ARN-75039
Based on 1 Customer Validation
ARN-75039 is an orally active arenavirus inhibitor. ARN-75039 binds to sites on the GP2 subunit of the mammarenavirus glycoprotein complex, stabilizes prefusion conformation, and blocks viral entry and endosomal membrane fusion to inhibit viral replication and spread. ARN-75039 can be used for the research of lassa fever, arenaviral hemorrhagic fever, and lethal Junín virus infection.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 98.0%
- CAS. Nr.: 2436472-47-6
- Formel: C27H30N2O2
- Molecular Weight:414.54
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Beschreibung
In Vitro
ARN-75039 (1 h pretreatment) potently inhibits WT LASV and GPA LASV replication in Vero E6 cells with EC90 values ranging from 1.26 to 46 nM, is noncytotoxic at concentrations up to 25 μM, and has high selectivity indices for both viruses[1].
ARN-75039 (24 h) potently inhibits entry of pGTOV (EC50 = 0.13 nM), pCHAPV (EC50 = 4.3 nM), and pTCRV (EC50 = 0.22 nM) into Vero cells[2].
ARN-75039 (5 days) potently inhibits native TCRV replication in Vero cells with an EC50 of 0.75 nM and a selectivity index of 11,150[2].
ARN-75039 (24 h) inhibits wild-type pTCRV entry into Vero cells with an EC50 of 0.2 nM, while TCRV GP2 mutations E411K/H438R, I418N, and S433G/H438R confer complete resistance, and the T434I mutation confers partial resistance to ARN-75039[2].
ARN-75039 (5 days) has a CC50 of 8362 nM in Vero cells, resulting in a high selectivity index of 11,150 relative to its anti-TCRV activity[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
ARN-75039 (60 mg/kg loading dose; 7.5-30 mg/kg maintenance dose; p.o.; single loading dose at 7 dpe, twice daily maintenance doses for 13 days) provides 100% survival protection against lethal guinea pig-adapted Lassa virus infection in outbred Hartley guinea pigs, with minimal clinical signs and complete viral clearance by study end[1].
ARN-75039 (10-35 mg/kg; p.o.; daily; 12 days) administered prophylactically provides 100% survival protection against lethal TCRV infection in AG129 mice and completely clears viral infection from serum and tissues[2].
ARN-75039 (20-50 mg/kg; p.o.; daily; 12 days) administered therapeutically provides up to 100% survival protection against lethal TCRV infection in AG129 mice, even when treatment starts up to 7 days post-infection, and completely clears viral infection from serum and tissues[2].
ARN-75039 (60 mg/kg; p.o.; daily; starting 2 days post-challenge) administered starting 2 or 5 days post-JUNV challenge provides 100% survival in Hartley guinea pigs[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:outbred Hartley (6-week-old; male and female; inoculated intraperitoneally with 10,000 PFU of guinea pig-adapted Lassa virus)[1]
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Dosage:3.75 mg/kg; 7.5 mg/kg; 15 mg/kg; 30 mg/kg; 60 mg/kg
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Administration:p.o.; once daily; 14 days
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Result:Achieved 100% survival across the 3.75 to 60 mg/kg dose range (excluding one animal in the 15 mg/kg group with suspected unrelated comorbidities).
Maintained clinical scores of 0 or showed only temporary mild clinical signs (score of 1 for ~4 days).
Rendered plasma viremia undetectable.
Reduced infectious virus titers in spleen by 4 to 5 logs compared with placebo-treated animals, with undetectable infectious virus in all other tissues.
Reduced viral genomic RNA copies in tissues by 2 to 5 logs compared with placebo-treated animals.
Showed no LASV-related pathological lesions in most treated animals, with minimal severity in those that had lesions compared with placebo-treated animals.
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Animal Model:outbred Hartley (6-week-old; male and female; inoculated intraperitoneally with 10,000 PFU of guinea pig-adapted Lassa virus)[1]
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Dosage:7.5 mg/kg; 15 mg/kg; 30 mg/kg; 60 mg/kg
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Administration:p.o.; single loading dose at 7 dpe, twice daily maintenance doses for 13 days; total 14 days
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Result:Achieved 100% survival at the 7.5 mg/kg twice-daily dose.
Showed only mild clinical signs (score of 1) for 3 to 5 days before returning to 0, with no weight loss in the 7.5 mg/kg twice-daily group.
Rendered plasma viremia undetectable.
Reduced infectious virus titers in spleen (up to 6.4 × 104 PFU/mL) compared with placebo-treated animals, with undetectable infectious virus in most tissues.
Reduced viral genomic RNA copies in tissues significantly (P ≤ 0.003) compared with placebo-treated animals.
Detected no infectious virus in any plasma or tissue samples from surviving treated animals at terminal necropsy, with minimal or absent pathological lesions compared with placebo-treated animals.
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Animal Model:AG129 (IFN-α/β and γ receptor-deficient; 6 to 8-week-old; male and female; Tacaribe virus challenge)[2]
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Dosage:10 mg/kg; 35 mg/kg
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Administration:p.o.; daily; 12 days
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Result:Provided 100% survival protection against TCRV-associated mortality.
Showed little to no weight loss during acute infection.
Achieved undetectable TCRV titers in serum, liver, and spleen samples on day 9 post-infection.
Resulted in undetectable TCRV titers in serum, liver, spleen, and brain at study termination, indicating complete clearance of infection.
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Animal Model:Hartley (4- to 6-week-old, equal numbers of male and female)[3]
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Dosage:60 mg/kg
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Administration:p.o.; daily; starting 2/5 days post-challenge
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Result:Provided complete protection (100% survival) against lethal JUNV disease.
Chemical Information
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CAS. Nr. 2436472-47-6
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Appearance Solid
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Molecular Weight 414.54
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Formel C27H30N2O2
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Color White to off-white
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SMILES
CC1=CC2=NC=C(N2C=C1C3=CC=C(C=C3)OC(C)C)C4=CC=C(C=C4)OC(C)(C)C
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 100 mg/mL (241.23 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.03 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.03 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation
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Data Sheet (283 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Eudy E, et al. The virus entry inhibitor ARN-75039 provides therapeutic protection against Lassa virus infection in guinea pigs. Sci Transl Med. 2026;18(845):eadx0938. [Content Brief]
[2]. Gowen BB, et al. Potent inhibition of arenavirus infection by a novel fusion inhibitor. Antiviral Res. 2021 Sep;193:105125. [Content Brief]
[3]. Westover JB, et al. Coadministration of LHF-535 and favipiravir protects against experimental Junín virus infection and disease. Antiviral Res. 2024;229:105952. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.4123 mL | 12.0616 mL | 24.1231 mL | 60.3078 mL |
| 5 mM | 0.4825 mL | 2.4123 mL | 4.8246 mL | 12.0616 mL | |
| 10 mM | 0.2412 mL | 1.2062 mL | 2.4123 mL | 6.0308 mL | |
| 15 mM | 0.1608 mL | 0.8041 mL | 1.6082 mL | 4.0205 mL | |
| 20 mM | 0.1206 mL | 0.6031 mL | 1.2062 mL | 3.0154 mL | |
| 25 mM | 0.0965 mL | 0.4825 mL | 0.9649 mL | 2.4123 mL | |
| 30 mM | 0.0804 mL | 0.4021 mL | 0.8041 mL | 2.0103 mL | |
| 40 mM | 0.0603 mL | 0.3015 mL | 0.6031 mL | 1.5077 mL | |
| 50 mM | 0.0482 mL | 0.2412 mL | 0.4825 mL | 1.2062 mL | |
| 60 mM | 0.0402 mL | 0.2010 mL | 0.4021 mL | 1.0051 mL | |
| 80 mM | 0.0302 mL | 0.1508 mL | 0.3015 mL | 0.7538 mL | |
| 100 mM | 0.0241 mL | 0.1206 mL | 0.2412 mL | 0.6031 mL |
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