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MLN-4760

Cat. No. M14300
MLN-4760 Structure
Size Price Availability Quantity
5mg USD 450  USD450 In stock
10mg USD 720  USD720 In stock
25mg USD 1320  USD1320 In stock
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Quality Control & Documentation
Biological Activity

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).

Chemical Information
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
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Andrea Berenyiova, et al. Vascular Effects of Low-Dose ACE2 Inhibitor MLN-4760-Benefit or Detriment in Essential Hypertension?

[2] Tomas Jasenovec, et al. Angiotensin System Modulations in Spontaneously Hypertensive Rats and Consequences on Erythrocyte Properties; Action of MLN-4760 and Zofenopril

[3] Apurba Bhattarai, et al. Mechanism of Ligand Recognition by Human ACE2 Receptor

[4] Shrinidh Joshi, et al. Angiotensin converting enzyme versus angiotensin converting enzyme-2 selectivity of MLN-4760 and DX600 in human and murine bone marrow-derived cells

[5] Paul Towler, et al. ACE2 X-ray structures reveal a large hinge-bending motion important for inhibitor binding and catalysis

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Keywords: MLN-4760 supplier, ACE, inhibitors, activators


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