Zagociguat
Based on 1 Customer Validation
Zagociguat (CY-6463) is an orally active and BBB-permeable soluble guanylate cyclase (sGC) stimulator. Zagociguat can increase cGMP levels, regulate blood pressure, improve neuronal function, reduce inflammatory responses, and exert neuroprotective and cognitive-improving effects. Zagociguat can be used in the research of neurodegenerative diseases.
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: 99.09%
- CAS 番号: 2201048-82-8
- 分子式: C16H10F4N6
- 分子量:362.28
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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
Soluble Guanylate Cyclase[1]
Zagociguat (0.01 nM-30 μM; 20-30 min) can effectively stimulate sGC (EC50: 46 nM) and CREB phosphorylation (EC50: 25.7 nM) in rat primary neurons[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Zagociguat (7-308 nM; perfusion; single dose) increases long-term potentiation in hippocampal slices of a Huntington's disease mouse model[1].
Zagociguat (0.5-10 mg/kg; dietary administration; 6 weeks) can reduce the levels of plasma inflammatory markers TNFα and IL-16 and increase BDNF levels in the hindbrain and hypothalamus in diet-induced obese male mice[1].
Zagociguat (71.6 mg/kg; dietary administration; 18 weeks) can reduce the loss of dendritic spines in the hippocampus of aged male mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 2201048-82-8
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性状 Solid
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分子量 362.28
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分子式 C16H10F4N6
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Color Off-white to light yellow
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SMILES
FC1=C(CC2=NC(C3=NN=C(C(F)(F)F)N3)=CN4C=CN=C24)C=CC=C1
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別名
CY-6463; IW-6463
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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 : 250 mg/mL (690.07 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)
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 (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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 | 2.7603 mL | 13.8015 mL | 27.6030 mL | 69.0074 mL |
| 5 mM | 0.5521 mL | 2.7603 mL | 5.5206 mL | 13.8015 mL | |
| 10 mM | 0.2760 mL | 1.3801 mL | 2.7603 mL | 6.9007 mL | |
| 15 mM | 0.1840 mL | 0.9201 mL | 1.8402 mL | 4.6005 mL | |
| 20 mM | 0.1380 mL | 0.6901 mL | 1.3801 mL | 3.4504 mL | |
| 25 mM | 0.1104 mL | 0.5521 mL | 1.1041 mL | 2.7603 mL | |
| 30 mM | 0.0920 mL | 0.4600 mL | 0.9201 mL | 2.3002 mL | |
| 40 mM | 0.0690 mL | 0.3450 mL | 0.6901 mL | 1.7252 mL | |
| 50 mM | 0.0552 mL | 0.2760 mL | 0.5521 mL | 1.3801 mL | |
| 60 mM | 0.0460 mL | 0.2300 mL | 0.4600 mL | 1.1501 mL | |
| 80 mM | 0.0345 mL | 0.1725 mL | 0.3450 mL | 0.8626 mL | |
| 100 mM | 0.0276 mL | 0.1380 mL | 0.2760 mL | 0.6901 mL |