1. Anti-infection Cell Cycle/DNA Damage PI3K/Akt/mTOR
  2. HBV Orthopoxvirus HSV DNA/RNA Synthesis ATM/ATR CDK
  3. Adefovir dipivoxil

Adefovir dipivoxil  (Synonyms: GS 0840)

Cat. No.: HY-B0255 Purity: 99.03%
Handling Instructions Technical Support

Adefovir dipivoxil is an orally active adenosine analog and Adefovir prodrug. Adefovir dipivoxil inhibits DNA synthesis, activates the ATR signaling pathway, and disrupts the KCTD12-CDK1 interaction. Adefovir dipivoxil has antiviral activity against PRV, HBV, and orthopoxviruses. Adefovir dipivoxil has inhibitory effects on both lamivudine-resistant and wild-type strains. Adefovir dipivoxil has antitumor activity against lung and colon cancer.

For research use only. We do not sell to patients.

Adefovir dipivoxil Chemical Structure

Adefovir dipivoxil Chemical Structure

CAS No. : 142340-99-6

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Adefovir dipivoxil is an orally active adenosine analog and Adefovir prodrug. Adefovir dipivoxil inhibits DNA synthesis, activates the ATR signaling pathway, and disrupts the KCTD12-CDK1 interaction. Adefovir dipivoxil has antiviral activity against PRV, HBV, and orthopoxviruses. Adefovir dipivoxil has inhibitory effects on both lamivudine-resistant and wild-type strains. Adefovir dipivoxil has antitumor activity against lung and colon cancer[1][2][3][4][5][6][7][8][9][10][11].

Cellular Effect
Cell Line Type Value Description References
CCRF-CEM EC50
0.045 μM
Compound: 11, Bis-POM-PMEA
Antiviral activity against wild type HIV-1 3B infected in human CEM cells assessed as inhibition of syncytia formation after 4 days by microscopic analysis
Antiviral activity against wild type HIV-1 3B infected in human CEM cells assessed as inhibition of syncytia formation after 4 days by microscopic analysis
[PMID: 23603046]
CCRF-CEM EC50
0.062 μM
Compound: 11, Bis-POM-PMEA
Antiviral activity against wild type HIV-2 ROD infected in human CEM cells assessed as inhibition of syncytia formation after 4 days by microscopic analysis
Antiviral activity against wild type HIV-2 ROD infected in human CEM cells assessed as inhibition of syncytia formation after 4 days by microscopic analysis
[PMID: 23603046]
HEK293 IC50
13.5 μM
Compound: ADV
Inhibition of human OAT1 expressed in HEK293 cells assessed as P-amino hippuric acid uptake inhibition incubated for 10 mins by UPLC-MS/MS method
Inhibition of human OAT1 expressed in HEK293 cells assessed as P-amino hippuric acid uptake inhibition incubated for 10 mins by UPLC-MS/MS method
[PMID: 31301948]
HEL EC50
0.2 μM
Compound: 11, Bis-POM-PMEA
Antiviral activity against Human simplex virus 2 G infected in human HEL cells assessed as reduction of virus-induced cytopathicity measured at day 3 by microscopic analysis
Antiviral activity against Human simplex virus 2 G infected in human HEL cells assessed as reduction of virus-induced cytopathicity measured at day 3 by microscopic analysis
[PMID: 23603046]
HEL EC50
0.2 μM
Compound: 11, Bis-POM-PMEA
Antiviral activity against thymidine kinase-deficient Human simplex virus 1 KOS infected in human HEL cells assessed as reduction of virus-induced cytopathicity measured at day 3 by microscopic analysis
Antiviral activity against thymidine kinase-deficient Human simplex virus 1 KOS infected in human HEL cells assessed as reduction of virus-induced cytopathicity measured at day 3 by microscopic analysis
[PMID: 23603046]
HEL EC50
0.2 μM
Compound: 11, Bis-POM-PMEA
Antiviral activity against Human simplex virus 1 KOS infected in human HEL cells assessed as reduction of virus-induced cytopathicity measured at day 3 by microscopic analysis
Antiviral activity against Human simplex virus 1 KOS infected in human HEL cells assessed as reduction of virus-induced cytopathicity measured at day 3 by microscopic analysis
[PMID: 23603046]
HEL EC50
4 μM
Compound: 11, Bis-POM-PMEA
Antiviral activity against Vaccinia virus infected in human HEL cells assessed as reduction of virus-induced cytopathicity measured at day 3 by microscopic analysis
Antiviral activity against Vaccinia virus infected in human HEL cells assessed as reduction of virus-induced cytopathicity measured at day 3 by microscopic analysis
[PMID: 23603046]
HepG2 2.2.15 CC50
> 400 μM
Compound: ADV
Toxicity against human HepG2.2.15 cells infected with HBV after 72 hrs by MTT assay
Toxicity against human HepG2.2.15 cells infected with HBV after 72 hrs by MTT assay
[PMID: 27458783]
HepG2 2.2.15 IC50
0.33 μM
Compound: 2
Antiviral activity against Hepatitis B virus infected HepG2(2.2.15) cells assessed as inhibition of viral cytoplasmic DNA synthesis by real-time PCR
Antiviral activity against Hepatitis B virus infected HepG2(2.2.15) cells assessed as inhibition of viral cytoplasmic DNA synthesis by real-time PCR
[PMID: 19889538]
HepG2 2.2.15 IC50
0.48 μM
Compound: ADV
Antiviral activity against Hepatitis B virus infected human HepG2(2.2.15) cells assessed as viral DNA level after 9 days by southern blot analysis
Antiviral activity against Hepatitis B virus infected human HepG2(2.2.15) cells assessed as viral DNA level after 9 days by southern blot analysis
10.1007/s00044-011-9616-2
HepG2 2.2.15 IC50
0.58 μM
Compound: ADV
Antiviral activity against Hepatitis B virus infected human HepG2(2.2.15) cells assessed as inhibition of viral DNA replication after 9 days by RT-PCR analysis
Antiviral activity against Hepatitis B virus infected human HepG2(2.2.15) cells assessed as inhibition of viral DNA replication after 9 days by RT-PCR analysis
10.1007/s00044-011-9616-2
HepG2 2.2.15 EC50
0.96 μM
Compound: 1
Antiviral activity against Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as inhibition of viral replication incubated for 2 days followed by wash out measured after 10 days by RT-PCR analysis
Antiviral activity against Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as inhibition of viral replication incubated for 2 days followed by wash out measured after 10 days by RT-PCR analysis
[PMID: 22305613]
HepG2 2.2.15 EC50
1.5 μM
Compound: ADV
Antiviral activity against wild type HBV infected in HepG2.2.15 cells assessed as nucleic acid and protein levels dosed daily for 9 days and measured 24 hrs after last treatment by Southern blot hybridization
Antiviral activity against wild type HBV infected in HepG2.2.15 cells assessed as nucleic acid and protein levels dosed daily for 9 days and measured 24 hrs after last treatment by Southern blot hybridization
[PMID: 20117930]
HepG2 2.2.15 EC50
1.8 μM
Compound: ADV
Antiviral activity against 3TC-resistant HBV with polymerase M204V mutation infected in HepG2.2.15 cells assessed as nucleic acid and protein levels dosed daily for 9 days and measured 24 hrs after last treatment by Southern blot hybridization
Antiviral activity against 3TC-resistant HBV with polymerase M204V mutation infected in HepG2.2.15 cells assessed as nucleic acid and protein levels dosed daily for 9 days and measured 24 hrs after last treatment by Southern blot hybridization
[PMID: 20117930]
HepG2 2.2.15 EC50
2 μM
Compound: ADV
Antiviral activity against 3TC-resistant HBV with polymerase M204I mutation infected in HepG2.2.15 cells assessed as nucleic acid and protein levels dosed daily for 9 days and measured 24 hrs after last treatment by Southern blot hybridization
Antiviral activity against 3TC-resistant HBV with polymerase M204I mutation infected in HepG2.2.15 cells assessed as nucleic acid and protein levels dosed daily for 9 days and measured 24 hrs after last treatment by Southern blot hybridization
[PMID: 20117930]
HepG2 2.2.15 EC50
2.1 μM
Compound: ADV
Antiviral activity against 3TC-resistant HBV with polymerase L180M mutation infected in HepG2.2.15 cells assessed as nucleic acid and protein levels dosed daily for 9 days and measured 24 hrs after last treatment by Southern blot hybridization
Antiviral activity against 3TC-resistant HBV with polymerase L180M mutation infected in HepG2.2.15 cells assessed as nucleic acid and protein levels dosed daily for 9 days and measured 24 hrs after last treatment by Southern blot hybridization
[PMID: 20117930]
HepG2 2.2.15 EC50
2.2 μM
Compound: ADV
Antiviral activity against 3TC-resistant HBV with polymerase LMMV mutation infected in HepG2.2.15 cells assessed as nucleic acid and protein levels dosed daily for 9 days and measured 24 hrs after last treatment by Southern blot hybridization
Antiviral activity against 3TC-resistant HBV with polymerase LMMV mutation infected in HepG2.2.15 cells assessed as nucleic acid and protein levels dosed daily for 9 days and measured 24 hrs after last treatment by Southern blot hybridization
[PMID: 20117930]
HepG2 2.2.15 CC50
438.92 μM
Compound: ADV
Cytotoxicity against human HepG2.2.15 cells assessed as reduction in cell viability incubated for 12 hrs followed by replacement of fresh medium containing compound and measured after 2 days by CCK-8 assay
Cytotoxicity against human HepG2.2.15 cells assessed as reduction in cell viability incubated for 12 hrs followed by replacement of fresh medium containing compound and measured after 2 days by CCK-8 assay
[PMID: 31301948]
HepG2 2.2.15 EC50
7.5 μM
Compound: ADV
Antiviral activity against ADV-resistant HBV N236T mutation infected in HepG2.2.15 cells assessed as nucleic acid and protein levels dosed daily for 9 days and measured 24 hrs after last treatment by Southern blot hybridization
Antiviral activity against ADV-resistant HBV N236T mutation infected in HepG2.2.15 cells assessed as nucleic acid and protein levels dosed daily for 9 days and measured 24 hrs after last treatment by Southern blot hybridization
[PMID: 20117930]
HK-2 CC50
488.05 μM
Compound: 1
Cytotoxicity against human HK2 cells by MTT assay
Cytotoxicity against human HK2 cells by MTT assay
[PMID: 22305613]
Huh-7 EC50
0.83 μM
Compound: 11, Bis-POM-PMEA
Antiviral activity against wild type HBV transfected in human HuH7 cells assessed as reduction of viral DNA level after 7 days by qPCR analysis
Antiviral activity against wild type HBV transfected in human HuH7 cells assessed as reduction of viral DNA level after 7 days by qPCR analysis
[PMID: 23603046]
Huh-7 EC50
1.5 μM
Compound: Adefovir dipivoxil
Antiviral activity against HBV harboring RNA polymerase M204V mutant gene infected in human HuH7 cells assessed as decrease in viral transient transfection after 24 hrs
Antiviral activity against HBV harboring RNA polymerase M204V mutant gene infected in human HuH7 cells assessed as decrease in viral transient transfection after 24 hrs
[PMID: 19398648]
Huh-7 EC50
14 μM
Compound: Adefovir dipivoxil
Antiviral activity against HBV harboring RNA polymerase N236T mutant gene infected in human HuH7 cells assessed as decrease in viral transient transfection after 24 hrs
Antiviral activity against HBV harboring RNA polymerase N236T mutant gene infected in human HuH7 cells assessed as decrease in viral transient transfection after 24 hrs
[PMID: 19398648]
Huh-7 EC50
2 μM
Compound: Adefovir dipivoxil
Antiviral activity against wild type HBV infected in human HuH7 cells assessed as decrease in viral transient transfection after 24 hrs
Antiviral activity against wild type HBV infected in human HuH7 cells assessed as decrease in viral transient transfection after 24 hrs
[PMID: 19398648]
Huh-7 EC50
2.4 μM
Compound: Adefovir dipivoxil
Antiviral activity against HBV harboring RNA polymerase M204I mutant gene infected in human HuH7 cells assessed as decrease in viral transient transfection after 24 hrs
Antiviral activity against HBV harboring RNA polymerase M204I mutant gene infected in human HuH7 cells assessed as decrease in viral transient transfection after 24 hrs
[PMID: 19398648]
Huh-7 EC50
2.5 μM
Compound: Adefovir dipivoxil
Antiviral activity against HBV harboring RNA polymerase L180M/M204V mutant gene infected in human HuH7 cells assessed as decrease in viral transient transfection after 24 hrs
Antiviral activity against HBV harboring RNA polymerase L180M/M204V mutant gene infected in human HuH7 cells assessed as decrease in viral transient transfection after 24 hrs
[PMID: 19398648]
Huh-7 EC50
2.6 μM
Compound: Adefovir dipivoxil
Antiviral activity against HBV harboring RNA polymerase L180M mutant gene infected in human HuH7 cells assessed as decrease in viral transient transfection after 24 hrs
Antiviral activity against HBV harboring RNA polymerase L180M mutant gene infected in human HuH7 cells assessed as decrease in viral transient transfection after 24 hrs
[PMID: 19398648]
Vero IC50
0.6 μM
Compound: 10a
Concentration that reduced plaque formation by 50% was measured in HSV-2 infected vero cells in vitro
Concentration that reduced plaque formation by 50% was measured in HSV-2 infected vero cells in vitro
[PMID: 8021925]
WI-38 EC50
0.7 μM
Compound: PMEA dipivoxil
Antimicrobial activity against BK polyomavirus ATCC VR837 infected in human WI38 cells assessed as reduction in viral titer after 7 days by PCR analysis
Antimicrobial activity against BK polyomavirus ATCC VR837 infected in human WI38 cells assessed as reduction in viral titer after 7 days by PCR analysis
[PMID: 18285481]
WI-38 CC50
3.1 μM
Compound: PMEA dipivoxil
Cytotoxicity against human WI38 cells by neutral red assay
Cytotoxicity against human WI38 cells by neutral red assay
[PMID: 18285481]
In Vitro

Adefovir dipivoxil (0.03-30 μM; 6 days) significantly inhibits the proliferation of H1975, A549 and PC9 cells, with more pronounced inhibition when co-treated with VE822[1].
Adefovir dipivoxil (1 μM; 3 days) exhibits increased basolateral-to-apical transport and an elevated efflux ratio in Caco-2 cells treated with 1,25(OH)2D3[2].
Adefovir dipivoxil (24 h) can effectively inhibit PRV proliferation in PK-15 cells, with an IC50 of 92.39 nM[4].
Adefovir dipivoxil (1-10 μM) sensitizes colon cancer cells (HCT116-CDK1 and HT29-CDK1 cells) to Vemurafenib (HY-12057) by disrupting KCTD12-CDK1 interaction[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: H1975
Concentration: 0.1, 1, 3, 10, 30 μM
Incubation Time: 24 h
Result: Activated the ATR signaling pathway.
Resulted in changes in the levels of cell cycle protein F, phosphorylated CDK2, RRM2, phosphorylated RPA, γH2AX, and other related proteins as a result of co-treatment with VE822.
In Vivo

Adefovir dipivoxil (5 mg/kg; i.p.; once a day, 5 days) can potently protect mice against lethal PRV infection, as shown by reduced pathological lesions, lower viral particles in major organs, and increased survival rate[4].
Adefovir dipivoxil (10-50 mg/kg; p.o.; every other day) inhibits the growth of colon cancer cell-derived tumor xenografts in BALB/c nude mice[5].
Adefovir dipivoxil (100 mg/kg/day; p.o.; twice daily; 10 days) reduces viral load in the liver and serum in transgenic mice expressing hepatitis B virus (HBV)[6].
Adefovir dipivoxil (250 mg prodrug per dog for suspension; p.o.; single dose) shows oral bioavailability of 35.0% (suspension) in beagle dogs[7].
Adefovir dipivoxil (30 mg/kg; every other day; 21 days) causes a marked reduction of duck HBV (DHBV) DNA in serum in congenitally HBV-infected ducklings[8].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Transgenic mice expressing HBV[6]
Dosage: 100 mg/kg/day
Administration: Oral gavage, twice daily for 10 days; once daily for 10-21 days
Result: Reduced liver HBV DNA to near the levels of detection (0.02 pg viral DNA/g cellular DNA) at 100 mg/kg/day twice daily.
Had significant antiviral effects on serum HBV DNA on days 4, 7, 10, and 21 when administered once daily at a dose of 100 mg/kg/day.
Was effective in significantly reducing liver HBV DNA with once-daily treatment at doses as low as 1.0 mg/kg/day.
Had no significant effect on core antigen (HBcAg) in the liver or pre-core antigen (HBeAg) in the serum, and did not significantly reduce liver HBV RNA.
Clinical Trial
Molecular Weight

501.47

Formula

C20H32N5O8P

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

NC1=C2N=CN(CCOCP(OCOC(C(C)(C)C)=O)(OCOC(C(C)(C)C)=O)=O)C2=NC=N1

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (199.41 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 0.67 mg/mL (1.34 mM; Need ultrasonic)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9941 mL 9.9707 mL 19.9414 mL
5 mM 0.3988 mL 1.9941 mL 3.9883 mL
View the 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (4.99 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (4.99 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:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
References

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 1.9941 mL 9.9707 mL 19.9414 mL 49.8534 mL
DMSO 5 mM 0.3988 mL 1.9941 mL 3.9883 mL 9.9707 mL
10 mM 0.1994 mL 0.9971 mL 1.9941 mL 4.9853 mL
15 mM 0.1329 mL 0.6647 mL 1.3294 mL 3.3236 mL
20 mM 0.0997 mL 0.4985 mL 0.9971 mL 2.4927 mL
25 mM 0.0798 mL 0.3988 mL 0.7977 mL 1.9941 mL
30 mM 0.0665 mL 0.3324 mL 0.6647 mL 1.6618 mL
40 mM 0.0499 mL 0.2493 mL 0.4985 mL 1.2463 mL
50 mM 0.0399 mL 0.1994 mL 0.3988 mL 0.9971 mL
60 mM 0.0332 mL 0.1662 mL 0.3324 mL 0.8309 mL
80 mM 0.0249 mL 0.1246 mL 0.2493 mL 0.6232 mL
100 mM 0.0199 mL 0.0997 mL 0.1994 mL 0.4985 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Adefovir dipivoxil
Cat. No.:
HY-B0255
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