Aldose reductase-IN-1 NEW
| Price | $52 | $123 | $187 |
| Package | 1mg | 5mg | 10mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-08 |
Product Details
| Product Name: Aldose reductase-IN-1 | CAS No.: 1355612-71-3 |
| Purity: 99.82% | Supply Ability: 10g |
| Release date: 2024/11/08 |
Product Introduction
Bioactivity
| 名稱 | Aldose reductase-IN-1 |
| 描述 | Aldose reductase-IN-1 (AT-001, Caficrestat) is a highly potent inhibitor of aldose reductase with an IC50 value of 28.9 pM, which can target the relaxin hormone signaling pathway in prostate cancer models. |
| 體外活性 | METHODS: To confirm that Aldose reductase-IN-1（ AT-001，Caficrestat） retains its ability to bind to the major relaxin receptor RXFP1, H2 relaxin was labeled with 125I using Pierce iodination reagent, which radioiodinates the phenol aromatic ring of the Tyr residue (Tyr3 on the A chain). RESULTS In an in vitro cell assay using the 293T.RXFP1 cell line, we showed that H2 relaxin binds to RXFP1 in the presence of a cognate competitive RBA with a Kd of 17.0 nM; similarly, Aldose reductase-IN-1（ AT-001，Caficrestat） was shown to retain its binding ability to RXFP1 in the presence of a competitive RBA, inhibiting the binding of 125I-labeled H2 relaxin with a Ki of 9.2 μM[3]. |
| 體內(nèi)活性 | METHODS: Male C57BL/6J mice (8 weeks old) were subjected to experimental type 2 diabetes/diabetic cardiomyopathy for 10 weeks. At 4 weeks, they were given a single intraperitoneal injection of streptozotocin (75 mg/kg). Animals were then randomly assigned to Aldose reductase-IN-1 (AT-001, Caficrestat) (40 mg/kg/day, intraperitoneal injection, for 3 weeks). At the completion of the study, hearts were perfused in an isolated working mode to assess energy metabolism. RESULTS Aldose reductase-IN-1 (AT-001, Caficrestat) improved diastolic function and cardiac efficiency in mice with experimental type 2 diabetes; in mice with diabetic cardiomyopathy, Aldose reductase-IN-1 (AT-001, Caficrestat) also reduced cardiac fibrosis and hypertrophy. [1] |
| 存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 45 mg/mL (106.8 mM) |
| 關(guān)鍵字 | inhibit | Aldose reductaseIN1 | Inhibitor | Aldose Reductase | AT001 | Aldose reductase IN 1 | AT 001 | Aldose reductase-IN-1 |
| 相關(guān)產(chǎn)品 | MK 0434 | Alconil | Epalrestat | D-Methionine sulfoxide | 2-Chloro-1-(4-fluorobenzyl)benzimidazole | Tolrestat | Lidorestat | Alpha-Estradiol | Isoliquiritigenin | Finasteride | Epristeride | Dutasteride |
| 相關(guān)庫 | 經(jīng)典已知活性庫 | ReFRAME 相關(guān)化合物庫 | 抑制劑庫 | NO PAINS 化合物庫 | 內(nèi)分泌激素分子庫 | 代謝化合物庫 | 已知活性化合物庫 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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United States- Since: 2011-01-07
- Address: 36?Washington?Street, Wellesley?Hills
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