| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
Inarigivir soproxil targets the innate immune system by activating the RIG-I (retinoic acid-inducible gene I) and NOD2 (nucleotide-binding oligomerization domain-containing protein 2) pathways. It is a prodrug form of SB-9000. By activating these pathways, it stimulates the production of interferons and other antiviral cytokines, enhancing the host's immune response against viral infections. It is an oral agonist of innate immunity.
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| ln Vitro |
First-in-class oral innate immune modulator inarigivir soproxil (SB 9200) works by stimulating the RIG-I and NOD2 pathways [1]. A strong inhibitor of HCV replication in cell culture is inarigivir soproxil. In repeat studies with four medication concentrations, the antiviral efficacy of inarigivir soproxil against HCV was assessed using the genotype 1 HCV replicon system. With EC50s of 2.2 and 1.0 µM and EC90s of 8.0 and 6.0 µM for genotypes 1A and 1B, respectively, inarigivir soproxil suppresses HCV replication [1]. An oral bioavailable dinucleotide called inarigivir soproxil (SB 9200) stimulates the interferon (IFN) signaling cascade of antiviral defense by activating viral sensor proteins, retinoic acid-inducible gene 1 (RIG-I), and nucleotide-binding oligomerization domain-containing protein 2 (NOD2) [2].
Inarigivir soproxil is a first-in-class oral modulator of innate immunity that activates the RIG-I and NOD2 pathways. It is an effective inhibitor of HCV replication in cell culture. It has broad-spectrum antiviral activity against RNA viruses including HCV, norovirus, RSV, and influenza, and has activity against HBV in vitro and in vivo. Its activity has been confirmed in various in vitro and in vivo studies. |
| ln Vivo |
Pretreatment with Inarigivir soproxil (SB 9200) and later entecavir (ETV) causes a host immune response, and its antiviral efficacy is superior than the method of utilizing ETV to minimize post-viral immune regulation [2]. Sequential treatment of chronic WHV carrier woodchucks with Inarigivir soproxil (30 mg/kg) followed by ETV elicited considerable decrease of serum viremia and antigenemia compared with sequential therapy with ETV followed by Inarigivir soproxil , and delay the resumption of viral replication [2].
Inarigivir soproxil has broad-spectrum antiviral activity against RNA viruses including HCV, norovirus, respiratory syncytial virus, and influenza, and has demonstrated activity against HBV in vitro and in vivo. It is an oral modulator of innate immunity that acts via the activation of the RIG-I and NOD2 pathways. It has been investigated for the treatment of viral infections, including HCV and HBV. |
| Enzyme Assay |
The primary in vitro assays for Inarigivir soproxil measure its antiviral activity against various viruses in cell culture. HCV replicon cells or virus-infected cells are treated with the compound, and viral replication is measured by quantifying viral RNA or protein levels. The EC50 values for inhibition of viral replication are determined. Its effects on innate immune signaling, such as interferon production, are measured by ELISA or qPCR.
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| Cell Assay |
In vitro cellular experiments for Inarigivir soproxil involve treating cells with the compound and measuring its effects on RIG-I and NOD2 activation and downstream signaling. The activation of these pathways is assessed by measuring the phosphorylation of downstream signaling molecules and the expression of interferon-stimulated genes. The antiviral activity is assessed in virus-infected cell cultures.
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| Animal Protocol |
Animal/Disease Models: woodchucks chronically infected with woodchuck hepatitis virus (WHV) [2]
Doses: 30 mg/kg Route of Administration: Orally, one time/day; Group 1 received ETV treatment for 4 weeks, followed by Inarigivir soproxil treatment 12 weeks. Group 2 received Inarigivir soproxil for 12 weeks, followed by ETV for 4 weeks. Experimental Results: The liver WHV nucleic acid levels of patients in both groups were Dramatically diminished, and Group 2 was more obvious. In vivo animal experiments for Inarigivir soproxil have been conducted in animal models of viral infection to assess its antiviral efficacy. The compound is administered orally, and its effects on viral load, immune responses, and disease progression are assessed. Its pharmacokinetic properties are also characterized in these studies. |
| ADME/Pharmacokinetics |
Inarigivir soproxil has a molecular weight of 703.62 and a molecular formula of C25H34N7O13PS. It is also known as SB 9200 and GS 9992. The compound has a CAS number of 942123-43-5. It is a first-in-class oral modulator of innate immunity and a prodrug form of SB-9000.
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| Toxicity/Toxicokinetics |
Inarigivir soproxil is a research compound that is not intended for human use. Its toxicological profile is not extensively characterized in the available literature. As an immune modulator, it may have potential immune-related adverse effects. Its safety would need to be established for therapeutic applications.
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| References |
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| Additional Infomation |
Inarigivir soproxil is being studied in the clinical trial NCT03434353 (a study evaluating the antiviral activity of Inarigivir (GS-9992) plus tenofovir alafenamide (TAF) for 12 weeks in adult patients with chronic hepatitis B (CHB).
Inarigivir soproxil (SB 9200) is a first-in-class oral modulator of innate immunity that acts via the activation of the RIG-I and NOD2 pathways. It is an effective inhibitor of HCV replication and has broad-spectrum antiviral activity against RNA viruses including HCV, norovirus, RSV, and influenza, and has activity against HBV in vitro and in vivo. |
| Molecular Formula |
C26H38N7O12PS
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|---|---|
| Molecular Weight |
703.6608
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| Exact Mass |
703.167
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| Elemental Analysis |
C, 44.38; H, 5.44; N, 13.93; O, 27.28; P, 4.40; S, 4.56
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| CAS # |
942123-43-5
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| Related CAS # |
942123-43-5 (soproxil);475650-36-3 (free);2172788-92-8 (ammonium);
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| PubChem CID |
24737742
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| Appearance |
White to off-white solid powder
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| Density |
1.8±0.1 g/cm3
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| Index of Refraction |
1.732
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| LogP |
-0.66
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
18
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| Rotatable Bond Count |
15
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| Heavy Atom Count |
47
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| Complexity |
1220
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| Defined Atom Stereocenter Count |
7
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| SMILES |
O([C@@H]1[C@H](OP(=O)(SCOC(=O)OC(C)C)OC[C@@H]2[C@@H](O)C[C@H](N3C=NC4C(=NC=NC3=4)N)O2)[C@@H](CO)O[C@H]1N1C=CC(=O)NC1=O)C
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| InChi Key |
VINVIVOICCZWKJSHV-OLTNJDQQSA-N
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| InChi Code |
InChI=1S/C26H38N7O12PS/c1-5-15-20(21(39-4)24(44-15)32-7-6-17(35)31-25(32)36)45-46(38,47-12-40-26(37)42-13(2)3)41-9-16-14(34)8-18(43-16)33-11-30-19-22(27)28-10-29-23(19)33/h10-11,13-16,18,20-21,24,34H,5-9,12H2,1-4H3,(H2,27,28,29)(H,31,35,36)/t14-,15+,16-,18-,20+,21+,24+,46?/m0/s1
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| Chemical Name |
(((((2S,3S,5S)-5-(6-amino-9H-purin-9-yl)-3-hydroxytetrahydrofuran-2-yl)methoxy)(((2R,3R,4R,5R)-5-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-2-ethyl-4-methoxytetrahydrofuran-3-yl)oxy)phosphoryl)thio)methyl isopropyl carbonate
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| Synonyms |
Inarigivir soproxil; SB 44 (dinucleotide); SB 9200; SB-9200; SB9200.
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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 Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| 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) |
DMSO : ~80 mg/mL (~113.70 mM)
H2O : ~10 mg/mL (~14.21 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (7.11 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 2: ≥ 4 mg/mL (5.68 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 40.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 4 mg/mL (5.68 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 2.5 mg/mL (3.55 mM) (saturation unknown) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 5: (saturation unknown) in 10% DMSO+90% Corn Oil: ≥ 5 mg/mL (7.11 mM) (add these co-solvents sequentially from left to right, and one by one), Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.4211 mL | 7.1057 mL | 14.2114 mL | |
| 5 mM | 0.2842 mL | 1.4211 mL | 2.8423 mL | |
| 10 mM | 0.1421 mL | 0.7106 mL | 1.4211 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
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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