Inarigivir

Alias: Inarigivir soproxil; ORI-9020; ORI 9020; ORI9020; SB-40; SB-9000; SB9000, SB-9000.
Cat No.:V4627 Purity: ≥98%
Inarigivir (formerly also known as ORI-9020; SB-9000) is a novel and potent dinucleotide which can significantly reduce liver HBV DNA in transgenic mice expressing hepatitis B virus.
Inarigivir Chemical Structure CAS No.: 475650-36-3
Product category: New7
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
1mg
Other Sizes

Other Forms of Inarigivir:

  • Inarigivir ammonium (ORI-9020 ammonium; SB-9000 ammonium)
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Inarigivir (formerly also known as ORI-9020; SB-9000) is a novel and potent dinucleotide which can significantly reduce liver HBV DNA in transgenic mice expressing hepatitis B virus. It was evaluated in transgenic mice expressing hepatitis B virus (HBV), significantly reduced liver HBV DNA (P

Biological Activity I Assay Protocols (From Reference)
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].
ln Vivo
Inarigivir (100 mg/kg/day, i.p.) shown anti-HBV efficacy and markedly decreased the amount of viral DNA in the liver. Treatment has no effect on the level of serum HBV DNA. Serum HBeAg levels, mean HBsAg titers, and liver HBV RNA levels were all unaffected by inarigivir. Based on liver HBV DNA levels, the lowest effective dose is 1.6 to 0.5 mg/kg/day [1].
Animal Protocol
Animal/Disease Models: Mice[1]
Doses: 100 mg/kg. Management: IP, daily.
Experimental Results: Viral DNA was Dramatically diminished in the liver and demonstrated anti-HBV activity similar to the ADV positive control.
References
[1]. Iyer RP, et al. Anti-hepatitis B virus activity of ORI-9020, a novel phosphorothioate dinucleotide, in a transgenic mouse model. Antimicrob Agents Chemother. 2004 Jun;48(6):2318-20.
[2]. Danni Colledge, et al. The Novel Antiviral Agent Inarigivir Inhibits Both Nucleos(t)ide Analogue and Capsid Assembly Inhibitor Resistant HBV in vitro.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C20H26N7O10PS
Molecular Weight
587.500103473663
CAS #
475650-36-3
Related CAS #
Inarigivir ammonium;2172788-92-8
SMILES
O=P(OC[C@H]1O[C@@H](N2C=NC3=C(N)N=CN=C23)C[C@@H]1O)(S)O[C@@H]4[C@@H](CO)O[C@@H](N(C(N5)=O)C=CC5=O)[C@@H]4OC
InChi Key
LYMICVBGNUEHGE-FUQPUAIBSA-N
InChi Code
InChI=1S/C20H26N7O10PS/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)/t9-,10+,11+,13+,15+,16+,19+,38?/m0/s1
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
Synonyms
Inarigivir soproxil; ORI-9020; ORI 9020; ORI9020; SB-40; SB-9000; SB9000, SB-9000.
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)
Solubility Data
Solubility (In Vitro)
DMSO : ~200 mg/mL (~340.43 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.26 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 2: ≥ 2.5 mg/mL (4.26 mM) (saturation unknown) in 5% DMSO + 95% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
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.

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Solubility in Formulation 3: ≥ 0.25 mg/mL (0.43 mM) (saturation unknown) in 1% DMSO 99% 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.


 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.7021 mL 8.5106 mL 17.0213 mL
5 mM 0.3404 mL 1.7021 mL 3.4043 mL
10 mM 0.1702 mL 0.8511 mL 1.7021 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.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

  • Calculate the Mass of a compound required to prepare a solution of known volume and concentration
  • Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume
An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
  • Click the “Calculate” button
  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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.

Biological Data
  • Inarigivir


    Southern blot hybridization for HBV DNA in the livers of mice treated i.p. with ORI-9020, ADV, or vehicle only.. 2004 Jun; 48(6): 2318–2320.

  • Inarigivir


    Determination of minimal effective concentration of ORI-9020 using liver HBV DNA parameter in transgenic mice.. 2004 Jun; 48(6): 2318–2320.

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