Firibastat (QGC001) is an orally active EC33 precursor drug. Firibastat is A first-in-class (first-in-class) brain aminopeptidase A (APA) inhibitor (Ki=200 nM) that selectively and specifically inhibits the conversion of cerebral angiotensin II to angiotensin III and lowers blood pressure in hypertensive rats.
| Molecular Weight | 368.51 |
| Formula | C8H20N2O6S4 |
| CAS Number | 648927-86-0 |
| Solubility (25°C) | Wate ≥ 20 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[2] Shawna D Nesbitt. Curr Hypertens Rep. Firibastat: a Novel Treatment for Hypertension
| Related Aminopeptidase Products |
|---|
| LYS006 hydrochloride
LYS-006 hydrochloride is a potent inhibitor of leukotriene A4 hydrolase (LTA4H) with IC50 of 2 nM. LYS-006 hydrochloride can be used for the research of inflammatory and autoimmune disorders, including ulcerative colitis and NASH. |
| Aminopeptidase N Ligand (CD13) NGR peptide
Aminopeptidase N Ligand (CD13) NGR peptide is a polypeptide targeting CD13 and can be used as a carrier to mediate intracellular transmission. |
| H-D-Ala-D-Ala-D-Ala-D-Ala-OH
H-D-Ala-D-Ala-D-Ala-D-Ala-OH is a substrate for D-aminopeptidase. |
| H-Leu-Trp-Met-Arg-OH
H-Leu-Trp-Met-Arg-OH is a tetrapeptide. |
| NGR peptide
NGR peptide containing the Asn-Gly-Arg (NGR) motif. |
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