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| Targets |
STS-E412 is a selective activator of the tissue-protective erythropoietin (EPO) receptor, targeting both EPOR and CD131. It is a first-in-class nonpeptidyl activator of the EPOR/CD131 heterodimer. By activating these receptors, STS-E412 modulates signaling pathways involved in tissue protection and neuroprotection. The compound's mechanism of action involves the activation of tissue-protective EPO receptors, which are distinct from the erythropoietic EPO receptors. This selective activation provides tissue-protective effects without stimulating erythropoiesis.
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| ln Vitro |
In vitro, STS-E412 is a selective activator of tissue-protective EPO receptors, including EPOR and CD131. It demonstrates significant biological activity in protecting neural tissues. The compound's in vitro activity is characterized by potent activation of EPOR/CD131 signaling pathways. STS-E412 is used as a research tool to study the tissue-protective effects of EPO receptor activation.
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| ln Vivo |
In vivo, STS-E412 can be used for research of neurodegenerative diseases and organ protection. It demonstrates significant biological activity in protecting neural tissues and enhancing organ resilience. As a selective activator of tissue-protective EPO receptors, it may provide therapeutic benefits in conditions such as stroke, traumatic brain injury, and neurodegenerative diseases. However, detailed in vivo efficacy data for specific disease models are limited. STS-E412 is primarily used as a research tool.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for STS-E412 typically involve measuring its binding to EPOR and CD131 receptors. The compound is a selective activator of these receptors. Binding assays can be performed using surface plasmon resonance (SPR) or radioligand binding techniques. These assays confirm the compound's mechanism of action as an EPOR/CD131 receptor activator.
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| Cell Assay |
In vitro cellular assays for STS-E412 typically involve treating cells expressing EPOR and CD131 with the compound and measuring downstream signaling events, such as STAT5 phosphorylation or other tissue-protective signaling pathways. The compound activates these receptors and triggers tissue-protective signaling. These cell-based studies demonstrate the compound's functional activity as an EPOR/CD131 receptor activator.
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| Animal Protocol |
In vivo animal models for STS-E412 may include models of neurodegenerative diseases, stroke, or organ injury. The compound is administered by appropriate routes, and tissue protection or functional recovery is assessed. STS-E412 demonstrates significant biological activity in protecting neural tissues and enhancing organ resilience. However, detailed animal protocol information for STS-E412 is limited in the available literature. The compound is primarily used as a research tool.
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| ADME/Pharmacokinetics |
STS-E412 has a molecular formula of C15H15ClN4O2 and a molecular weight of 318.76 g/mol. The compound is typically stored under appropriate conditions to maintain stability. Its physicochemical properties support its use in both in vitro and in vivo studies. STS-E412's solubility and formulation for administration should be optimized based on specific experimental requirements. The compound is a first-in-class nonpeptidyl activator of the EPOR/CD131 heterodimer.
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| Toxicity/Toxicokinetics |
STS-E412 is a selective activator of tissue-protective EPO receptors with a well-characterized mechanism of action. As with any drug, potential toxicity may include effects on the hematopoietic system or other organ systems. The compound's safety profile should be evaluated in preclinical toxicology studies. STS-E412 is for research use only and is not approved for human therapeutic use. It represents a valuable tool for studying tissue-protective EPO receptor signaling.
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| References | |
| Additional Infomation |
EPO receptor activator; structure can be found in the first article.
STS-E412 (CAS# 1609980-39-3) is a selective activator of the tissue-protective erythropoietin (EPO) receptor, targeting both EPOR and CD131. It is a first-in-class nonpeptidyl activator of the EPOR/CD131 heterodimer. STS-E412 demonstrates significant biological activity in protecting neural tissues and enhancing organ resilience. It can be used for research of neurodegenerative diseases and organ protection. The compound is for research use only and is not approved for human therapeutic use. |
| Molecular Formula |
C15H15CLN4O2
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|---|---|
| Molecular Weight |
318.76
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| Exact Mass |
318.088
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| CAS # |
1609980-39-3
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| PubChem CID |
73891137
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Index of Refraction |
1.638
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| LogP |
3.55
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
22
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| Complexity |
354
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=CC(=NC2=NC(=NN12)OCCOC3=CC=C(C=C3)Cl)C
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| InChi Key |
XQFMOBKQELKMKF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H15ClN4O2/c1-10-9-11(2)20-14(17-10)18-15(19-20)22-8-7-21-13-5-3-12(16)4-6-13/h3-6,9H,7-8H2,1-2H3
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| Chemical Name |
2-[2-(4-chlorophenoxy)ethoxy]-5,7-dimethyl-[1,2,4]triazolo[1,5-a]pyrimidine
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| Synonyms |
STSE412; STS E412; STS-E412
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1372 mL | 15.6858 mL | 31.3716 mL | |
| 5 mM | 0.6274 mL | 3.1372 mL | 6.2743 mL | |
| 10 mM | 0.3137 mL | 1.5686 mL | 3.1372 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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