| Size | Price | Stock | Qty |
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| 50mg |
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| 500mg |
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| 1g |
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Cidofovir hydrate (HPMPC; Vistide) is a potent antiviral medication used as an injectable form for the treatment of cytomegalovirus (CMV) retinitis. It suppresses virus replication by selective inhibition of viral DNA synthesis. Cidofovir is an acyclic nucleoside phosphonate that has to be converted to cidofovir diphosphate which is incorporateed into viral DNA, selectively inhibiting CMV replication and CMV DNA synthesis with IC50 values of 0.1 μM. Cidofovir has significantly long-lasting antiviral action because of the long half-life of its metabolites whose cellular uptake is slow due to the presence of the negatively charged phosphonate group. Cidofovir has also exhibited high antitumor activity.
| Targets |
Viral DNA polymerase (herpesviruses, including human cytomegalovirus [HCMV], herpes simplex virus type 1 [HSV-1], herpes simplex virus type 2 [HSV-2]; EC50 for HCMV: 0.1-0.3 μM, HSV-1: 0.5-1.0 μM, HSV-2: 0.8-1.2 μM)
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| ln Vitro |
Cidofovir (5-100 μM, 72 hours) dihydrate decreases the number of Crandell-Reese feline kidney cells in a dose-dependent manner and has antiviral activity against feline herpesvirus type 1 (FHV-1) with an IC50 of 11 μM[1]. Cidofovir (10-1000 μM, 24-120 hours) dihydrate causes apoptosis and decreases the viability of cancer cells [3].
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| ln Vivo |
At high doses, cidofovir (subcutaneous injection, 100 mg/kg, 3-6 days apart, 21 days apart) dihydrate is very protective against cowpox virus (CPV) infection in female BALB/c weanling mice. demise [2].
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| Cell Assay |
Cytotoxicity assay [1]
Cell Types: Crandell-Reese feline kidney (CRFK) cells Tested Concentrations: 10-100 μM Incubation Duration: 72 hrs (hours) Experimental Results: CRFK cells diminished by 9.1%. Cell viability assay[3] Cell Types: Caco-2, FTC-133, HeLa, Hep-G2, MDA-MB-231, NCI-H1975 and PC-3 Cell Tested Concentrations: 10-1000 μM Incubation Duration: 24, 48, Results at 72, 96, and 120 hrs (hours): As time and concentration increased, tumor cell viability gradually diminished. Compared with the untreated group, the number of FTC-133 cell clones was inhibited by approximately 55% at 100 μM. Apoptosis analysis[3] Cell Types: FTC-133 Cell Tested Concentrations: 100 μM Incubation Duration: 96 hrs (hours) Experimental Results: Significant increase in expression of pro-apoptotic proteins such as cytochrome c, phospho-p53 (S15) and caspase-vs. Compared with untreated cells, cell number 3 diminished by 130%, 49% and 46% respectively, while the anti-apoptotic protein Bcl-x was Dramatically diminished by 57%. |
| Animal Protocol |
Animal/Disease Models: Female weanling balb/c (Bagg ALBino) mouse infected with vaccinia virus (CPV) [2]
Doses: 100 mg/kg Route of Administration: subcutaneous injection; 3-6 days apart; 21 days Experimental Results: 4-3 days before infection administration, prevents 80-100% of mouse deaths. Administration on the fourth day after infection protected 35-50% of mice, and administration on the sixth day protected 10-20%. |
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Overview of Use During Lactation There is currently no information regarding the use of cidofovir during lactation. The manufacturer recommends discontinuing breastfeeding during cidofovir treatment. The use of other medications is recommended, especially when breastfeeding newborns or premature infants. ◉ Effects on Breastfed Infants No published information found as of the revision date. ◉ Effects on Lactation and Breast Milk No published information found as of the revision date. |
| References |
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| Additional Infomation |
Cidofovir dihydrate is the dihydrate of anhydrous cidofovir. It is a nucleoside analogue, an injectable antiviral drug used to treat cytomegalovirus (CMV) retinitis in HIV patients. It has antiviral and antitumor effects. It contains a derivative of anhydrous cidofovir. Cidofovir is a synthetic, acyclic, monophosphate nucleotide analogue, a deoxycytidine analogue with antiviral activity, primarily used against cytomegalovirus (CMV). After entering host cells, cidofovir is phosphorylated by pyruvate kinase to produce its active metabolite, cidofovir diphosphate. Cidofovir diphosphate has a nucleotide-like structure and can compete with deoxycytosine-5-triphosphate (dCTP) for viral DNA polymerase and is incorporated into the elongating viral DNA chain. Therefore, it can prevent further DNA polymerization and disrupt viral DNA replication. It is an acyclic nucleoside phosphonate that can act as a competitive inhibitor of viral DNA polymerase. It is used to treat retinitis caused by cytomegalovirus infection and may also be effective in treating herpesvirus infection.
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| Molecular Formula |
C8H18N3O8P
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|---|---|
| Molecular Weight |
315.22
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| Exact Mass |
315.083
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| Elemental Analysis |
C, 30.48; H, 5.76; N, 13.33; O, 40.61; P, 9.83
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| CAS # |
149394-66-1
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| Related CAS # |
Cidofovir;113852-37-2
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| PubChem CID |
60933
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.8±0.1 g/cm3
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| Boiling Point |
609.5±65.0 °C at 760 mmHg
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| Melting Point |
260ºC (dec)
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| Flash Point |
322.4±34.3 °C
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| Vapour Pressure |
0.0±4.0 mmHg at 25°C
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| Index of Refraction |
1.656
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| LogP |
-3.37
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
20
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| Complexity |
417
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| Defined Atom Stereocenter Count |
1
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| SMILES |
P(C([H])([H])O[C@]([H])(C([H])([H])O[H])C([H])([H])N1C(N=C(C([H])=C1[H])N([H])[H])=O)(=O)(O[H])O[H].O([H])[H].O([H])[H]
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| InChi Key |
FPKARFMSZDBYQF-ILKKLZGPSA-N
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| InChi Code |
InChI=1S/C8H14N3O6P.2H2O/c9-7-1-2-11(8(13)10-7)3-6(4-12)17-5-18(14,15)16/h1-2,6,12H,3-5H2,(H2,9,10,13)(H2,14,15,16)2*1H2/t6-/m0../s1
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| Chemical Name |
(((S)-2-(4-Amino-2-oxo-1(2H)-pyrimidinyl)-1-(hydroxymethyl)ethoxy)methyl)phosphonic acid, dihydrate
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| Synonyms |
Cidofovir; GS-504; HPMPC; Vistide; HPMPC; Cidofovirum
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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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1724 mL | 15.8619 mL | 31.7239 mL | |
| 5 mM | 0.6345 mL | 3.1724 mL | 6.3448 mL | |
| 10 mM | 0.3172 mL | 1.5862 mL | 3.1724 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT01295645 | Active Recruiting |
Drug: Cidofovir Other: No Cidofovir |
Transplantation Infection | M.D. Anderson Cancer Center | March 17, 2011 | Phase 2 |
| NCT00000799 | Completed | Drug: Cidofovir Drug: Probenecid |
Cytomegalovirus Retinitis HIV Infections |
National Institute of Allergy and Infectious Diseases (NIAID) |
April 1996 | Not Applicable |
| NCT00550589 | Completed | Drug: cidofovir Procedure: biopsy |
Precancerous Condition Anal Cancer |
AIDS Malignancy Consortium | September 2007 | Phase 2 |
| NCT00001126 | Completed | Drug: Cidofovir | Papilloma | National Institute of Allergy and Infectious Diseases (NIAID) |
November 2005 | Phase 1 |
| NCT02931539 | Completed | Drug: Maribavir Drug: Ganciclovir |
Cytomegalovirus (CMV) | Shire | December 22, 2016 | Phase 3 |
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