| Size | Price | Stock | Qty |
|---|---|---|---|
| 500mg |
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| 1g |
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| 2g | |||
| 5g | |||
| Other Sizes |
Purity: ≥98%
| Targets |
Hexaminolevulinate targets the heme biosynthesis pathway. It is converted to protoporphyrin IX (PpIX), a photosensitizer, in cells. PpIX accumulates preferentially in cancer cells due to their altered metabolism. Upon illumination with blue light, PpIX fluoresces, allowing for the visualization of cancerous lesions. Upon illumination with red light, PpIX generates reactive oxygen species, leading to cell death.
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|---|---|
| ln Vitro |
In vitro, Hexaminolevulinate is converted to protoporphyrin IX (PpIX) in cancer cells. PpIX accumulation is higher in cancer cells than in normal cells, allowing for selective detection. The compound's activity is measured by assessing PpIX fluorescence in cell cultures. It is used to study photodynamic diagnosis and therapy.
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| ln Vivo |
In vivo, Hexaminolevulinate is used for photodynamic diagnosis of bladder cancer. It is administered intravesically, and after a period of incubation, the bladder is illuminated with blue light. Cancerous lesions fluoresce red, allowing for their visualization and biopsy. It is also being studied for photodynamic therapy of other cancers.
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| Enzyme Assay |
In vitro PpIX accumulation assays for Hexaminolevulinate involve incubating cells with the compound and measuring PpIX fluorescence using a fluorometer or flow cytometer. Cells are treated with varying concentrations of Hexaminolevulinate for several hours, and PpIX fluorescence is measured. The selectivity of PpIX accumulation in cancer cells versus normal cells is assessed.
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| Cell Assay |
In vitro cell-based assays for Hexaminolevulinate are performed using cancer cell lines. Cells are cultured in appropriate media and treated with Hexaminolevulinate at various concentrations. PpIX accumulation is measured by fluorescence microscopy or flow cytometry. Cell viability is assessed by MTT assays following illumination to assess phototoxicity.
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| Animal Protocol |
In vivo animal studies for Hexaminolevulinate are conducted in models of bladder cancer or other tumors. The compound is administered intravesically or systemically, and PpIX fluorescence is measured in tumor tissue. The efficacy of photodynamic diagnosis or therapy is assessed by tumor detection rates or tumor growth inhibition.
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| ADME/Pharmacokinetics |
Hexaminolevulinate is administered intravesically for bladder cancer diagnosis. It is absorbed by the bladder mucosa and converted to PpIX in cells. PpIX accumulates in cancer cells and is eliminated over time. The compound is metabolized in the liver and excreted primarily in urine.
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| Toxicity/Toxicokinetics |
Hexaminolevulinate is generally well-tolerated when used for photodynamic diagnosis. Local side effects may include bladder irritation, hematuria, and discomfort. Systemic toxicity is rare due to limited absorption. It is contraindicated in patients with porphyria or known hypersensitivity to the compound.
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| References |
BJU Int.2016 Jun;117(6B):E102-13.
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| Additional Infomation |
Hexaaminolevulinate hydrochloride is the hydrochloride form of hexaaminolevulinate, a hexyl ester of the heme precursor 5-aminolevulinic acid (ALA), which possesses potential photosensitizing activity. Hexaaminolevulinate is a precursor to photosensitive porphyrins (PAPs), particularly protoporphyrin IX (PpIX), which selectively accumulates in rapidly proliferating cells, such as those in tumor tissue. When exposed to blue light, PAPs are activated and emit red light, enabling tumor imaging.
See also: Hexaaminolevulinate (with active moiety). Hexaminolevulinate HCl is a photosensitizing agent used for photodynamic diagnosis of bladder cancer. It is converted to protoporphyrin IX (PpIX) in cancer cells, which fluoresces upon illumination. It is also being studied for photodynamic therapy of various cancers. This product is for research and diagnostic use. |
| Molecular Formula |
C11H22CLNO3
|
|---|---|
| Molecular Weight |
251.7503
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| Exact Mass |
251.128
|
| CAS # |
140898-91-5
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| Related CAS # |
140898-91-5 (HCl);140898-97-1 (free);
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| PubChem CID |
6433082
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| Appearance |
White to off-white solid powder
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| Boiling Point |
313.2ºC at 760mmHg
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| Melting Point |
145 - 147 °C
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| Flash Point |
112.6ºC
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| Vapour Pressure |
0.000504mmHg at 25°C
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| LogP |
2.92
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
16
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| Complexity |
192
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
LZYXPFZBAZTOCH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C11H21NO3.ClH/c1-2-3-4-5-8-15-11(14)7-6-10(13)9-12;/h2-9,12H2,1H3;1H
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| Chemical Name |
hexyl 5-amino-4-oxopentanoate hydrochloride.
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| Synonyms |
P-1206; P1206; P1206. HAL. hexaminolevulinate; 5-Aminolevulinic acid hexyl ester; 5-ALA hexylester; Hexyl 5-aminolevulinate hydrochloride; 5-Aminolevulinic acid hexyl ester hydrochloride; US trade names: Hexvix; Cysview
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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 : ≥ 100 mg/mL (~397.22 mM)
H2O : ~100 mg/mL (~397.22 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.93 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 (9.93 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 (9.93 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (397.22 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.9722 mL | 19.8610 mL | 39.7219 mL | |
| 5 mM | 0.7944 mL | 3.9722 mL | 7.9444 mL | |
| 10 mM | 0.3972 mL | 1.9861 mL | 3.9722 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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