ER-464195-01
Based on 1 Customer Validation
ER-464195-01 is an orally active calreticulin (CRT) and integrin α subunits (ITGAs) binding inhibitor. ER-464195-01 inhibits leukocyte infiltration and subsequent inflammatory cascade reactions by dissociating the binding between CRT and ITGA. ER-464195-01 down-regulates the expression of pro-inflammatory genes (such as TNF-α, IL-1β, IL-6, IL-17f) induced by DSS (HY-116282C), and inhibit the phosphorylation of STAT3 and the production of serum amyloid A (SAA). ER-464195-01 can be used for the study of inflammatory bowel disease (IBD).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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: 99.72%
- CAS 番号: 859218-37-4
- 分子式: C23H39ClN2
- 分子量:379.02
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
生物活性
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STAT3 |
IL-1β |
IL-6 |
IL-17F |
ER-464195-01 (5 μM) effectively inhibits the interaction between CRT and ITGA4 within the Jurkat cells and significantly reduces the level of CRT on the cell surface[1].
ER-464195-01 (0.01-10 μM, 60 min) inhibits the adhesion ability of VCAM-1 cells stimulated by PMA (HY-18739) and ICAM-1 cells stimulated by fMLP (HY-P0224), with IC50 values of 0.15 μM and 0.19 μM respectively, and has no inhibitory effect under MnCl2 stimulation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:DSS induced IBD model established in female Balb/c mice (9- to 10-week-old)[1]
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Dosage:10 mg/kg (preventive administration) and 5 mg/kg (therapeutic administration)
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Administration:Oral administration (p.o.), once daily for 6-7 days
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Result:Effectively alleviated the weight loss, increased DAI, and shortened colon in mice under both administration methods.
Reduced the interaction signal between CRT and ITGA4.
Inhibited the upregulation of key pro-inflammatory cytokine mRNAs such as TNF-α, IL1-b, IL-6, and IL-17f induced by DSS.
Inhibited the phosphorylation of STAT3 (p-STAT3) induced by DSS and the production of serum amyloid A (SAA).
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Animal Model:CD4+CD45RBhigh T-cell transfer model established in female Balb/c mice (6-week-old)[1]
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Dosage:10 mg/kg
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Administration:Oral administration (p.o.), once daily for 32 days
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Result:Significantly improved the weight loss in mice and the changes in their fecal characteristics (diarrhea).
化学情報
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CAS 番号 859218-37-4
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性状 Solid
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分子量 379.02
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分子式 C23H39ClN2
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Color White to off-white
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SMILES
CC1(C)CC(C)(C)CC(C2=CC=CC=C2N3CCN(CCC)CC3)C1.Cl
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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 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 5 mg/mL (13.19 mM; ultrasonic and warming and heat to 60°C; 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)
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 (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
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 | 2.6384 mL | 13.1919 mL | 26.3838 mL | 65.9596 mL |
| 5 mM | 0.5277 mL | 2.6384 mL | 5.2768 mL | 13.1919 mL | |
| 10 mM | 0.2638 mL | 1.3192 mL | 2.6384 mL | 6.5960 mL |