SCH28080
Based on 1 Customer Validation
SCH28080 is a reversible, K+-competitive inhibitor of the gastric H,K-ATPase, with a Ki of 0.12 μM. SCH28080 is an effective inhibitor of acid secretion in vivo and with anti-gastric ulcer activity.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.0%
- CAS 番号: 76081-98-6
- 分子式: C17H15N3O
- 分子量:277.32
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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生物活性
Ki: 0.12 μM ((H+/K+)-ATPase)[1]
SCH28080 competitively inhibits the K+-stimulated hydrolysis of ATP, with a Ki of 0.12 μM [1].
SCH28080 inhibits histamine-induced [14C]aminopyrine uptake into isolated rabbit parietal cells with an IC50 of 0.029 μM[1].
SCH28080 causes a dose-dependent reduction in cell viability with IC50 values of 22.9 μM and 15.3 μM after 2 h and 24 h treatments, respectively, and cell viability was below 10% at 100 μM already after 2 h treatment[2].
SCH28080 induces apoptosis and is cytotoxic at higher doses[2].
SCH28080 inhibits insulin secretion by activation of IK ATP and inhibition of L-type voltage-gated Ca2+ channels, reduces cell viability and dose-dependently induces apoptosis/necrosis[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:INS-1E cell
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Concentration:3.1 μM, 6.25 μM, 12.5 μM, 25 μM, 50 μM, 100 μM
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Incubation Time:2 hours, 24 hours
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Result:Caused a dose-dependent reduction in cell viability.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Wistar rat (280-350 g), the Shay rat model[3]
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Dosage:20 mg/kg
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Administration:Intraperitoneal injection
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Result:Showed 91% inhibition on gastric ulcers induced by pylorusligation in rats.
化学情報
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CAS 番号 76081-98-6
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性状 Solid
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分子量 277.32
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分子式 C17H15N3O
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Color Light yellow to brown
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SMILES
N#CCC1=C(C)N=C2C(OCC3=CC=CC=C3)=CC=CN21
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 100 mg/mL (360.59 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. 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. 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: ≥ 2.5 mg/mL (9.01 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (9.01 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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 (277 KB)
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SDS (393 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Scott CK, et al. Studies on the mechanism of action of the gastric microsomal (H+ + K+)-ATPase inhibitors SCH 32651 and SCH 28080. Biochem Pharmacol. 1987 Jan 1;36(1):97-104. [Content Brief]
[2]. Martin Jakab, et al. The H+/K+ ATPase Inhibitor SCH-28080 Inhibits Insulin Secretion and Induces Cell Death in INS-1E Rat Insulinoma Cells. Cell Physiol Biochem. 2017;43(3):1037-1051. [Content Brief]
[3]. Y Hamagishi, et al. Inhibitory Effects of Copiamycin A, a Macrocyclic Lactone Antibiotic, on Gastric H+,K(+)-ATPase, Acid Secretion and Ulcer Formation. Jpn J Pharmacol. 1991 Feb;55(2):283-6. [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. 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 | 3.6059 mL | 18.0297 mL | 36.0594 mL | 90.1486 mL |
| 5 mM | 0.7212 mL | 3.6059 mL | 7.2119 mL | 18.0297 mL | |
| 10 mM | 0.3606 mL | 1.8030 mL | 3.6059 mL | 9.0149 mL | |
| 15 mM | 0.2404 mL | 1.2020 mL | 2.4040 mL | 6.0099 mL | |
| 20 mM | 0.1803 mL | 0.9015 mL | 1.8030 mL | 4.5074 mL | |
| 25 mM | 0.1442 mL | 0.7212 mL | 1.4424 mL | 3.6059 mL | |
| 30 mM | 0.1202 mL | 0.6010 mL | 1.2020 mL | 3.0050 mL | |
| 40 mM | 0.0901 mL | 0.4507 mL | 0.9015 mL | 2.2537 mL | |
| 50 mM | 0.0721 mL | 0.3606 mL | 0.7212 mL | 1.8030 mL | |
| 60 mM | 0.0601 mL | 0.3005 mL | 0.6010 mL | 1.5025 mL | |
| 80 mM | 0.0451 mL | 0.2254 mL | 0.4507 mL | 1.1269 mL | |
| 100 mM | 0.0361 mL | 0.1803 mL | 0.3606 mL | 0.9015 mL |
SCH28080 関連分類
HY-103261 関連分類
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