| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
Target: HBV[1].
Inarigivir ammonium targets the RIG-I (Retinoic acid-inducible gene-I) pathway. RIG-I is a cytosolic pattern recognition receptor that detects viral RNA and activates innate immune responses. By acting as a RIG-I agonist, Inarigivir ammonium triggers the production of type I interferons and other cytokines, enhancing the host's antiviral defense. The compound is developed as an orally administered antiviral immunomodulator for treating chronic hepatitis B virus (HBV) infection. |
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| ln Vitro |
The nucleos(t)ide analogs authorized for the treatment of chronic hepatitis B are all susceptible to resistance markers when it comes to HBV variations that are active against inarigivir (SB 9200)[2].
In vitro, Inarigivir ammonium decreases extracellular HBV DNA and intracellular HBV RNA levels in HepG2 2.2.15 cells with EC50s of 0.258 and 1.4 µM, respectively. It shows no cytotoxicity with a CC50 value of >1,000 µM. As a RIG-I agonist, it activates cellular innate immune responses. These in vitro activities support its potential as an antiviral agent for treating chronic hepatitis B virus infection. |
| ln Vivo |
Inarigivir (100 mg/kg/day, i.p.) exhibits anti-HBV action and dramatically lowers viral DNA in the liver. Treatment does not result in a decrease in serum HBV DNA. HBV RNA levels in the liver, HBeAg levels in the blood, and mean titers of HBsAg are unaffected by inarigivir. Based on liver HBV DNA levels, the lowest effective dose is shown to be between 1.6 and 0.5 mg/kg/day[1].
In vivo, Inarigivir ammonium significantly reduces liver HBV DNA in transgenic mice expressing hepatitis B virus. As an orally administered RIG-I agonist, it activates innate immune responses to combat viral infection. These results support its potential for treating chronic hepatitis B virus infection. The compound has been investigated in clinical studies for its antiviral efficacy and safety profile. |
| Enzyme Assay |
The in vitro antiviral assay for Inarigivir ammonium is conducted in HepG2 2.2.15 cells, which express HBV. Cells are treated with varying concentrations of the compound, and extracellular HBV DNA and intracellular HBV RNA levels are measured using qPCR or other quantitative methods. EC50 values are calculated from dose-response curves. Cytotoxicity is assessed using standard cell viability assays to determine CC50 values. RIG-I activation is confirmed by measuring downstream signaling markers.
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| Cell Assay |
Cellular assays for Inarigivir ammonium are conducted in HepG2 2.2.15 cells. Cells are treated with varying concentrations of the compound. HBV DNA and RNA levels are quantified using qPCR. Cell viability is assessed using standard assays such as MTT to determine CC50 values. RIG-I pathway activation is evaluated by measuring interferon and cytokine production. The compound's immunomodulatory effects are assessed in immune cell models.
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| Animal Protocol |
Animal/Disease Models: Mice[1]
Doses: 100 mg/kg. Route of Administration: IP, daily. Experimental Results: Dramatically diminished viral DNA in the liver and shows anti-HBV activity similar ADV positive control. In vivo studies for Inarigivir ammonium are conducted in transgenic mice expressing hepatitis B virus. The compound is administered orally at doses determined by pharmacokinetic studies. Efficacy is assessed by measuring liver HBV DNA levels and other viral parameters. Pharmacodynamic markers such as interferon and cytokine levels are measured to confirm RIG-I pathway activation. Clinical studies have also been conducted in HBV-infected patients. |
| ADME/Pharmacokinetics |
Inarigivir ammonium is orally administered with favorable pharmacokinetic properties. It has a molecular weight of 604.53 g/mol and a molecular formula of C20H29N8O10PS. As a dinucleotide antiviral drug, it is expected to have good oral bioavailability. The compound is a RIG-I agonist that activates innate immune responses. Detailed PK parameters such as half-life and bioavailability are not extensively reported in the available literature.
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| Toxicity/Toxicokinetics |
Toxicity data for Inarigivir ammonium shows no cytotoxicity in HepG2 2.2.15 cells with a CC50 value of >1,000 µM. As with all research compounds, Inarigivir ammonium is intended for research use only and not for human therapeutic applications outside of approved clinical trials. The compound's safety profile has been evaluated in clinical studies for chronic hepatitis B treatment. Comprehensive toxicology studies are required for therapeutic development.
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| References |
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| Additional Infomation |
Inarigivir ammonium (ORI-9020 ammonium) is a dinucleotide antiviral drug and RIG-I agonist that activates cellular innate immune responses. It significantly reduces liver HBV DNA in transgenic mice expressing hepatitis B virus. In vitro, it decreases extracellular HBV DNA and intracellular HBV RNA in HepG2 2.2.15 cells (EC50s = 0.258 and 1.4 µM) without cytotoxicity (CC50 >1,000 µM). It has a molecular weight of 604.53 g/mol. Inarigivir ammonium is developed as an orally administered antiviral immunomodulator for chronic hepatitis B.
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| Molecular Formula |
C20H29N8O10PS
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|---|---|
| Molecular Weight |
604.5306
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| Exact Mass |
604.146
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| Elemental Analysis |
C, 39.74; H, 4.84; N, 18.54; O, 26.47; P, 5.12; S, 5.30
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| CAS # |
2172788-92-8
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| Related CAS # |
Inarigivir;475650-36-3
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| PubChem CID |
162623408
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| Appearance |
White to light yellow solid powder
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
16
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
40
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| Complexity |
1010
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| Defined Atom Stereocenter Count |
7
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| SMILES |
S=P(O)(OC[C@@H]1[C@H](C[C@H](N2C=NC3=C(N)N=CN=C23)O1)O)O[C@@H]1[C@@H](CO)O[C@H]([C@@H]1OC)N1C=CC(NC1=O)=O.N
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| InChi Key |
CAUBLFJDYDLFRY-NJCNYLKWSA-N
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| InChi Code |
InChI=1S/C20H26N7O10PS.H3N/c1-33-16-15(10(5-28)36-19(16)26-3-2-12(30)25-20(26)31)37-38(32,39)34-6-11-9(29)4-13(35-11)27-8-24-14-17(21)22-7-23-18(14)27;/h2-3,7-11,13,15-16,19,28-29H,4-6H2,1H3,(H,32,39)(H2,21,22,23)(H,25,30,31);1H3/t9-,10+,11+,13+,15+,16+,19+,38?;/m0./s1
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| Chemical Name |
O-(((2R,3S,5R)-5-(6-amino-9H-purin-9-yl)-3-hydroxytetrahydrofuran-2-yl)methyl) O-((2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-2-(hydroxymethyl)-4-methoxytetrahydrofuran-3-yl) S-hydrogen phosphorothioate, ammonia salt
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| Synonyms |
Inarigivir ammonium; ORI-9020; ORI 9020; ORI9020; SB-40; SB-9000; SB9000, SB-9000.
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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: Please store this product in a sealed and protected environment, 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) |
H2O : 100 mg/mL (165.42 mM)
DMSO : 100 mg/mL (165.42 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (165.42 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6542 mL | 8.2709 mL | 16.5418 mL | |
| 5 mM | 0.3308 mL | 1.6542 mL | 3.3084 mL | |
| 10 mM | 0.1654 mL | 0.8271 mL | 1.6542 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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