Firibastat
Based on 1 publication(s) in Google Scholar
Firibastat (QGC001), an orally active brain penetrating proagent of EC33, is a first-in-class brain aminopeptidase A (APA) inhibitor (Ki=200 nM). Firibastat selectively and specifically inhibits conversion of brain angiotensin-II into angiotensin-III and decreases blood pressure in hypertensive rats.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.0%
- No. CAS: 648927-86-0
- Fòrmula: C8H20N2O6S4
- Peso molecular:368.51
-
Almacenamiento:Powder -20°C, 3 years , 4°C, 2 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]
-
Actividad biológica
-
Chemical Information
-
Solvente y solubilidad
- Pureza y Documentación
- Referencias
-
Help & FAQs
-
Metabolism/Protease Compound Library
HY-L012
-
Clinical Compound Library
HY-L026
-
CNS-Penetrant Compound Library
HY-L028
-
Drug Repurposing Compound Library
HY-L035
-
Anti-Cardiovascular Disease Compound Library
HY-L046
-
Orally Active Compound Library
HY-L061
-
Human Metabolite Library
HY-L123
-
Metabolic Enzyme Compound Library
HY-L146
-
Protease Inhibitor Library
HY-L147
-
Highly Selective Inhibitors Library
HY-L158
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Drug Repurposing Compound Library Plus
HY-L035P
-
Clinical Compound Library Plus
HY-L026P
-
Bioactive Compound Library
HY-L001
-
High-Throughput Bioactive Compound Library
HY-L205
-
Mass Spectrometry Human Metabolite Library
HY-L215
Publications Citing Use of MedChemExpress (MCE) Firibastat
More
Actividad biológica
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Normotensive and hypertensive DOCA-salt rats[1]
-
Dosage:0.1-30 mg/kg
-
Administration:P.o.
-
Result:Resulting in a dose-dependent decrease in mean arterial blood pressure (MABP).
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
No. CAS 648927-86-0
-
Appearance Solid
-
Peso molecular 368.51
-
Fòrmula C8H20N2O6S4
-
Color White to off-white
-
SMILES
O=S(CC[C@H](N)CSSC[C@@H](N)CCS(=O)(O)=O)(O)=O
-
Synonyms
QGC001; RB150
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
-
Journal Impact Factor
-
Most Recent
Solvente y solubilidad
H2O : 25 mg/mL (67.84 mM; Need ultrasonic)
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 100 mg/mL (271.36 mM); Clear solution; Need ultrasonic
Pureza y Documentación
-
Ficha de datos (271 KB)
-
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
-
Instrucciones de manejo (2659 KB)
Referencias
[1]. Ferdinand KC, et al. Efficacy and Safety of Firibastat, A First-in-Class Brain Aminopeptidase A Inhibitor, in Hypertensive Overweight Patients of Multiple Ethnic Origins. Circulation. 2019;140(2):138-146. [Content Brief]
[2]. Keck M, et al. Orally Active Aminopeptidase A Inhibitor Prodrugs: Current State and Future Directions. Curr Hypertens Rep. 2019;21(7):50. Published 2019 May 21. [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 |
|---|---|---|---|---|---|
| H2O | 1 mM | 2.7136 mL | 13.5682 mL | 27.1363 mL | 67.8408 mL |
| 5 mM | 0.5427 mL | 2.7136 mL | 5.4273 mL | 13.5682 mL | |
| 10 mM | 0.2714 mL | 1.3568 mL | 2.7136 mL | 6.7841 mL | |
| 15 mM | 0.1809 mL | 0.9045 mL | 1.8091 mL | 4.5227 mL | |
| 20 mM | 0.1357 mL | 0.6784 mL | 1.3568 mL | 3.3920 mL | |
| 25 mM | 0.1085 mL | 0.5427 mL | 1.0855 mL | 2.7136 mL | |
| 30 mM | 0.0905 mL | 0.4523 mL | 0.9045 mL | 2.2614 mL | |
| 40 mM | 0.0678 mL | 0.3392 mL | 0.6784 mL | 1.6960 mL | |
| 50 mM | 0.0543 mL | 0.2714 mL | 0.5427 mL | 1.3568 mL | |
| 60 mM | 0.0452 mL | 0.2261 mL | 0.4523 mL | 1.1307 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Firibastat Related Classifications
HY-109058 Related Classifications
Powered by Bioz