| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
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| Other Sizes |
| Targets |
The primary target of ITPP is hemoglobin, to which it binds as an allosteric effector. By binding to hemoglobin, ITPP reduces the affinity of hemoglobin for oxygen, thereby facilitating the release of oxygen to tissues. This mechanism is particularly relevant in hypoxic conditions where improved oxygen delivery is therapeutic. The compound may also interact with other cellular targets involved in oxygen sensing and metabolism.
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| ln Vitro |
All six of the cell lines (FSaII, SiHa, MDA-MB-231, NT2, 9L-glioma, and rhabdomyosarcoma) exhibit significant inhibition of OCR when exposed to myo-Inositol trispyrophosphate hexasodium (10 mmol/L; 2 hours) [2].
In vitro studies demonstrate that ITPP enhances the oxygen release capacity of red blood cells by reducing the affinity of hemoglobin to oxygen. As a membrane-permeant compound, it can enter cells and exert its effects on intracellular hemoglobin. The compound's ability to reverse hypoxia has been demonstrated in cell-based assays. These properties make ITPP a valuable tool for studying oxygen delivery and hypoxia-related pathways. |
| ln Vivo |
The substantial effect of myo-Inositol trispyrophosphate hexasodium (2 g/kg weekly; IP; 7 weeks) on life prolonging persists[1]. Immunocompetent male Lewis rats weighing 120-150 g with DSL-6A/C1 cells do not develop metastases on pancreatic carcinomas when myo-Inositol trispyrophosphate hexasodium (1.5 g/kg weekly; IV; for 8 weeks) is administered. Tumor pO2 pressure is restored by myo-Inositol trispyrophosphate hexasodium, which also lowers proangiogenic and hypoxia-inducible factors[1]. Myo-Inositol trispyrophosphate hexasodium (2 g/kg; once daily for 2 days) in four mouse tumor models (mouse fibrosarcoma FSaII implanted in C3H mice, mouse mammary tumor NT2 in FVb/Nrj mice, and human breast cancer MDA-MB-231) exhibits the highest level of enhanced tumor oxygenation at 2 hours.
In vivo studies have shown that ITPP can reverse hypoxia, control tumor growth, and improve chemotherapy response in animal models. The compound is used in research on cardiovascular disease and cancer. Its ability to enhance oxygen delivery to tissues makes it a potential therapeutic agent for conditions characterized by hypoxia. Further in vivo studies are ongoing to fully characterize its therapeutic potential. |
| Enzyme Assay |
Non-cellular assays for ITPP typically involve measuring its effects on hemoglobin oxygen affinity using oxygen dissociation curve analysis. Hemoglobin is incubated with varying concentrations of ITPP, and the oxygen saturation is measured at different oxygen partial pressures. The P50 value (oxygen partial pressure at 50% saturation) is calculated to assess the compound's effect on hemoglobin oxygen affinity. These cell-free systems allow for direct characterization of the compound's allosteric effects on hemoglobin.
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| Cell Assay |
Cellular assays for ITPP are conducted using red blood cells to assess the compound's effects on oxygen release. Red blood cells are treated with ITPP, and oxygen release is measured using oxygen electrodes or similar techniques. The compound's ability to enter cells and bind to intracellular hemoglobin is also assessed. Cancer cell lines may be used to study the compound's effects on tumor growth and chemotherapy response under hypoxic conditions.
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| Animal Protocol |
Animal/Disease Models: Nude mice (20 g) with MiaPaCa-2 or DSL-6A/C1 cells[1]
Doses: 2 g/kg (weekly) Route of Administration: IP; weekly; 7weeks Experimental Results: Sustained its significant effect on life prolongation. In vivo animal experiments for ITPP typically use rodent models of cancer, cardiovascular disease, or other conditions characterized by hypoxia. The compound is administered via intravenous injection or oral gavage, and its effects on tumor growth, oxygen delivery, and chemotherapy response are assessed. Tissue oxygen levels may be measured using oxygen electrodes or imaging techniques. Blood samples are collected to measure hemoglobin oxygen affinity. |
| ADME/Pharmacokinetics |
Pharmacokinetic properties of ITPP include its membrane-permeant nature, which allows it to enter cells and bind to intracellular hemoglobin. The compound is water-soluble and is typically administered as a crystalline powder. Its half-life, distribution, metabolism, and excretion have not been fully characterized in the literature. As a highly polar molecule with multiple phosphate groups, it may have limited oral bioavailability.
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| Toxicity/Toxicokinetics |
Toxicological data for ITPP are limited, though the compound is used in research applications and is not approved for human use. As a derivative of myo-inositol, it may have a favorable safety profile, but comprehensive toxicological studies have not been extensively reported. Standard laboratory safety precautions should be followed when handling the compound.
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| References |
[1]. Zahary Raykov, et al. Myo-inositol trispyrophosphate-mediated hypoxia reversion controls pancreatic cancer in rodents and enhances gemcitabine efficacy. Int J Cancer. 2014 Jun 1;134(11):2572-82.
[2]. Ly-Binh-An Tran, et al. Impact of myo-inositol trispyrophosphate (ITPP) on tumour oxygenation and response to irradiation in rodent tumour models. J Cell Mol Med. 2019 Mar;23(3):1908-1916. [3]. Marta Oknińska, et al. Treatment of hypoxia-dependent cardiovascular diseases by myo-inositol trispyrophosphate (ITPP)-enhancement of oxygen delivery by red blood cells. J Cell Mol Med. 2020 Feb;24(3):2272-2283. |
| Additional Infomation |
Other information includes ITPP's role as a membrane-permeant allosteric effector of hemoglobin. It enhances oxygen release from red blood cells by reducing hemoglobin-oxygen affinity. The compound can reverse hypoxia, control tumor growth, and improve chemotherapy response. It is used in research on cardiovascular disease and cancer and has been explored for potential therapeutic benefits in conditions characterized by hypoxia.
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| Molecular Formula |
C6H6NA6O21P6
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|---|---|
| Molecular Weight |
737.88
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| Exact Mass |
737.721
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| CAS # |
23103-35-7
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| PubChem CID |
10439980
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| Appearance |
White to off-white solid powder
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| LogP |
2.633
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
21
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
39
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| Complexity |
857
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| Defined Atom Stereocenter Count |
0
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| SMILES |
[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].O=P1(OP(=O)([O-])OC2C(C3OP(=O)([O-])OP(=O)([O-])OC3C3OP(=O)([O-])OP(=O)([O-])OC32)O1)[O-]
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| InChi Key |
DTOYSAZRROROSE-UHFFFAOYSA-H
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| InChi Code |
InChI=1S/C6H12O21P6.6Na/c7-28(8)19-1-2(20-29(9,10)25-28)4-6(24-33(17,18)27-32(15,16)23-4)5-3(1)21-30(11,12)26-31(13,14)22-5;;;;;;/h1-6H,(H,7,8)(H,9,10)(H,11,12)(H,13,14)(H,15,16)(H,17,18);;;;;;/q;6*+1/p-6
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| Chemical Name |
hexasodium;4,6,11,13,18,20-hexaoxido-3,5,7,10,12,14,17,19,21-nonaoxa-4λ5,6λ5,11λ5,13λ5,18λ5,20λ5-hexaphosphatetracyclo[14.5.0.02,8.09,15]henicosane 4,6,11,13,18,20-hexaoxide
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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: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), 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 (33.88 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 | 1.3552 mL | 6.7762 mL | 13.5523 mL | |
| 5 mM | 0.2710 mL | 1.3552 mL | 2.7105 mL | |
| 10 mM | 0.1355 mL | 0.6776 mL | 1.3552 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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