available in the primary literature. |
| ADME/Pharmacokinetics |
Systematic pharmacokinetic data for bpV(phen) trihydrate are limited. As a bisperoxovanadium compound, it is expected to have moderate oral bioavailability and is typically administered via intraperitoneal or oral routes in preclinical studies. The compound should be stored as a powder at -20degC for up to 3 years.
|
| Toxicity/Toxicokinetics |
Toxicity data for bpV(phen) trihydrate are primarily derived from in vitro studies. The compound can induce apoptosis in certain cell types and has been reported to promote the secretion of pro-inflammatory factors. As a phosphatase inhibitor, it may affect multiple signaling pathways; therefore, careful dose optimization is required in experimental settings.
|
| References |
[1]. Tang W, et al. PTEN-mediated mitophagy and APE1 overexpression protects against cardiac hypoxia/reoxygenation injury. In Vitro Cell Dev Biol Anim. 2019 Oct;55(9):741-748.
[2]. Caron D, et al. Protein tyrosine phosphatase inhibition induces anti-tumor activity: evidence of Cdk2/p27 kip1 and Cdk2/SHP-1 complex formation in human ovarian cancer cells. Cancer Lett. 2008 Apr 18;262(2):265-75. [3]. Schmid AC, et al. Bisperoxovanadium compounds are potent PTEN inhibitors. FEBS Lett. 2004 May 21;566(1-3):35-8. [4]. Band CJ, et al. Early signaling events triggered by peroxovanadium [bpV(phen)] are insulin receptor kinase (IRK)-dependent: specificity of inhibition of IRK-associated protein tyrosine phosphatase(s) by bpV(phen). Mol Endocrinol. 1997 Dec;11(13):1899-910. [5]. Chen Q, et al. Potassium Bisperoxo(1,10-phenanthroline)oxovanadate (bpV(phen)) Induces Apoptosis and Pyroptosis and Disrupts the P62-HDAC6 Protein Interaction to Suppress the Acetylated Microtubule-dependent Degradation of Autophagosomes. J Biol Chem. 2015 Oct 23;290(43):26051-8. |
| Additional Infomation |
bpV(phen) trihydrate (potassium bisperoxo(1,10-phenanthroline)oxovanadate(V) trihydrate) has a molecular weight of 404.29 and purity >98%. It is an insulin-mimetic agent that activates the Th1 pathway and has anti-angiogenic and anti-tumor activity. The compound is supplied as a solid powder and should be stored at -20degC. Not approved for clinical use; for research purposes only.
|
| Molecular Formula |
C12H14KN2O8V
|
|---|---|
| Molecular Weight |
404.29
|
| Exact Mass |
403.983
|
| CAS # |
171202-16-7
|
| Related CAS # |
bpV(phen);42494-73-5
|
| Appearance |
Yellow to orange solid powder
|
| LogP |
0.456
|
| SMILES |
[V]=O.[K+].[O-][O-].[O-][O-].O.O.O.N1C=CC=C2C=CC3=CC=CN=C3C=12
|
| 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 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)
|
| Solubility (In Vitro) |
H2O : 18.18 mg/mL (44.97 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 25 mg/mL (61.84 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with heating and sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4735 mL | 12.3674 mL | 24.7347 mL | |
| 5 mM | 0.4947 mL | 2.4735 mL | 4.9469 mL | |
| 10 mM | 0.2473 mL | 1.2367 mL | 2.4735 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
