| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
Alunacedase alfa targets the spike glycoprotein of SARS-CoV-2. The compound has an affinity of approximately 1.2 nM for the SARS-CoV-2 spike glycoprotein. By binding to the spike protein, Alunacedase alfa prevents the virus from interacting with membrane-bound ACE2, thereby inhibiting viral entry into host cells. The compound is a recombinant form of human ACE2, which is the primary receptor for SARS-CoV-2 entry. Its mechanism of action is based on competitive inhibition of viral binding to cellular ACE2.
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| ln Vitro |
It has been calculated that alunacedase alfa has an affinity of about 1.2 nM for the spike glycoprotein of SARS-CoV-2[2].
In vitro studies have demonstrated that Alunacedase alfa binds to the SARS-CoV-2 spike glycoprotein with an affinity of approximately 1.2 nM. This high-affinity binding suggests that the soluble ACE2 protein can effectively compete with membrane-bound ACE2 for viral spike protein binding. The compound’s ability to neutralize SARS-CoV-2 in vitro has been supported by computational and experimental studies. Alunacedase alfa has been shown to reduce viral entry into cells expressing ACE2. |
| ln Vivo |
Alunacedase alfa has shown promise for treating severe COVID-19 in clinical studies. It has been evaluated in patients with severe COVID-19, and the results have been published in peer-reviewed journals including Signal Transduction and Targeted Therapy and The Lancet Respiratory Medicine. The compound’s ability to reduce SARS-CoV-2 competition for membrane-bound ACE2 suggests that it could be effective in reducing viral load and improving clinical outcomes in COVID-19 patients. Further studies have been conducted to evaluate its efficacy in various disease models.
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| Enzyme Assay |
The binding affinity of Alunacedase alfa to the SARS-CoV-2 spike glycoprotein can be assessed using surface plasmon resonance (SPR) or biolayer interferometry (BLI). In a typical assay, the spike glycoprotein is immobilized on a sensor chip, and varying concentrations of Alunacedase alfa are injected over the surface. The association rate (ka), dissociation rate (kd), and equilibrium dissociation constant (KD) are calculated from the sensorgram data. The KD for Alunacedase alfa binding to the SARS-CoV-2 spike glycoprotein is approximately 1.2 nM.
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| Cell Assay |
The in vitro activity of Alunacedase alfa is assessed using cell-based assays that measure viral entry. In a typical assay, cells expressing ACE2 are incubated with SARS-CoV-2 pseudovirus or live virus in the presence of varying concentrations of Alunacedase alfa. Viral entry is measured by quantifying luciferase activity (for pseudovirus) or by measuring viral RNA levels (for live virus). The compound’s ability to neutralize viral entry is calculated from dose-response curves. The IC50 for neutralization has been calculated based on the compound’s affinity for the spike glycoprotein.
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| Animal Protocol |
Alunacedase alfa has been evaluated in clinical studies in patients with severe COVID-19. In these studies, the compound was administered to hospitalized patients with severe COVID-19. The primary endpoints included safety, tolerability, and viral load reduction. Secondary endpoints included clinical improvement and mortality. The results of these studies have been published in peer-reviewed journals. The compound has also been studied in animal models of pulmonary hypertension and acute lung injury.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of Alunacedase alfa have been characterized in clinical studies. As a recombinant protein, Alunacedase alfa is expected to have pharmacokinetic properties typical of biologics, including a limited half-life and clearance through proteolytic degradation. The compound’s affinity for the SARS-CoV-2 spike glycoprotein (KD ≈ 1.2 nM) suggests that it can achieve effective target engagement at therapeutic concentrations. Further details on the compound’s pharmacokinetic parameters have not been disclosed in the available literature.
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| Toxicity/Toxicokinetics |
The safety profile of Alunacedase alfa has been evaluated in clinical studies. As a recombinant human protein, the compound is expected to have a manageable safety profile with potential immunogenicity risks. In clinical studies, the compound has been evaluated for the treatment of severe COVID-19. The safety and tolerability of Alunacedase alfa have been reported in peer-reviewed publications. Comprehensive toxicity data has not been detailed in the available literature.
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| References |
[1]. Abd El-Aziz TM, et al. Human recombinant soluble ACE2 (hrsACE2) shows promise for treating severe COVID-19. Signal Transduct Target Ther. 2020 Nov 3;5(1):258.
[2]. Zoufaly A, et al. Human recombinant soluble ACE2 in severe COVID-19. Lancet Respir Med. 2020 Nov;8(11):1154-1158. |
| Additional Infomation |
Alunacedase alfa (HrsACE2; GSK 2586881) is a human recombinant soluble angiotensin-converting enzyme 2 (hrsACE2) that binds to the SARS-CoV-2 spike glycoprotein with an affinity of approximately 1.2 nM. It reduces viral entry by competing with membrane-bound ACE2. The compound has been investigated for the treatment of severe COVID-19, pulmonary hypertension, and acute lung injury. It has been cited in publications in Signal Transduction and Targeted Therapy and The Lancet Respiratory Medicine. The compound is available as a research reagent with a purity of ≥98%.
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| CAS # |
2416824-55-8
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| Appearance |
Typically exists as solid at room temperature
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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