MLN-4760 is a potent and selective human ACE2 inhibitor (IC50, 0.44 nM), with excellent selectivity (>5000-fold) versus related enzymes including human testicular ACE (IC50, >100 μM) and bovine carboxypeptidase A (CPDA; IC50, 27 μM).
| Molecular Weight | 428.31 |
| CAS Number | 305335-31-3 |
| Solubility (25°C) | DMSO 90 mg/mL (ultrasonic and adjust pH to 9 with NaOH) |
| Storage | 2-8°C, dry, sealed |
| 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.
[3] Apurba Bhattarai, et al. Mechanism of Ligand Recognition by Human ACE2 Receptor
| Related ACE Products |
|---|
| Abz-Ser-Pro-3-nitro-Tyr
Abz-Ser-Pro-3-nitro-Tyr is the substrate of ACE2 (angiotensin-converting enzyme-2). |
| Temocaprilat
Temocaprilat (Temocapril diacid) is an inhibitor of angiotensin-converting enzyme (ACE). |
| FA-Phe-Phe
FA-Phe-Phe is a furylacryloyl (fa)-amino acid derivative, targeting to Angiotensin-converting Enzyme (ACE). |
| Garcinone B
Garcinone B, a xanthone derivative, is a nature product that could be isolated from the pericarp of Mangosteen. |
| Spirapril hydrochloride
Spirapril (SCH 33844) hydrochloride is a potent angiotensin converting enzyme (ACE) inhibitor with antihypertensive activity. Spirapril competitively binds to ACE and prevents the conversion of angiotensin I to angiotensin II. Spirapril is an orally active proagent of Spiraprilat and can be used for the research of hypertension, congestive heart failure. |
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