UAMC-3203 HCl (also known as UAMC3203 hydrochloride) is a novel, potent, and selective Ferroptosis inhibitor (IC50 value =12 nM) with higher solublility and anti-inflammatory/antioxidant effects. Ferroptosis is a nonapoptotic, iron-catalyzed form of controlled necrosis that causes oxidative lipid damage to cell membranes and can be stopped by the antioxidant ferrostatin-1 (Fer-1). Despite having solubility problems, new inhibitors derived from the Fer-1 scaffold effectively inhibited ferroptosis. After daily injections of UAMC-3203 for 4 weeks, no toxic effects were seen in mice. According to the current understanding of these compounds' mechanisms of action, UAMC-3203 integrates quickly into a phospholipid bilayer in silico. In conclusion, these analogs outperform Fer-1 in terms of properties, exhibit efficacy in vivo, and represent novel lead compounds with therapeutic potential in pertinent ferroptosis-driven disease models.
Physicochemical Properties
| Molecular Formula | C25H38CLN5O2S |
| Molecular Weight | 508.119523525238 |
| Exact Mass | 507.243 |
| Elemental Analysis | C, 59.10; H, 7.54; Cl, 6.98; N, 13.78; O, 6.30; S, 6.31 |
| CAS # | 2271358-65-5 |
| Related CAS # | UAMC-3203;2271358-64-4 |
| PubChem CID | 137701964 |
| Appearance | White to off-white solid powder |
| Hydrogen Bond Donor Count | 5 |
| Hydrogen Bond Acceptor Count | 7 |
| Rotatable Bond Count | 10 |
| Heavy Atom Count | 34 |
| Complexity | 652 |
| Defined Atom Stereocenter Count | 0 |
| InChi Key | WBZHHIZXEXJBSM-UHFFFAOYSA-N |
| InChi Code | InChI=1S/C25H37N5O2S.ClH/c31-33(32,28-15-18-30-16-13-26-14-17-30)23-11-12-24(29-22-9-5-2-6-10-22)25(19-23)27-20-21-7-3-1-4-8-21;/h1,3-4,7-8,11-12,19,22,26-29H,2,5-6,9-10,13-18,20H2;1H |
| Chemical Name | 3-(benzylamino)-4-(cyclohexylamino)-N-(2-piperazin-1-ylethyl)benzenesulfonamide;hydrochloride |
| Synonyms | UAMC3203; UAMC-3203 HCl; UAMC 3203; UAMC-3203 hydrochloride; UAMC-3203 HCl |
| HS Tariff Code | 2934.99.03.00 |
| 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 and light. |
| Shipping Condition | Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs) |
Biological Activity
| Targets | Ferroptosis (IC50 = 12 nM) |
| ln Vivo | Repeated injection of UAMC-3203 (20μ mol/kg; Injected intraperitoneally; After daily, over a period of 4 weeks), no toxic reaction was observed in mice [1]. |
| References |
[1]. Discovery of Novel, Drug-Like Ferroptosis Inhibitors with in Vivo Efficacy. J Med Chem. 2018 Nov 21;61(22):10126-10140. |
Solubility Data
| Solubility (In Vitro) | DMSO: ~50 mg/mL (~98.4 mM) |
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.09 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 (4.09 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. Solubility in Formulation 3: ≥ 2.08 mg/mL (4.09 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9680 mL | 9.8402 mL | 19.6804 mL | |
| 5 mM | 0.3936 mL | 1.9680 mL | 3.9361 mL | |
| 10 mM | 0.1968 mL | 0.9840 mL | 1.9680 mL |