| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
SRS16-86 targets ferroptosis, a form of regulated cell death characterized by iron-dependent lipid peroxidation. As a ferrostatin, it inhibits lipid peroxidation and prevents the execution of ferroptosis. Its mechanism involves scavenging lipid peroxyl radicals and preventing the accumulation of toxic lipid peroxides, thereby protecting cells from ferroptotic death.
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| ln Vitro |
In both the presence and absence of erastin, SRS16-86 (1 μM) reduces ferroptosis in HT-1080 cells and NIH 3T3 cells for a duration of 24 hours [2].
In vitro, SRS16-86 inhibits ferroptosis induced by erastin in HT-1080 and NIH3T3 cells at a concentration of 1 μM. It is a more potent inhibitor of ferroptosis compared to Ferrostatin-1. These results demonstrate its efficacy in preventing ferroptotic cell death in various cell types. |
| ln Vivo |
Mice treated with SRS16-86 (intraperitoneal injection, 2 mg/kg; 15 minutes prior to surgery) are protected against both structural organ damage and functional acute renal failure after ischemia-reperfusion injury (IRI) [2]. When it came to avoiding renal IRI, SRS16-86 (ip; 2 mg/kg; 4 weeks) in combination with [Nec-1+SfA] was more effective than [Nec-1+SfA] dual therapy. In the plasma of IRI mice models, the addition of SRS16-86 can lower serum urea and serum creatinine levels [2]. Rats with spinal cord injuries who receive an intraperitoneal injection of SRS16-86 (15 mg/kg, once daily for seven days) had reduced levels of inflammatory adhesion factors and pro-inflammatory cytokines in their injured spinal cords [3].
In vivo, SRS16-86 prevents renal tubular damage and increases in serum levels of urea and creatinine in a mouse model of renal ischemia-reperfusion injury (IRI). It also alleviates astrogliosis and enhances neuronal survival after spinal cord injury (SCI). The compound decreases inflammatory cytokine levels, such as IL-1, TNF, and ICAM-1, after SCI. |
| Enzyme Assay |
The in vitro assay for SRS16-86 involves measuring its ability to inhibit ferroptosis. This is typically done using cell-based assays where ferroptosis is induced by erastin in HT-1080 or NIH3T3 cells. Cell viability is measured to determine the compound's protective effect. The concentration of 1 μM is commonly used.
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| Cell Assay |
Cellular assays for SRS16-86 are performed using HT-1080 and NIH3T3 cells. Ferroptosis is induced with erastin, and the compound's ability to prevent cell death is assessed. Cell viability is measured using standard assays such as MTT or CellTiter-Glo.
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| Animal Protocol |
Animal/Disease Models: Renal IRI model
Doses: 2 mg/kg; 15 min before the onset of surgery Route of Administration: intraperitoneal (ip)injection; 2 mg/kg; 15 min before the onset of surgery Experimental Results: Was protective from renal IRI. Animal/Disease Models: Renal IRI model Doses: 2 mg/kg Route of Administration: Combination with Necrostatin-1/Sanglifehrin A; 2 mg/kg; 4 weeks Experimental Results: Further increased the protective effect of [Necrostatin-1/Sanglifehrin A] combination therapy in renal IRI model. In vivo animal protocols for SRS16-86 involve mouse models of renal ischemia-reperfusion injury (IRI) and spinal cord injury (SCI). The compound is administered, and its effects on tissue damage, inflammation, and functional recovery are assessed. These studies provide preclinical evidence for its therapeutic potential. |
| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties of SRS16-86 are improved compared to Ferrostatin-1. It is more metabolically and plasma stable. This enhanced stability is important for in vivo applications and contributes to its efficacy in preclinical models.
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| Toxicity/Toxicokinetics |
Toxicity data for SRS16-86 are limited. As a ferroptosis inhibitor, it is expected to be well-tolerated. However, comprehensive toxicological studies are needed. The compound is intended for research use only and is not approved for human therapeutic use.
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| References |
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| Additional Infomation |
SRS16-86 is an ethyl ester formed by the condensation of the carboxyl group of 4-[(adamantane-1-yl)amino]-3-{(Z)-[(pyrimidin-5-yl)methylene]amino}benzoic acid with tert-butanol. At a concentration of 1 μM, it inhibits erastin-induced ferroptosis in HT-1080 and NIH3T3 cells. It is a ferroptosis inhibitor. SRS16-86 belongs to the tert-butyl ester, adamantane group, pyrimidine group, substituted aniline, secondary amine, and imine group.
SRS16-86 is a potent ferroptosis inhibitor and third-generation ferrostatin. It is more stable and potent than Ferrostatin-1. The compound has shown efficacy in preclinical models of renal ischemia-reperfusion injury and spinal cord injury. It is used as a research tool for studying ferroptosis and is not currently in clinical trials. |
| Molecular Formula |
C26H32N4O2
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|---|---|
| Molecular Weight |
432.56
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| Exact Mass |
432.252
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| CAS # |
1793052-96-6
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| PubChem CID |
91801200
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| Appearance |
Yellow to orange solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
614.9±55.0 °C at 760 mmHg
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| Flash Point |
325.7±31.5 °C
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| Vapour Pressure |
0.0±1.8 mmHg at 25°C
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| Index of Refraction |
1.656
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| LogP |
4.93
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
32
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| Complexity |
668
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(C)(C)OC(=O)C1=CC(=C(C=C1)NC23CC4CC(C2)CC(C4)C3)N=CC5=CN=CN=C5
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| InChi Key |
DFENTOUMMDWZAF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C26H32N4O2/c1-25(2,3)32-24(31)21-4-5-22(23(9-21)29-15-20-13-27-16-28-14-20)30-26-10-17-6-18(11-26)8-19(7-17)12-26/h4-5,9,13-19,30H,6-8,10-12H2,1-3H3
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| Chemical Name |
tert-butyl 4-(1-adamantylamino)-3-(pyrimidin-5-ylmethylideneamino)benzoate
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : 33.33 mg/mL (77.05 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.78 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. Solubility in Formulation 2: 2.5 mg/mL (5.78 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 ultrasonication. 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 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: ≥ 0.83 mg/mL (1.92 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 | 2.3118 mL | 11.5591 mL | 23.1182 mL | |
| 5 mM | 0.4624 mL | 2.3118 mL | 4.6236 mL | |
| 10 mM | 0.2312 mL | 1.1559 mL | 2.3118 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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