Icerguastat
Based on 4 publication(s) in Google Scholar
Icerguastat (Sephin1), a derivative of Guanabenz lacking the α2-adrenergic activity, is a selective inhibitor of the phosphatase regulatory subunit PPP1R15A (R15A). Icerguastat inhibits eIF2α dephosphorylation, thereby prolonging the protective response. Anti-prion effect.
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- 純度: 99.93%
- CAS 番号: 951441-04-6
- 分子式: C8H9ClN4
- 分子量:196.64
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保管条件:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 Icerguastat
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In Vivo Efficacy Study
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Histological Imaging/Staining
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In Vivo Efficacy Study
生物活性
Icerguastat (5 μM) prolongs eIF2α phosphorylation in oligodendrocytes under stress[1].
Icerguastat (Sephin1) (selective inhibitor of a holophosphatase), safely and selectively inhibits a regulatory subunit of protein phosphatase 1 in vivo. Icerguastat selectively binds and inhibits the stress-induced PPP1R15A, but not the related and constitutive PPP1R15B, to prolong the benefit of an adaptive phospho-signaling pathway, protecting cells from otherwise lethal protein misfolding stress[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Icerguastat (100 μg; i.p.) prolongs the survival of prion-infected mice[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J female mice immunized with MOG35-55/CFA to induce chronic EAE[1]
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Dosage:4 mg/kg, 8 mg/kg
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Administration:I.p.; daily for 35 days
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Result:Significantly delayed clinical disease onset with both dosages, but to a greater extent with the 8 mg/kg treatment.
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Animal Model:Five-week-old female FVB mice (intracerebrally with mouse-adapted RML prions)[3]
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Dosage:100 μg
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Administration:I.p.; 3 times per week for 60 days, after 60 days of treatment, the treatment was reduced to two i.p. injections per week for another 20 days.
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Result:Significantly prolonged survival of prion-infected mice.
化学情報
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CAS 番号 951441-04-6
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性状 Solid
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分子量 196.64
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分子式 C8H9ClN4
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Color White to off-white
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SMILES
ClC1=CC=CC=C1/C=N/NC(N)=N
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別名
Sephin1; IFB-088
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (4)
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Journal Impact Factor
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Most Recent
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JACC Basic Transl Sci
Pharmacological Enhancement of Integrated Stress Response Confers Protection in Calcific Aortic Valve Disease. [Abstract]2025 Dec 15;11(1):101433. PMID: 41401678
Icerguastat purchased from MedChemExpress. Usage Cited in: JACC Basic Transl Sci. 2025 Dec 15;11(1):101433. [Abstract]
Icerguastat (Sephin1) (0.5 μM; 14 d) significantly reduced calcium deposition by 47% and decreased calcium concentration by 40% in AVIC treated with OGM.
Icerguastat purchased from MedChemExpress. Usage Cited in: JACC Basic Transl Sci. 2025 Dec 15;11(1):101433. [Abstract]
Icerguastat (Sephin1) (0.5 μM; 14 d) markedly reduced the protein levels of calcification markers OPN and Runx2 in AVICs treated with OGM.
Icerguastat purchased from MedChemExpress. Usage Cited in: JACC Basic Transl Sci. 2025 Dec 15;11(1):101433. [Abstract]
Icerguastat (Sephin1) (1 mg/kg; i.p.; once daily for 10 d) significantly alleviated aortic stenosis in CAVD mice subjected to the adenine/Vitamin D regimen, as evidenced by marked reductions in transvalvular peak jet velocity and transaortic valve pressure.
Icerguastat purchased from MedChemExpress. Usage Cited in: JACC Basic Transl Sci. 2025 Dec 15;11(1):101433. [Abstract]
Icerguastat (Sephin1) (1 mg/kg; i.p.; once daily for 10 d) led to the observed mitigation of calcified nodule formation in the AVs of CAVD mice.
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Free Radic Biol Med
Advanced oxidation protein products exacerbate osteoarthritis progression by disrupting stress granules assembly via endoplasmic reticulum stress. [Abstract]2026 Aug 1:251:440-453. PMID: 42009145 -
Icerguastat purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Jun 30.
Icerguastat (Sephin1) (10 mg/kg; i.p.; once daily for 28 d) significantly improved the sensorimotor coordination and fatigue resistance of ICH (intracerebral hemorrhage) mice.
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溶剤 & 溶解度
DMSO : 50 mg/mL (254.27 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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: ≥ 2.08 mg/mL (10.58 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (10.58 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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.
純度とドキュメンテーション
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データシート (274 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Chen Y, et al. Sephin1, which prolongs the integrated stress response, is a promising therapeutic for multiple sclerosis. Brain. 2019;142(2):344-361. [Content Brief]
[2]. Das I, et al. Preventing proteostasis diseases by selective inhibition of a phosphatase regulatory subunit. Science. 2015;348(6231):239-242. [Content Brief]
[3]. Thapa S, et al. Sephin1 Reduces Prion Infection in Prion-Infected Cells and Animal Model. Mol Neurobiol. 2020;57(5):2206-2219. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 5.0854 mL | 25.4272 mL | 50.8544 mL | 127.1359 mL |
| 5 mM | 1.0171 mL | 5.0854 mL | 10.1709 mL | 25.4272 mL | |
| 10 mM | 0.5085 mL | 2.5427 mL | 5.0854 mL | 12.7136 mL | |
| 15 mM | 0.3390 mL | 1.6951 mL | 3.3903 mL | 8.4757 mL | |
| 20 mM | 0.2543 mL | 1.2714 mL | 2.5427 mL | 6.3568 mL | |
| 25 mM | 0.2034 mL | 1.0171 mL | 2.0342 mL | 5.0854 mL | |
| 30 mM | 0.1695 mL | 0.8476 mL | 1.6951 mL | 4.2379 mL | |
| 40 mM | 0.1271 mL | 0.6357 mL | 1.2714 mL | 3.1784 mL | |
| 50 mM | 0.1017 mL | 0.5085 mL | 1.0171 mL | 2.5427 mL | |
| 60 mM | 0.0848 mL | 0.4238 mL | 0.8476 mL | 2.1189 mL | |
| 80 mM | 0.0636 mL | 0.3178 mL | 0.6357 mL | 1.5892 mL | |
| 100 mM | 0.0509 mL | 0.2543 mL | 0.5085 mL | 1.2714 mL |
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