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| Targets |
The primary targets of Amotosalen hydrochloride are nucleic acids, specifically DNA and RNA of pathogens and leukocytes. Prior to administration, amotosalen is added to plasma and platelets; then the agent penetrates pathogens and targets DNA and RNA. Upon activation by UVA light, the compound forms covalent interstrand crosslinks between pyrimidine bases in DNA and RNA. This crosslinking prevents nucleic acid replication and transcription, effectively inactivating the pathogen. Inactivation of leukocytes can prevent graft-versus-host disease upon transfusion. The compound does not target specific proteins or receptors but rather the genetic material of cells.
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| ln Vitro |
Amoxalin hydrochloride attaches to the carotene linkage and stops replication when it is exposed to light. Amoxalin hydrochloride that has been activated by light attaches to DNA and creates a permanent cross-link, which inhibits replication and halts the growth of donor T cells [1].
In vitro, Amotosalen hydrochloride demonstrates potent pathogen inactivation activity when activated by UVA light. The compound attaches to nucleic acids and stops replication upon light exposure. Light-activated amotosalen attaches to DNA and creates a permanent cross-link, which inhibits replication and halts the growth of donor T cells. The compound is effective against a broad spectrum of pathogens including bacteria, viruses, and protozoa. In vitro studies have demonstrated its efficacy in inactivating pathogens in platelet concentrates and plasma preparations without significantly affecting platelet function or plasma protein activity. These protocols are for reference only. |
| ln Vivo |
In vivo, Amotosalen hydrochloride is used ex vivo for the treatment of blood components prior to transfusion rather than as a systemically administered therapeutic. After UVA activation, the compound forms irreversible crosslinks in pathogen nucleic acids, preventing replication and rendering the pathogens non-infectious. The inactivated blood components can then be safely transfused to patients. The compound does not accumulate in the body as it is primarily used for ex vivo pathogen inactivation. Its effectiveness in preventing transfusion-transmitted infections has been demonstrated in clinical studies. Inactivation of leukocytes also reduces the risk of transfusion-associated graft-versus-host disease.
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| Enzyme Assay |
In vitro enzyme/receptor binding studies for Amotosalen hydrochloride typically focus on its interaction with nucleic acids rather than enzymes or receptors. The compound's ability to form crosslinks with DNA and RNA can be assessed using gel electrophoresis, where crosslinked nucleic acids show altered migration patterns. UVA activation conditions (typically 3 J/cm² UVA) are standardized. Binding to DNA can be quantified using spectrophotometric methods or fluorescence-based assays. The compound's photochemical properties can be characterized by measuring its absorption spectrum and photoreactivity. Pathogen inactivation efficacy can be evaluated by plaque assays or cell culture infectivity assays. These methods are for reference only and require independent validation.
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| Cell Assay |
In vitro cell-based assays for Amotosalen hydrochloride evaluate its pathogen inactivation efficacy and potential cytotoxicity. Pathogen inactivation is assessed by spiking blood components with known quantities of pathogens (e.g., bacteria, viruses) followed by amotosalen treatment and UVA activation, then measuring residual infectivity via culture methods. Cytotoxicity assays (e.g., MTT or LDH release) are performed on relevant cell lines to evaluate any potential toxic effects of the compound or its photoproducts. Platelet function assays (e.g., aggregation, activation markers) and plasma protein activity assays are conducted to ensure that the treatment does not compromise the quality of the blood component. Standard cell culture conditions are used.
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| Animal Protocol |
In vivo animal studies for Amotosalen hydrochloride are conducted to evaluate the safety and efficacy of pathogen-inactivated blood components. Typical protocols involve transfusion of amotosalen/UVA-treated blood components into animal models (e.g., mice, rats, or non-human primates) followed by assessment of transfusion safety, efficacy, and any adverse effects. Pathogen challenge studies may be performed where animals receive pathogen-spiked blood components treated with amotosalen/UVA to demonstrate protection from infection. Pharmacokinetic studies may evaluate the clearance of the compound and its photoproducts following transfusion. All procedures must comply with institutional animal care guidelines.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of Amotosalen hydrochloride are relevant to its ex vivo use in blood component processing. After addition to blood components and UVA activation, the compound forms covalent adducts with nucleic acids. Unreacted compound and photoproducts are largely removed during the processing steps or are rapidly cleared following transfusion. The compound has low systemic exposure as it is not administered directly to patients. Its metabolites are primarily excreted in urine. The pharmacokinetic profile in the context of ex vivo use is characterized by rapid clearance and minimal accumulation. Detailed pharmacokinetic parameters may vary depending on the specific blood component and processing conditions.
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| Toxicity/Toxicokinetics |
Toxicological data for Amotosalen hydrochloride are primarily derived from its use in blood component processing. The compound is for research use only and not for direct human administration. In ex vivo applications, the risk of toxicity is minimized as the compound is largely removed or inactivated before transfusion. However, potential toxicities include the formation of photoproducts and the possibility of nucleic acid damage in transfused cells. Preclinical toxicology studies in animal models have evaluated the safety of transfused pathogen-inactivated blood components. The compound should be handled with appropriate safety precautions, including protection from light exposure.
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| References | |
| Additional Infomation |
Amotosalen hydrochloride is the hydrochloride form of Amotosalen, a synthetic psoralen and a photoactivated DNA/RNA cross-linking agent with protective effects against pathogens such as bacteria, viruses, protozoa, and leukocytes. Before administration, Amotosalen is added to plasma and platelets. In vivo, the drug penetrates pathogens and targets DNA and RNA. Upon activation by UVA irradiation, the drug forms cross-links between DNA and RNA chains, thereby inhibiting replication. Leukocyte inactivation can prevent graft-versus-host disease (GVHD) following blood transfusion.
Additional information: Amotosalen hydrochloride has the CAS number 161262-45-9 and the related CAS number 161262-29-9 (free base). The compound is also known as S-59. It is a white to light yellow solid powder with a boiling point of 488.8°C at 760 mmHg and a flash point of 249.4°C. The compound is soluble in DMSO at approximately 7.14 mg/mL (~21.14 mM). Storage: powder at -20°C for 3 years or 4°C for 2 years; in solvent at -80°C for 6 months or -20°C for 1 month. The compound should be stored in a sealed and protected environment, avoiding moisture exposure. Amotosalen hydrochloride is for research use only and is not approved for human therapeutic applications. |
| Molecular Formula |
C17H19NO4.HCL
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| Molecular Weight |
337.798
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| Exact Mass |
337.108
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| CAS # |
161262-45-9
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| Related CAS # |
161262-45-9 (HCl);161262-29-9;
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| PubChem CID |
159598
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| Appearance |
White to light yellow solid powder
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| Boiling Point |
488.8ºC at 760mmHg
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| Flash Point |
249.4ºC
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| Vapour Pressure |
1.06E-09mmHg at 25°C
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| LogP |
4.442
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
23
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| Complexity |
464
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Cl.NCCOCC1=C(C)OC2C(=C3OC(=O)C=C(C)C3=CC1=2)C
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| InChi Key |
MHLAMQBABOJZQW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H19NO4.ClH/c1-9-6-15(19)22-16-10(2)17-13(7-12(9)16)14(11(3)21-17)8-20-5-4-18;/h6-7H,4-5,8,18H2,1-3H3;1H
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| Chemical Name |
3-(2-aminoethoxymethyl)-2,5,9-trimethylfuro[3,2-g]chromen-7-one;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 : ~7.14 mg/mL (~21.14 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.71 mg/mL (2.10 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 7.1 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: ≥ 0.71 mg/mL (2.10 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 7.1 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: ≥ 0.71 mg/mL (2.10 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 | 2.9603 mL | 14.8017 mL | 29.6033 mL | |
| 5 mM | 0.5921 mL | 2.9603 mL | 5.9207 mL | |
| 10 mM | 0.2960 mL | 1.4802 mL | 2.9603 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05128084 | Unknown status | Congenital Heart Disease in Children | University Hospital, Strasbourg, France | 2020-10-01 | ||
| NCT05162378 | Unknown status | Heart Surgery | University Hospital, Strasbourg, France | 2020-10-21 | ||
| NCT04372979 | Terminated | Drug: Transfusion of SARS-CoV-2 Convalescent Plasma. Drug: Transfusion of standard Plasma. |
COVID-19 | Direction Centrale du Service de Santé des Armées | 2020-09-14 | Phase 3 |
| NCT04389944 | Completed | Other: convalescent plasma application to SARS-CoV-2 infected patients |
Coronavirus Disease 2019 Infectious Disease (COVID-19 Infection) |
University Hospital, Basel, Switzerland | 2020-03-31 | Not Applicable |
| NCT06291025 | Not yet recruiting | Procedure: PEX-FREE | Thrombotic Microangiopathies | University Hospital, Rouen | 2024-04-01 | Not Applicable |
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