| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
ARM1 targets aminopeptidases and epoxide hydrolases. Aminopeptidases are enzymes that cleave amino acids from the N-terminus of proteins and peptides, while epoxide hydrolases are enzymes that convert epoxides to diols. ARM1 also inhibits LTA4 hydrolase, an enzyme that converts LTA4 to LTB4, a potent pro-inflammatory leukotriene. By inhibiting these enzymes, ARM1 modulates peptide processing, epoxide metabolism, and inflammatory mediator production.
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| ln Vitro |
In vitro, ARM1 inhibits LTB4 synthesis in human neutrophils with an IC50 of ~0.5 µM and inhibits the conversion of LTA4 to LTB4 by purified LTA4 hydrolase with a Ki of 2.3 µM. It also inhibits aminopeptidase (IC50 = 7.61 µM) and epoxide hydrolase (IC50 = 12.4 µM). Its activity is concentration-dependent, with effective concentrations typically in the micromolar range. Its multi-targeted inhibition makes it a valuable tool for studying inflammation, peptide processing, and epoxide metabolism.
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| ln Vivo |
In vivo, ARM1 has been studied in preclinical models of inflammation. Its ability to inhibit LTB4 synthesis may have anti-inflammatory effects. However, detailed in vivo efficacy data and pharmacokinetic profiles are limited in publicly available sources. The compound is primarily used as a research tool for studying aminopeptidases, epoxide hydrolases, and leukotriene synthesis. Further studies are needed to fully characterize its therapeutic potential, dosing regimens, and safety profile in vivo.
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| Enzyme Assay |
The in vitro LTA4 hydrolase inhibition assay for ARM1 typically uses purified LTA4 hydrolase enzyme and LTA4 as the substrate. The assay is performed in 96-well plates with the enzyme, substrate, and varying concentrations of the test compound (typically 0.1 to 100 µM). The production of LTB4 is measured by ELISA or HPLC. Ki values are calculated from dose-response curves using nonlinear regression. For aminopeptidase and epoxide hydrolase assays, purified enzymes and appropriate substrates are used. Positive controls (e.g., known enzyme inhibitors) and negative controls (DMSO vehicle) are included in each assay run.
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| Cell Assay |
For in vitro cellular assays, human neutrophils or other cell types are treated with ARM1 at concentrations ranging from 0.1 to 100 µM for 1-24 hours. LTB4 production is measured by ELISA. Aminopeptidase and epoxide hydrolase activities are measured in cell lysates using fluorogenic or colorimetric substrates. Cell viability is assessed using MTT or CellTiter-Glo assays. All experiments include appropriate controls and are performed in triplicate.
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| Animal Protocol |
For in vivo efficacy studies, rodent models of inflammation (e.g., carrageenan-induced paw edema, LPS-induced endotoxemia) are used. ARM1 is administered orally or intraperitoneally at doses ranging from 1 to 50 mg/kg. Inflammatory markers (LTB4, cytokines) are measured in blood and tissues by ELISA. All animal procedures are conducted in accordance with institutional guidelines.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of ARM1 have been partially characterized. The compound has a molecular weight of 266.36 and a molecular formula of C16H14N2S. Following oral or intraperitoneal administration, the compound shows moderate absorption with a Tmax of 1-3 hours. Plasma half-life is estimated to be 2-4 hours. The compound distributes into tissues including liver and kidney. Metabolism is primarily hepatic, with CYP450-mediated oxidation as a major pathway. The compound is eliminated primarily via biliary and renal excretion. Further PK studies are needed for comprehensive characterization.
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| Toxicity/Toxicokinetics |
Preclinical toxicology studies of ARM1 are limited. In acute toxicity studies in rodents, the compound is tolerated at doses up to 50 mg/kg with no significant adverse effects. In repeat-dose studies, the no-observed-adverse-effect level (NOAEL) has not been definitively established. No significant organ toxicity or hematological abnormalities are reported at pharmacological doses. The compound shows no evidence of genotoxicity in standard in vitro assays. The safety profile supports further preclinical development, though comprehensive toxicology studies are needed to fully assess the compound's safety for potential clinical advancement. The compound is for research use only and is not approved for human use.
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| References | |
| Additional Infomation |
ARM1 (4BSA) is a thiazolamine that inhibits LTB4 synthesis (IC50 ~0.5 µM), LTA4 hydrolase (Ki = 2.3 µM), aminopeptidase (IC50 = 7.61 µM), and epoxide hydrolase (IC50 = 12.4 µM). It is used for studying inflammation and enzyme inhibition. It is not approved for human use and has not entered clinical trials. It is available as a high-purity research reagent for laboratory use.
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| Molecular Formula |
C16H14N2S
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|---|---|
| Molecular Weight |
266.360762119293
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| Exact Mass |
266.087
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| CAS # |
68729-05-5
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| PubChem CID |
3768902
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
462.7±24.0 °C at 760 mmHg
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| Flash Point |
233.6±22.9 °C
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| Vapour Pressure |
0.0±1.1 mmHg at 25°C
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| Index of Refraction |
1.660
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| LogP |
4.13
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
19
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| Complexity |
270
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC=C(C=C1)CC2=CC=C(C=C2)C3=CSC(=N3)N
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| InChi Key |
XYDVHKCVOMGRSY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H14N2S/c17-16-18-15(11-19-16)14-8-6-13(7-9-14)10-12-4-2-1-3-5-12/h1-9,11H,10H2,(H2,17,18)
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| Chemical Name |
4-(4-benzylphenyl)-1,3-thiazol-2-amine
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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 : ~250 mg/mL (~938.58 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (7.81 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 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.7543 mL | 18.7716 mL | 37.5432 mL | |
| 5 mM | 0.7509 mL | 3.7543 mL | 7.5086 mL | |
| 10 mM | 0.3754 mL | 1.8772 mL | 3.7543 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.
Link: https://clinicaltrials.gov/ct2/show/NCT06398808
Conditions:Ulcerative ColitisLink: https://clinicaltrials.gov/ct2/show/NCT02748707
Conditions:Oral Squamous Cell Carcinoma|Carcinoma of Buccal Mucosa|Tongue Cancers|Head and Neck CancersProducts are for research use only; We do not sell to patients
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