| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Targets |
ADDA 5 Hydrochloride targets cytochrome c oxidase (CcO), the terminal enzyme of the mitochondrial electron transport chain. CcO catalyzes the transfer of electrons from cytochrome c to molecular oxygen, a critical step in oxidative phosphorylation and ATP production. ADDA 5 is a partially noncompetitive inhibitor of CcO, meaning it binds to a site distinct from the substrate binding site and reduces the enzyme's maximum rate of activity. By inhibiting CcO, ADDA 5 disrupts mitochondrial respiration, leading to a depletion of the bioenergetics reserve capacity in cells. This metabolic disruption is particularly detrimental to cancer cells, which are highly dependent on aerobic glycolysis and oxidative phosphorylation for survival and proliferation.
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| ln Vitro |
Purified CcO from human glioblastoma and bovine heart had IC50 values of 18.93 μM and 31.82 μM for ADDA 5 HydroHClide, indicating that it is a somewhat non-competitive inhibitor of CcO. In GSCs generated from UTMZ and Jx22, ADDA 5 inhibits CcO activity with IC50 values of 21.4 ± 3.9 μM and 15.5 ± 2.8 μM, respectively. With an EC50 of 8.17 μM, ADDA 5 (25 μM) inhibits the development of UTMZ cells[1].
In vitro, ADDA 5 Hydrochloride is a potent inhibitor of CcO activity. It inhibits CcO isolated from human glioma cells and bovine cardiomyocytes with IC50 values of 18.93 μM and 31.82 μM, respectively. In glioma stem cells (GSCs) generated from UTMZ and Jx22, ADDA 5 inhibits CcO activity with IC50 values of 21.4 ± 3.9 μM and 15.5 ± 2.8 μM, respectively. ADDA 5 (25 μM) inhibits the development of UTMZ cells with an EC50 of 8.17 μM. The compound specifically inhibits the proliferation of chemosensitive and chemoresistant glioma cells while sparing non-cancer cells. These in vitro studies confirm ADDA 5's potent and selective anti-glioma activity. |
| ln Vivo |
At dosages up to 80 mg/kg, ADDA 5 does not induce observable toxicity in animals, and it effectively suppressed tumor growth in mice (8 mg/kg, ip) [1].
In vivo, ADDA 5 Hydrochloride has shown efficacy in suppressing tumor growth in mice. At doses up to 80 mg/kg, ADDA 5 does not induce observable toxicity in animals, and it effectively suppressed tumor growth in mice at 8 mg/kg (intraperitoneal injection). These findings suggest that ADDA 5 has a favorable therapeutic window and can be administered at doses that are effective against tumors without causing significant toxicity. The compound's ability to specifically target glioma cells while sparing normal cells is a key feature of its therapeutic potential. These in vivo studies provide evidence for the potential of ADDA 5 as an anti-cancer agent. |
| Enzyme Assay |
In vitro enzyme assays for ADDA 5 Hydrochloride measure its inhibition of cytochrome c oxidase (CcO) activity. CcO is isolated from cells or tissues (e.g., human glioblastoma or bovine heart) and its activity is measured using a standard assay that monitors the oxidation of reduced cytochrome c. The enzyme is incubated with varying concentrations of ADDA 5, and the decrease in enzyme activity is measured. The IC50 is determined from the dose-response curve. These assays confirm ADDA 5's mechanism of action as a CcO inhibitor.
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| Cell Assay |
In vitro cell-based assays for ADDA 5 Hydrochloride are used to study its effects on cancer cell metabolism and proliferation. Glioma cells (e.g., UTMZ, Jx22) are treated with ADDA 5 at various concentrations. Cell viability is assessed using assays such as MTT or CellTiter-Glo. Mitochondrial function is assessed by measuring oxygen consumption rates or ATP levels. The compound's ability to deplete the bioenergetics reserve capacity and inhibit cell proliferation is measured. These assays confirm the compound's selective anti-glioma activity and its effects on mitochondrial respiration.
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| Animal Protocol |
In vivo animal experiments for ADDA 5 Hydrochloride have been conducted in mouse models of glioma. In a typical study, mice bearing glioma xenografts are treated with ADDA 5 at doses of 8 mg/kg (intraperitoneal injection). Tumor growth is monitored by caliper measurements, and tumor regression or growth inhibition is assessed. Toxicity is evaluated by monitoring body weight, clinical signs, and organ histology. At doses up to 80 mg/kg, ADDA 5 does not induce observable toxicity, and it effectively suppressed tumor growth in mice. These studies provide evidence for the in vivo efficacy and safety of ADDA 5.
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| ADME/Pharmacokinetics |
ADDA 5 Hydrochloride has a molecular weight of 406.0 g/mol and a molecular formula of C24H36ClNO2. Its chemical name is 1-[2-(adamantan-1-yl)ethoxy]-3-(1,2,3,4-tetrahydroisoquinolin-2-yl)propan-2-ol hydrochloride. It is a white to off-white solid powder. It is soluble in DMSO. For storage, it is recommended to keep the powder at -20°C for up to 3 years or at 4°C for up to 2 years. In solvent, it can be stored at -80°C for 6 months or at -20°C for 1 month. Detailed pharmacokinetic properties such as absorption, distribution, metabolism, and excretion (ADME) have not been extensively characterized.
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| Toxicity/Toxicokinetics |
Detailed toxicity data for ADDA 5 Hydrochloride is available from preclinical studies. At doses up to 80 mg/kg, ADDA 5 does not induce observable toxicity in animals. The compound specifically inhibits the proliferation of chemosensitive and chemoresistant glioma cells while sparing non-cancer cells, suggesting a favorable safety profile. However, comprehensive toxicological studies, including acute and chronic toxicity studies, have not been extensively reported. As with all research chemicals, standard laboratory safety precautions should be followed when handling ADDA 5 Hydrochloride. Its use is limited to research applications and it is not intended for human or veterinary use.
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| References |
[1]. Oliva CR, et al. Identification of Small Molecule Inhibitors of Human Cytochrome c Oxidase That Target Chemoresistant Glioma Cells. J Biol Chem. 2016 Nov 11;291(46):24188-24199. Epub 2016 Sep 27
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| Additional Infomation |
ADDA 5 Hydrochloride is a research compound and is not approved for any clinical or therapeutic use. It is a synthetic small-molecule inhibitor of cytochrome c oxidase (CcO). ADDA 5 is a partially noncompetitive inhibitor of CcO that depletes the bioenergetics reserve capacity in intact glioma cells. It specifically inhibits the proliferation of chemosensitive and chemoresistant glioma cells while sparing non-cancer cells. In vivo, it effectively suppressed tumor growth in mice at 8 mg/kg without observable toxicity up to 80 mg/kg. ADDA 5 Hydrochloride is a valuable research tool for studying mitochondrial bioenergetics and cancer metabolism, particularly in the context of glioblastoma.
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| Molecular Formula |
C24H36CLNO2
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| Molecular Weight |
406.001146316528
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| Exact Mass |
405.243
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| CAS # |
473268-46-1
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| PubChem CID |
2882960
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
28
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| Complexity |
465
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Cl.OC(CN1CCC2C(=CC=CC=2)C1)COCCC12CC3CC(C1)CC(C3)C2
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| InChi Key |
YZSRZEWBOXEFRJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H35NO2.ClH/c26-23(16-25-7-5-21-3-1-2-4-22(21)15-25)17-27-8-6-24-12-18-9-19(13-24)11-20(10-18)14-24;/h1-4,18-20,23,26H,5-17H2;1H
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| Chemical Name |
1-[2-(1-adamantyl)ethoxy]-3-(3,4-dihydro-1H-isoquinolin-2-yl)propan-2-ol;hydrochloride
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| Synonyms |
ADDA5 Hydrochloride ADDA 5 Hydrochloride ADDA-5 Hydrochloride
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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) |
DMSO : ~65 mg/mL (~160.10 mM)
H2O : ~2 mg/mL (~4.93 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.12 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 20.8 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: ≥ 2.08 mg/mL (5.12 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 20.8 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: ≥ 2.08 mg/mL (5.12 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4631 mL | 12.3153 mL | 24.6305 mL | |
| 5 mM | 0.4926 mL | 2.4631 mL | 4.9261 mL | |
| 10 mM | 0.2463 mL | 1.2315 mL | 2.4631 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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