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Art. -Nr.: HY-184485

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MB-32

MB-32 is a potent and selective allosteric inhibitor of human angiotensin-converting enzyme 2 (hACE2) with a K_d value of 7.078 μM. MB-32 binds to a non-catalytic surface pocket on the N-terminal helix of ACE2, disrupts the interaction between ACE2 and the receptor-binding domain of SARS-CoV-2 spike protein through allosteric action, and preserves the enzymatic activity of ACE2 across different species. MB-32 achieves high concentrations in the airway via intranasal administration, with no detected cardiovascular toxicity. MB-32 can be used for research on coronavirus disease 2019.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Formel: C₂₆H₃₀N₈O₃S
Molecular Weight:534.63

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

MB-32 Chemical Structure

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

ACE2

7.078 μM (Kd, SPR assay)

In Vitro

MB-32 (0.4-10 μM (hACE2); 60-second association and 120-second dissociation phases) binds to recombinant human ACE2 with a K_D value of 7.078 μM, and also binds to ACE2 homologs from various mammals with micromolar affinity^[1].
MB-32 (5 μg/mL; 15-minute pre-incubation, followed by 1-hour co-incubation with spike) reduces the binding capacity of SARS-CoV-2 spike protein to human ACE2 on the surface of transiently transfected HEK293T cells, without affecting the expression level of ACE2^[1].
The binding of MB-32 (0.4-20 μM; 60-second association and 120-second dissociation phases) to human ACE2 is strongly dependent on the P565 residue, with additional contributions from the Y83, Q86, Q98 and Q102 residues^[1].
MB-32 (0.01-100 μM; assay duration) potently and selectively inhibits pan-sarbecovirus pseudovirus entry into HEK293T-ACE2 cells, with an IC₅₀ of 105 nM against SARS-CoV-2 wild-type and a selectivity index of 183.8^[1].
MB-32 (0.308-25 μg/mL; 24 hours) inhibits the multi-cycle replication of authentic SARS-CoV-2 variants of concern (VOCs) and SARS-CoV-1 in HEK293T-ACE2 cells, with a mean IC₅₀ of 9.2 μM, and shows no cytotoxicity at concentrations up to 129 μM^[1].
MB-32 (0-8 μM; pre-incubated with virus for 2 hours followed by 24-hour culture) selectively inhibits SARS-CoV-2 replication in Calu-3 cells, with an IC₅₀ of 1.615 μM, and shows no activity against MERS-CoV^[1].
MB-32 (17.5 μM; 30 minutes (TMPRSS2); 5 minutes (Cathepsin L)) does not inhibit the enzymatic activity of TMPRSS2 or Cathepsin L^[1].
The inhibitory effect of MB-32 (0.01-100 μM; assay duration) on SARS-CoV-2 pseudovirus entry is attenuated in HEK293T cells expressing ACE2^Y83F or ACE2^Y83A ACE2 mutants, indicating that Y83 is critical for the antiviral activity of MB-32^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

RT-PCR^[1]

Cell Line:

Calu-3
Concentration:

0.5, 1, 2, 4, 8 μM
Incubation Time:

24 h, following a 2 h viral inoculation period
Result:

Reduced the SARS-CoV-2 nucleocapsid gene level with an IC₅₀ of 1.615 μM, while no measurable inhibition of MERS-CoV was observed under the same conditions.

Immunofluorescence^[1]

Cell Line:

HEK293T-ACE2
Concentration:

5 μg/mL
Incubation Time:

15 min pretreatment followed by 1 h incubation
Result:

Reduced Spike binding and internalization without affecting transferrin receptor-mediated endocytosis.

In Vivo

MB-32 (2.33 mg/kg; intranasal administration; single dose) provides potent protection against SARS-CoV-2 Omicron BA.2 infection in K18-hACE2 mice, reduces lung viral load by >2 log levels, and prevents detectable viral protein expression^[1].
MB-32 (400 μg per hamster; intranasal administration; single dose) protects golden hamsters from infection with the SARS-CoV-2 Omicron JN.1 strain^[1].
MB-32 (350 nmol per hamster; intranasal administration; single dose) prevents contact transmission of SARS-CoV-2 XBB.1.5 in golden hamsters, reducing infectious viral titers and viral gene copy numbers in the lungs by >2 logs^[1].
MB-32 (60 μg per mouse; intranasal administration; single dose; co-administered with virus) provides complete protection against lethal SARS-CoV-2 infection in K18-hACE2 mice, resulting in 100% mouse survival, near-complete inhibition of viral replication, and reduced pathological damage in the lungs^[1].
MB-32 (200 μg per rat; intranasal administration; single dose) shows no obvious cardiovascular adverse effects in Sprague Dawley rats^[1].
MB-32 (2.33 mg/kg, i.n., single dose) achieves high local exposure in male C57BL/6 mice, with AUC_last values of 466,726 ng·h/g in nasal turbinates and 13,346 ng·h/g in lungs, while systemic exposure remains relatively low^[1]

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

K18-hACE2 C57BL/6J transgenic (6-8-week-old male, intranasal challenge with 2.5 × 10⁴ PFU SARS-CoV-2 Omicron BA.2)^[1]
Dosage:

60 μg/mouse; 2.33 mg/kg
Administration:

i.n.; single dose
Result:

Preserved body weight.
Reduced viral RdRp gene copies in lungs by >2 logs.
Reduced viral NP gene copies by >2 logs.
Eliminated detectable viral N protein in lung tissue.
Prevented significant infection-related histopathological lesions.

Animal Model:

K18-hACE2 C57BL/6J transgenic (6-8-week-old male, intranasal challenge with 2.5 × 10⁴ PFU SARS-CoV-2 Omicron BA.5)^[1]
Dosage:

60 μg/mouse; 2.33 mg/kg
Administration:

i.n.; single dose
Result:

Prevented significant body weight loss.
Reduced viral RdRp gene copies in lungs by ~1.5 logs.
Reduced viral sgNP gene copies by ~1.5 logs.
Reduced viral N protein detection in lung tissue (2/4 positive vs. 4/4 positive in vehicle controls).
Prevented severe infection-related histopathological lesions.

Animal Model:

(8-week-old male, intranasal challenge with 1 × 10⁵ PFU SARS-CoV-2 Omicron JN.1)^[1]
Dosage:

400 μg/hamster; 2 mg/mL
Administration:

i.n.; single dose
Result:

Reduced lung viral loads compared to vehicle controls.

Animal Model:

(10-12-week-old male, COVID-19 contact transmission model with SARS-CoV-2 XBB.1.5)^[1]
Dosage:

350 nmol/hamster
Administration:

i.n.; single dose
Result:

Reduced infectious viral titres in lungs by >2 logs (P<0.0001).
Reduced viral RdRp and sgNP gene copies in lungs by >2 logs (P<0.0001).
Eliminated detectable viral N protein in lung tissue.
Prevented severe infection-related histopathological lesions.

Animal Model:

K18-hACE2 C57BL/6J transgenic (6-8-week-old male, intranasal challenge with 4 × 10³ PFU SARS-CoV-2 HKU-001a)^[1]
Dosage:

60 μg/mouse
Administration:

i.n.; single dose; co-administered with virus
Result:

Maintained stable body weights.
Achieved 100% survival compared to 0% survival in vehicle controls.
Suppressed viral RdRp gene copies by ~4.4 × 10⁵-fold in nasal turbinates.
Suppressed viral RdRp gene copies by ~8.6 × 10⁴-fold in lungs.
Eliminated detectable infectious virus in nasal turbinates or lungs (limit of detection <10 PFU/mL).
Eliminated detectable viral N protein in lung tissue.
Alleviated severe histopathological lesions (bronchiolitis, vasculitis, alveolitis with inflammatory infiltrates and hemorrhage).

Animal Model:

Sprague Dawley (220 g male and female, cardiovascular safety assessment)^[1]
Dosage:

200 μg/rat
Administration:

i.n.; single dose
Result:

Showed no significant abnormal changes in heart rate, blood pressure, or ECG parameters compared to pre-drug baselines or vehicle controls.

Chemical Information

Molecular Weight 534.63
Formel C₂₆H₃₀N₈O₃S
SMILES

CC1=CC=C(C=C1)C2=NC3=CC(NC(NCCN4C=C(N=C4C)[N+]([O-])=O)=O)=C(C=C3S2)N5CCN(CC5)C
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Liu L, et al. Human angiotensin‑converting enzyme 2‑specific benzothiazole-based allosteric inhibitor against pan‑sarbecoviruses. Nature communications. 2026 Jun 06. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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