FOY 251
目录号 : GC60856
An active metabolite of camostat
Cas No.:71079-09-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
FOY-251 is an active metabolite of the antiviral protease inhibitor camostat .1 It inhibits transmembrane serine protease 2 (TMPRSS2; IC50 = 33.3 nM).2 FOY-251 inhibits entry of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) pseudotyped particles in Calu-3 cells (EC50 = 178 nM) and reduces viral titers in SARS-CoV-2-infected Calu-3 cells when used at concentrations ranging from 1 to 10 ?M.1
1.Hoffmann, M., Hofmann-Winkler, H., Smith, J.C., et al.Camostat mesylate inhibits SARS-CoV-2 activation by TMPRSS2-related proteases and its metabolite GBPA exerts antiviral activityEBioMedicine65103255(2021) 2.Shrimp, J.H., Kales, S.C., Sanderson, P.E., et al.An enzymatic TMPRSS2 assay for assessment of clinical candidates and discovery of inhibitors as potential treatment of COVID-19bioRxiv167544(2020)
| Cas No. | 71079-09-9 | SDF | |
| Canonical SMILES | O=C(O)CC1=CC=C(OC(C2=CC=C(NC(N)=N)C=C2)=O)C=C1.CS(=O)(O)=O | ||
| 分子式 | C17H19N3O7S | 分子量 | 409.41 |
| 溶解度 | DMSO: 20 mg/mL (48.85 mM; ultrasonic and adjust pH to 5 with HCl); Water: < 0.1 mg/mL (insoluble) | 储存条件 | 4°C, away from moisture |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4425 mL | 12.2127 mL | 24.4254 mL |
| 5 mM | 0.4885 mL | 2.4425 mL | 4.8851 mL |
| 10 mM | 0.2443 mL | 1.2213 mL | 2.4425 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Elimination of the low-molecular weight proteinase inhibitor camostate (FOY 305) and its degradation products by the rat liver
Res Exp Med (Berl) 1987;187(6):401-6.PMID:3441682DOI:10.1007/BF01852177.
The elimination of the low molecular weight proteinase inhibitor camostate (FOY 305) was studied in rats after oral administration and in the the situ perfused rat liver. After feeding of camostate (400 mg/kg b.w.) only the metabolites (FOY 251, GBA) were detected in blood samples withdrawn from the portal and hepatic vein. This indicated a rapid degradation of FOY 305 after absorption from the gut lumen. The hepatic extraction of the anti-proteolytic active metabolite FOY 251 during a single liver passage was 23%. It remained almost constant over the period of 120 min. In the perfused rat liver, FOY 305 was given in concentrations comparable to the in vivo studies. It was eliminated by 20%. In these experiments, the compound was metabolized to FOY 251 and in minor amounts to guanidino-benzoate (GBA), the latter being an anti-proteolytic ineffective degradation product. In conclusion, a low hepatic extraction of FOY 305 led to pharmacologically effective concentrations of the active metabolite FOY 251 in the circulation after oral ingestion of the proteinase inhibitor.