| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 100mg | |||
| Other Sizes |
| Targets |
HO-1-IN-1 hydrochloride targets heme oxygenase 1 (HO-1), an inducible enzyme that plays a key role in maintaining cellular redox balance and protecting cells from oxidative stress. HO-1 catalyzes the degradation of heme to produce carbon monoxide (CO), biliverdin, and free iron. By inhibiting HO-1, the compound modulates cellular oxidative stress responses and inflammatory pathways.
|
|---|---|
| ln Vitro |
In vitro, HO-1-IN-1 hydrochloride (10 uM; 4 hours) attenuates GRIM-19 deficiency-induced NF-kappaB activation and p65 nuclear translocation in GES-1 cells. At concentrations of 5-10 uM for 6 hours, it significantly attenuates GRIM-19 deficiency-driven gastric cancer cell migration and invasion, and downregulates metastasis-associated gene expressions including HIF-1alpha, COX-2, VEGF-A, VEGF-C, MMP-9, and BACH-1.
|
| ln Vivo |
In vivo activity data for HO-1-IN-1 hydrochloride are limited, as it is primarily used as a research tool in cell-based studies. The compound is expected to modulate HO-1 activity in animal models, affecting oxidative stress and inflammatory responses. Studies using HO-1 inhibitors in vivo typically involve administration via intraperitoneal or oral routes to investigate the role of HO-1 in various disease models.
|
| Enzyme Assay |
In vitro enzyme inhibition assays for HO-1-IN-1 hydrochloride are performed using purified recombinant HO-1 enzyme or tissue homogenates rich in HO-1 activity. The compound is incubated with hemin substrate and NADPH-cytochrome P450 reductase at varying concentrations (0.01-10 uM). HO-1 activity is measured spectrophotometrically by monitoring biliverdin production at 460 nm, and IC₅0 values are determined from dose-response curves.
|
| Cell Assay |
Cellular assays for HO-1-IN-1 hydrochloride are conducted using cell lines such as GES-1 gastric epithelial cells or cancer cell lines. Cells are treated with the compound at concentrations of 5-10 uM for 4-6 hours. NF-kappaB activation is assessed by measuring p65 nuclear translocation via immunofluorescence or Western blot. Cell migration and invasion are evaluated using Transwell assays, and gene expression is analyzed by RT-qPCR.
|
| Animal Protocol |
In vivo protocols for HO-1-IN-1 hydrochloride typically involve administration in rodent models via intraperitoneal injection or oral gavage at doses determined from pharmacokinetic studies. Standard endpoints include assessment of oxidative stress markers (MDA, ROS), inflammatory cytokines (IL-6, TNF-alpha), and tissue histopathology. Dosing schedules and routes are optimized based on the specific disease model being investigated.
|
| ADME/Pharmacokinetics |
Pharmacokinetic data for HO-1-IN-1 hydrochloride are limited. As a small-molecule inhibitor, it is expected to have moderate bioavailability and tissue distribution. The compound's solubility in DMSO and other solvents supports in vitro and in vivo formulations. For in vivo use, formulations are typically prepared using DMSO, PEG300, Tween 80, and saline to achieve appropriate concentrations for administration.
|
| Toxicity/Toxicokinetics |
Toxicological information for HO-1-IN-1 hydrochloride is not extensively characterized. As with most research compounds, standard safety assessments include evaluation of cytotoxicity in cell-based assays at concentrations used for pharmacological studies. No significant acute toxicity has been reported at the concentrations used in vitro (5-10 uM). The compound is for research use only and not for human therapeutic applications.
|
| References |
|
| Additional Infomation |
HO-1-IN-1 hydrochloride is a research-use compound not approved for clinical therapeutic applications. It is a valuable tool for studying the role of HO-1 in oxidative stress, inflammation, cancer, and apoptosis. The compound is used to investigate the therapeutic potential of HO-1 modulation in various diseases, including gastric cancer, where HO-1 inhibition has shown anti-metastatic effects.
|
| Molecular Formula |
C13H16BRCLN2
|
|---|---|
| Molecular Weight |
315.636541366577
|
| Exact Mass |
314.018
|
| CAS # |
1092851-70-1
|
| Related CAS # |
Heme Oxygenase-1-IN-1;1093058-52-6
|
| PubChem CID |
66678516
|
| Appearance |
Light yellow to yellow solid powder
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
1
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
17
|
| Complexity |
190
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
BrC1C=CC(=CC=1)CCCCN1C=NC=C1.Cl
|
| InChi Key |
IUTCFFFBKPGSJF-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C13H15BrN2.ClH/c14-13-6-4-12(5-7-13)3-1-2-9-16-10-8-15-11-16;/h4-8,10-11H,1-3,9H2;1H
|
| Chemical Name |
1-[4-(4-bromophenyl)butyl]imidazole;hydrochloride
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~396.02 mM)
H2O : ~100 mg/mL (~316.82 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.59 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 (6.59 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 (6.59 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 (316.82 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 | 3.1682 mL | 15.8408 mL | 31.6817 mL | |
| 5 mM | 0.6336 mL | 3.1682 mL | 6.3363 mL | |
| 10 mM | 0.3168 mL | 1.5841 mL | 3.1682 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.