DX600

Catalog No.S9666 Batch:S966601

Technical Data

Formula	C₁₄₁H₁₈₅N₃₅O₄₀S₂
Molecular Weight	3074.32	CAS No.	478188-26-0
Solubility (25°C)*	In vitro	Water	100 mg/mL (32.52 mM)


* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

DX600 is a specific inhibitor of angiotensin-converting enzyme 2 (ACE2) that does not cross-react with ACE.

Targets

ACE2 ^[1]

In vitro

DX600 is an ACE2 specific inhibitor that does not cross-react with ACE. Three human cell lines (Calu-3, Caco-2, Huh-7) are evaluated for the cell surface expression of ACE2 by flow cytometry and Western blot. Subsequently, whole cell lysates, cell culture supernatant, and live cells are evaluated in the assay. Calu-3 has elevated levels of ACE2 compared to Caco-2 or Huh-7. Calu-3 also demonstrates elevated ACE2 enzymatic activity in all three sources and can be inhibited by DX600.^[1]

In vivo

Mouse ACE2-driven Ang-(1-7) formation from Ang II is blocked by MLN-4760 but not by either linear or cyclic DX600. DX600 only blocks human ACE2 activity.^[2]

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines Three human cell lines (Calu-3, Caco-2, Huh-7) Concentrations 10 μM Incubation Time 1 h Method To measure NAb activity against endogenous ACE2, the recombinant ACE2 is replaced by cellular ACE2. 100 μL of cell lysate at 4 mg/mL or same volume of cell culture supernatant is pre-incubated with either PCs at a final concentration of 10 μg/mL, equal volume control serum, DX600, ACE2 specific inhibitor at final concentration of 10 μM, or equal volume of control buffer (PBS) at room temperature for 1 h.

Cell Assay:^{^[1]}

Cell lines
Three human cell lines (Calu-3, Caco-2, Huh-7)
Concentrations
10 μM
Incubation Time
1 h
Method
To measure NAb activity against endogenous ACE2, the recombinant ACE2 is replaced by cellular ACE2. 100 μL of cell lysate at 4 mg/mL or same volume of cell culture supernatant is pre-incubated with either PCs at a final concentration of 10 μg/mL, equal volume control serum, DX600, ACE2 specific inhibitor at final concentration of 10 μM, or equal volume of control buffer (PBS) at room temperature for 1 h.

References

Selleck's DX600 has been cited by 2 publications

Extrinsic stabilization of antiviral ACE2-Fc fusion proteins targeting SARS-CoV-2 [ Commun Biol, 2023, 6(1):386]	PubMed: 37031320
Extrinsic stabilization of antiviral ACE2-Fc fusion proteins targeting SARS-CoV-2 [ Communications Biology, 2023, 6(1)]	PubMed: None

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.