| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
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Purity: ≥98%
| Targets |
PTEN (IC50 = 35 nM)
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| ln Vitro |
Since VO-OHpic is a sterically demanding compound with two OHpic and one oxo ligand, it makes sense that steric hindrance from the bound substrate would impact the inhibitor's subsequent binding. At low nanomolar doses (IC50, 46±10 nM), VO-OHpic substantially reduced PTEN activity, which is consistent with the efficacy found in a PIP3-based assay earlier (IC50, 35±2 nM). It was found that the inhibitory constants Kic and Kiu were, respectively, 27±6 and 45±11 nM[1]. A promising selective and effective PTEN inhibitor is VO-OHpic. The most effective PTEN lipid phosphatase activity inhibitor is VO-OHpic (IC50=35 nM)[2].
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| ln Vivo |
Mice's PTEN was suppressed by an intraperitoneal injection of VO-OHpic (10 μg/kg) 30 minutes before to ischemia, followed by exposure to ischemia for 30 minutes and reperfusion for 120 minutes. Triphenyltetrazolium chloride (TTC) was used to measure the size of the myocardial infarct at the conclusion of the experiment. In mice treated with VO, the size of the myocardial infarct was considerably smaller (25±6% vs. 56±5%, n=7, P<0.01). Between the two groups, there was no difference in the risk area (46±3% vs. 57±3%, n=7, P>0.05) [3].
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| References |
[1]. Mak LH, et al. Characterisation of the PTEN inhibitor VO-OHpic. J Chem Biol. 2010 Oct;3(4):157-63.
[2]. Rosivatz, E, et al. A small molecule inhibitor for phosphatase and tensin homologue deleted on chromosome 10 (PTEN). ACS Chem Biol. 2006 Dec 15;1(12):780-90. [3]. Zu L, et al. PTEN inhibitors cause a negative inotropic and chronotropic effect in mice. Eur J Pharmacol. 2011 Jan 10;650(1):298-302 |
| Molecular Formula |
C12H10N2O8V
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|---|---|
| Molecular Weight |
414.19
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| Exact Mass |
414.0115
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| Elemental Analysis |
C, 34.80; H, 3.65; N, 6.76; O, 42.49; V, 12.30
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| CAS # |
476310-60-8
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| Related CAS # |
VO-OHPic;675848-25-6
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| Appearance |
Solid powder
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| SMILES |
O=[V](OC(C1=NC=CC=C1O)=O)(O)OC(C2=NC=CC=C2O)=O.O.O.O
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| InChi Key |
HCJXRYXYWPOIGP-UHFFFAOYSA-K
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| InChi Code |
InChI=1S/2C6H5NO3.4H2O.O.V/c2*8-4-2-1-3-7-5(4)6(9)10;;;;;;/h2*1-3,8H,(H,9,10);4*1H2;;/q;;;;;;;+3/p-3
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| Chemical Name |
Hydroxy(oxo)vanadium 3-hydroxypyridine-2-carboxylic acid complex trihydrate
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| Synonyms |
VO OHpic; VO-OHpic; VOOHpic
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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: ~72 mg/mL (~173.4 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.02 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 25.0 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: ≥ 2.5 mg/mL (6.02 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 25.0 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% DMSO+40% PEG 300+2% Tween 80+ddH2O: 14mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4144 mL | 12.0718 mL | 24.1435 mL | |
| 5 mM | 0.4829 mL | 2.4144 mL | 4.8287 mL | |
| 10 mM | 0.2414 mL | 1.2072 mL | 2.4144 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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