| Size | Price | Stock | Qty |
|---|---|---|---|
| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| Other Sizes |
Purity: ≥98%
| Targets |
HX-1171 targets reactive oxygen species (ROS) and lipid peroxidation.
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| ln Vitro |
Treatment of PC12 cells with HTHQ (0-100 μM; 24 hours) enhances cell viability in a dose-dependent manner [1]. HTHQ (10 μM; 0.6-24 hours; PC12 cells) suppresses p38 mitogen activation Phosphorylation of protein kinase (MAPK), c-Jun N-terminal kinase (JNK1/2), and 3,4-L-dihydroxyphenylalanine (L-DOPA)-induced sustained extracellular signal-regulated kinase (ERK1/2). Additionally, HTHQ promotes cell viability by normalizing Bcl-2-associated X protein (Bax) expression and Bcl-2-associated death protein (Bad) phosphorylation that have been decreased by L-DOPA [1].
In vitro, HX-1171 is a potent anti-lipid-peroxidative compound. It attenuates interleukin-1beta-induced iNOS protein expression in cultured hepatocytes, with potency 10 times higher than that of vitamin E. It functions as a direct-acting radical scavenger. |
| ln Vivo |
Serum chemistry levels and liver weights of male Sprague Dawley rats (specific pathogen-free) considerably improved after 4 weeks of oral HTHQ treatment (50-200 mg/kg). Malondialdehyde and hydroxyproline levels in the liver are lowered by HTHQ. Fibrotic septa are also decreased by HTHQ therapy. When HTHQ was administered to mice with DMN-induced liver fibrosis, the amount of mRNA for TGF-β (transforming growth factor-β), α-SMA (α-smooth muscle actin), and PDGF (platelet-derived growth factor) in the liver tissue decreased[2].
In vivo, HX-1171 has shown potential for the treatment of hepatic fibrosis. Its antioxidant activity is elevated in biological systems, such as liver microsomes, via the generation of stable free radicals. |
| Enzyme Assay |
In vitro enzyme assays for HX-1171 typically involve measuring its ability to inhibit lipid peroxidation. This is commonly done using rat liver microsomes or other lipid-rich preparations. The compound is incubated with the microsomes and an inducer of lipid peroxidation (e.g., Fe²⁺/ascorbate or NADPH). The formation of malondialdehyde (MDA), a byproduct of lipid peroxidation, is measured using the thiobarbituric acid (TBA) assay.
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: PC12 Cell Tested Concentrations: 0 μM, 1 μM, 10 μM and 100 μM Incubation Duration: 24 hrs (hours) Experimental Results: The significant decrease in cell viability induced by 100 and 200 μM L-DOPA at 24 hrs (hours) was attenuated. Western Blot Analysis[1] Cell Types: PC12 Cell Tested Concentrations: 10 μM Incubation Duration: 0.6-24 hrs (hours) Experimental Results: Inhibition of L-DOPA-induced sustained extracellular signal-regulated kinase (ERK1/2), p38 mitogen-activated protein kinase Phosphorylation (MAPK) and c-Jun N-terminal kinase (JNK1/2). And also normalized the diminished Bcl-2-associated death protein (Bad) phosphorylation and Bcl-2-associated X protein (Bax) expression by L-DOPA. In vitro cellular assays for HX-1171 are performed using cultured hepatocytes. Cells are pre-treated with the compound and then stimulated with interleukin-1beta (IL-1β) to induce iNOS expression. The level of iNOS protein is measured by Western blot, and nitric oxide (NO) production is measured by the Griess assay to assess the compound's anti-inflammatory and antioxidant effects. |
| Animal Protocol |
Animal/Disease Models: 48 specific pathogen-free male Sprague Dawley (SD) rats (6 weeks old) were given dimethylnitrosamine (DMN) [2]
Doses: 50 mg/kg, 100 mg/kg, 200 mg /kg Doses: po (po (oral gavage)) lasted for 4 weeks. Experimental Results: Improved DMN-induced liver fibrosis in male SD rats. In vivo animal studies for HX-1171 are conducted in rodent models of hepatic fibrosis. The compound is administered orally or intraperitoneally, and liver fibrosis is induced by agents like carbon tetrachloride (CCl4) or bile duct ligation. Endpoints include histological analysis of liver fibrosis, measurement of liver enzymes (ALT, AST), and assessment of oxidative stress markers. |
| ADME/Pharmacokinetics |
Pharmacokinetic data for HX-1171 are limited. The compound has advanced to Phase I clinical evaluation for safety and pharmacokinetic assessment in healthy male subjects (NCT01548391). This indicates that its PK profile has been characterized to some extent.
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| Toxicity/Toxicokinetics |
Toxicological data for HX-1171 are not detailed in publicly available sources. As a compound that has entered Phase I clinical trials, it would have undergone preclinical safety assessments. No significant toxicity has been reported in the available literature.
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| References |
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| Additional Infomation |
Hx 1171 is being investigated in the clinical trial NCT01548391 (a Phase I clinical study of the safety, tolerability and pharmacokinetics of HX-1171 in healthy male subjects).
HX-1171, also known as HTHQ (1-O-Hexyl-2,3,5-trimethylhydroquinone), is a potent antioxidant and lipid peroxidation inhibitor. It has been investigated for the treatment of hepatic fibrosis and has advanced to Phase I clinical trials (NCT01548391). Its development status is not fully detailed. |
| Molecular Formula |
C15H24O2
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|---|---|
| Molecular Weight |
236.355
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| Exact Mass |
236.177
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| CAS # |
148081-72-5
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| Related CAS # |
148081-72-5
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| PubChem CID |
119193
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| Appearance |
White to off-white solid powder
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| Density |
0.971g/cm3
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| Boiling Point |
357.8ºC at 760mmHg
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| Melting Point |
72.5-73ºC
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| Flash Point |
154.4ºC
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| Vapour Pressure |
1.29E-05mmHg at 25°C
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| Index of Refraction |
1.507
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| LogP |
3.609
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
17
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| Complexity |
205
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
ATMNQRRJNBCQJO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H24O2/c1-5-6-7-8-9-17-14-10-11(2)15(16)13(4)12(14)3/h10,16H,5-9H2,1-4H3
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| Chemical Name |
4-(hexyloxy)-2,3,6-trimethylphenol
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| Synonyms |
HX-1171 HX-1171 HX-1171 HTHQ
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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 |
| 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 (~423.10 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 25 mg/mL (105.78 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 250.0 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (10.58 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (10.58 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 | 4.2308 mL | 21.1542 mL | 42.3083 mL | |
| 5 mM | 0.8462 mL | 4.2308 mL | 8.4617 mL | |
| 10 mM | 0.4231 mL | 2.1154 mL | 4.2308 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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