ISRACT-01
Based on 1 Customer Validation
ISRACT-01 is an integrated stress response (ISR) activator. ISRACT-01 has a Kd of 557 nM for eIF2BΔ-latch. ISRACT-01 cooperates with eIF2-P to inhibit guanine nucleotide exchange factor (GEF) activity by specifically binding to and stabilizing the inactive conformation (I-state) of eIF2B. ISRACT-01 can be used in studies related to amyotrophic lateral sclerosis.
For research use only. We do not sell to patients.
- Formula: C30H32Cl2N2O4
- Molecular Weight:555.49
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
eIF2BΔ-latch 557 nM (Kd) |
In Vitro
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BJ fibroblasts
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Concentration:2.4 μM (pre-incubation concentration 3 μM)
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Incubation Time:Pre-incubated for 4 h, recorded over 5 days
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Result:Protected the cells from tunicamycin-induced apoptosis.
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Cell Line:Wild-type mouse embryonic fibroblasts (MEFs, Eif2s1 S51/S51)
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Concentration:2 μM, 10 μM
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Incubation Time:3 h
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Result:Significantly increased the expression level of ATF4 protein.
Chemical Information
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Molecular Weight 555.49
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Formula C30H32Cl2N2O4
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SMILES
O=C(CCOC1=CC=C(Cl)C=C1)N[C@H]2CC[C@H](N(CC3=CC=CC=C3)C(COC4=CC=C(Cl)C=C4)=O)CC2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (180.02 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.50 mM); Suspended solution
This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8002 mL | 9.0011 mL | 18.0021 mL | 45.0053 mL |
| 5 mM | 0.3600 mL | 1.8002 mL | 3.6004 mL | 9.0011 mL | |
| 10 mM | 0.1800 mL | 0.9001 mL | 1.8002 mL | 4.5005 mL | |
| 15 mM | 0.1200 mL | 0.6001 mL | 1.2001 mL | 3.0004 mL | |
| 20 mM | 0.0900 mL | 0.4501 mL | 0.9001 mL | 2.2503 mL | |
| 25 mM | 0.0720 mL | 0.3600 mL | 0.7201 mL | 1.8002 mL | |
| 30 mM | 0.0600 mL | 0.3000 mL | 0.6001 mL | 1.5002 mL | |
| 40 mM | 0.0450 mL | 0.2250 mL | 0.4501 mL | 1.1251 mL | |
| 50 mM | 0.0360 mL | 0.1800 mL | 0.3600 mL | 0.9001 mL | |
| 60 mM | 0.0300 mL | 0.1500 mL | 0.3000 mL | 0.7501 mL | |
| 80 mM | 0.0225 mL | 0.1125 mL | 0.2250 mL | 0.5626 mL | |
| 100 mM | 0.0180 mL | 0.0900 mL | 0.1800 mL | 0.4501 mL |