| Size | Price | |
|---|---|---|
| Other Sizes |
| Targets |
HPMA is a monomer rather than a drug with a specific biological target. Its utility lies in its ability to polymerize into pHPMA, a biocompatible polymer used as a drug delivery vehicle. HPMA copolymer-drug conjugates with lysosomally degradable side chains have demonstrated considerable antileishmanial activity in vivo. The polymer serves as a macromolecular carrier for targeted delivery of therapeutic agents.
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|---|---|
| ln Vitro |
In vitro activity of HPMA is not applicable as the compound is a monomer used for polymer synthesis. However, HPMA copolymers have been studied in vitro for their ability to deliver drugs to cells. The polymers are taken up by cells via endocytosis and release their drug cargo in lysosomes due to the degradable side chains. HPMA copolymers are biocompatible and non-toxic to cells in vitro.
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| ln Vivo |
The N-(2-hydroxypropyl)methacrylamide copolymer-drug conjugates with side chains that are lysosomally degradable demonstrated considerable in vivo antibacterial activity at a drug equivalent dose of 5 mg/kg body weight. Shman activity with an inhibition of >99% [1].
In vivo, HPMA copolymer-drug conjugates (5 mg/kg) containing lysosomally degradable side chains have shown significant antileishmanial activity (>99% inhibition) in animal models of visceral leishmaniasis. The polymers accumulate in infected tissues and release the drug intracellularly, providing targeted therapy. These findings demonstrate the potential of HPMA-based drug delivery systems for infectious diseases. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays are not applicable for HPMA, as the compound is a monomer used for polymer synthesis rather than a pharmacologically active molecule. However, HPMA copolymers can be characterized by their molecular weight, polydispersity, and drug loading capacity. The release of drug from HPMA copolymer conjugates can be studied in vitro under conditions simulating the lysosomal environment.
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| Cell Assay |
Cell-based assays for HPMA copolymers involve treating cells with drug-loaded polymer conjugates and measuring cellular uptake, cytotoxicity, and drug release. Cells such as macrophages, which are the target cells for Leishmania infection, are incubated with HPMA copolymer-drug conjugates. The uptake of the polymer is assessed by fluorescence microscopy or flow cytometry, and drug efficacy is measured by the reduction of intracellular parasites.
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| Animal Protocol |
In vivo animal studies for HPMA copolymer-drug conjugates are conducted in mouse models of visceral leishmaniasis. Mice are infected with Leishmania donovani or other Leishmania species, and then treated with HPMA copolymer-drug conjugates at doses such as 5 mg/kg. Endpoints include parasite burden in the liver and spleen, as well as assessment of toxicity and pharmacokinetics.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of HPMA copolymers depend on their molecular weight and structure. The polymers are designed to have a long circulation time and to accumulate in tissues with leaky vasculature, such as tumors and inflamed tissues. HPMA copolymers are water-soluble and biocompatible. The monomer HPMA has a molecular weight of 143.18 g/mol and a molecular formula of C7H13NO2. For storage, the compound should be kept under appropriate conditions to prevent polymerization.
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| Toxicity/Toxicokinetics |
Toxicological data for HPMA and its copolymers indicate that they are biocompatible and have low toxicity. HPMA copolymers have been extensively studied as drug delivery vehicles and are generally well-tolerated. The polymers are non-immunogenic and do not cause significant adverse effects at therapeutic doses. For research use only, not for therapeutic or human use.
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| References |
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| Additional Infomation |
See also: Muretecan (monomer).
HPMA (CAS# 21442-01-3) is a hydrophilic vinyl monomer used as the building block for poly(HPMA) macromolecular carriers and hydrogels. HPMA copolymer-drug conjugates with lysosomally degradable side chains have demonstrated significant antileishmanial activity (>99% inhibition) in vivo at 5 mg/kg. The polymer is used for targeted delivery of antileishmanial agents in visceral leishmaniasis. The compound has a molecular weight of 143.18 g/mol and a molecular formula of C7H13NO2. |
| Molecular Formula |
C₇H₁₃NO₂
|
|---|---|
| Molecular Weight |
143.18
|
| Exact Mass |
143.095
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| CAS # |
21442-01-3
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| Related CAS # |
40704-75-4
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| PubChem CID |
38622
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| Appearance |
White to off-white solid powder
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| Density |
1.002g/cm3
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| Boiling Point |
321.2ºC at 760mmHg
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| Melting Point |
70 °C
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| Flash Point |
148.1ºC
|
| Vapour Pressure |
2.43E-05mmHg at 25°C
|
| Index of Refraction |
1.46
|
| LogP |
0.45
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
10
|
| Complexity |
143
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CC(C(NCC(O)C)=O)=C
|
| InChi Key |
OKPYIWASQZGASP-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C7H13NO2/c1-5(2)7(10)8-4-6(3)9/h6,9H,1,4H2,2-3H3,(H,8,10)
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| Chemical Name |
N-(2-hydroxypropyl)-2-methylprop-2-enamide
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| Synonyms |
N(2Hydroxypropyl)methacrylamide; N (2 Hydroxypropyl)methacrylamide
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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 (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) |
DMSO : ~100 mg/mL (~698.42 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (17.46 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 (17.46 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: ≥ 2.5 mg/mL (17.46 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 | 6.9842 mL | 34.9211 mL | 69.8422 mL | |
| 5 mM | 1.3968 mL | 6.9842 mL | 13.9684 mL | |
| 10 mM | 0.6984 mL | 3.4921 mL | 6.9842 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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