| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
|
||
| 500mg | |||
| Other Sizes |
| Targets |
Lysyl hydroxylase 2 (LH2)
|
|---|---|
| ln Vitro |
The compound displays an IC50 value of approximately 300 nM against lysyl hydroxylase 2. It demonstrates excellent selectivity for LH2 over the other family members LH1 and LH3, which minimizes potential off-target effects on other collagen hydroxylation enzymes.
|
| ln Vivo |
No detailed in vivo activity data is available in standard databases. As a research tool for studying collagen remodeling, its in vivo efficacy requires evaluation in relevant fibrosis or cancer metastasis animal models.
|
| Enzyme Assay |
The in vitro enzyme activity assay uses recombinant LH2 enzyme. Compound is incubated with purified LH2 and its substrate procollagen lysine. Activity is measured by LC-MS quantification of hydroxylysine formation, comparing levels between treated and control groups.
|
| Cell Assay |
No specific cell-based assay protocol is documented. Standard cell protocols could involve culturing fibroblasts or cancer cells with varying compound concentrations, then measuring cellular lysyl hydroxylase activity by detecting hydroxylysine levels in secreted collagen.
|
| Animal Protocol |
Animal studies likely involve mouse models of tumor metastasis or lung fibrosis. Mice receive compound at specified doses via oral gavage or intraperitoneal injection. Endpoints include tissue hydroxylysine levels, collagen cross-linking, and pathological assessment.
|
| ADME/Pharmacokinetics |
Comprehensive PK data is not publicly available. As a selective enzyme inhibitor, it is expected to have moderate stability and oral bioavailability typical of small molecule hydroxylase inhibitors for preclinical research.
|
| Toxicity/Toxicokinetics |
Limited toxicology data exists. Based on its selectivity profile, it is predicted to have an acceptable safety margin compared to pan-hydroxylase inhibitors, though comprehensive toxicity studies would be required for clinical development.
|
| References | |
| Additional Infomation |
This compound is an active biochemical for research use, specifically developed to study LH2 function in collagen biology, fibrosis, and cancer metastasis. It has not been approved for human therapeutic use.
|
| Molecular Formula |
C18H18N2O3
|
|---|---|
| Molecular Weight |
310.35
|
| Appearance |
Light yellow to yellow solid powder
|
| SMILES |
O=C(C1=CC=CC(N2CCOCC2)=C1)CC(C3=CC=NC=C3)=O
|
| 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)
|
| Solubility (In Vitro) |
DMSO: ~50 mg/mL (~161.1 mM; with ultrasonication)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.06 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 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 DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and 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 (8.06 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 DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2222 mL | 16.1108 mL | 32.2217 mL | |
| 5 mM | 0.6444 mL | 3.2222 mL | 6.4443 mL | |
| 10 mM | 0.3222 mL | 1.6111 mL | 3.2222 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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