Astodrimer (SPL7013 free base) is a large (3-4 nm, ~16.5 kDa), negatively charged, highly branched dendrimer that is a potent virucidal agent. Astodrimer has antiviral and virucidal activity against a broad spectrum of viruses including SARS-CoV-2, HIV-1, HSV-1, HSV-2, and HPV. Astodrimer also has antibacterial properties.

Physicochemical Properties

CAS #	1379746-42-5
Appearance	Typically exists as solid at room temperature
HS Tariff Code	2934.99.9001
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)

Biological Activity

ln Vitro	Astodrimer (0–10 mg/mL; 4 days) suppresses the replication of SARS-CoV-2 (hCoV-19/Australia/VIC01/2020) when it infects Vero E6 cells[1]. Astodrimer suppresses the 2019-nCoV/USA-WA1/2020 strain of the infectious virus in Vero E6 cells and Calu-3 cells, respectively, with EC50 values of 0.019–0.032 mg/mL and 0.030–0.037 mg/mL [1].
ln Vivo	Astodrimer (3%, administered eight times a day for four days, followed by four times a day for six days) shows anti-adenoviral activity in NZW rabbits and is not harmful to rabbit eyes[2]. The highly vulnerable K18-hACE2 mouse model's SARS-CoV-2 proliferation and pathology is lessened by intratradical injection of astodrimer (1%; once daily for five days)[3].
Cell Assay	Cell Proliferation Assay[1] Cell Types: Vero E6 cells Tested Concentrations: 0-10 mg/mL(1 h prior to infection, or 1 h post-infection with SARS-CoV-2) Incubation Duration: 4 days Experimental Results: Inhibited viral replication when added either 1 h prior to infection, or 1 h post-infection with SARS-CoV-2 in a dose dependent manner.
Animal Protocol	Animal/Disease Models: Two- to three-pound female NZW rabbits (both eyes with HAdV5 following corneal scarification)[2]. Doses: 3% SPL7013 Route of Administration: 8 times daily for 4 days then 4 times daily for 6 days Experimental Results: Inactivated the virus, and the resulting reduction in the exposure to the virus in vivo limits SARS-CoV-2 infection, resulting in Dramatically lower viral loads and infectious virus in the lung, trachea, brain and liver of K18-hACE2 mic, and Dramatically lower pro-inflammatory cytokine production. Animal/Disease Models: Six-to-eightweeks old K18-hACE2 mice[3] Doses: 1% astodrimer sodium nasal spray Route of Administration: Intranasal administration; 25 µL/nostril; one time/day on Days 1-6. Experimental Results: Dramatically diminished the severity of SARS-CoV-2 replication and pathogenesis in the highly susceptible K18-hACE2 mouse model.
References	[1]. Virucidal and antiviral activity of astodrimer sodium against SARS-CoV-2 in vitro. Antiviral Res. 2021 Jul;191:105089. [2]. Topical Astodrimer Sodium, a Non-Toxic Polyanionic Dendrimer, Demonstrates Antiviral Activity in an Experimental Ocular Adenovirus Infection Model. Molecules. 2021 Jun 5;26(11):3419.

Solubility Data

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

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 (e.g. IP/IV/IM/SC) Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline) *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). 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)] *Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline) Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline) Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline) Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil) Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL 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). Oral Formulation 3: Dissolved in PEG400 Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose Oral Formulation 6: Mixing with food powders Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.  (Please use freshly prepared in vivo formulations for optimal results.)