| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg | |||
| Other Sizes |
| Targets |
Stampidine targets HIV-1 reverse transcriptase (RT), the enzyme responsible for converting viral RNA into DNA. As a nucleoside reverse transcriptase inhibitor (NRTI), stampidine acts as a chain terminator, preventing the elongation of viral DNA. It has shown potent activity against both wild-type and drug-resistant HIV-1 isolates.
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| ln Vitro |
Genital tract epithelial cells are not cytotoxically affected by stampidine (7.8–1,000 μM; 24 hours) [2]. In cervical mucous, stampidine has no influence on sperm motility [2].
Stampidine has potent anti-HIV activity against clinical HIV-1 isolates with subnanomolar to nanomolar IC50 values. In a side-by-side comparison against 10 zidovudine-sensitive clinical HIV-1 isolates, stampidine was 100-fold more potent than stavudine and twice as effective as zidovudine. Stampidine also exhibits activity against drug-resistant HIV strains. |
| ln Vivo |
Oral stampidine (50–100 mg/kg) has strong antiretroviral effects in cats infected with the feline immunodeficiency virus (FIV) [3]. In dogs, Stampidine (100 mg/kg; po) had the following mean plasma Cmax, AUC, half-life (t1/2), and mean residence time (MRT) values: 15.4 µM, 23.1 µM·h, 108.6 min, and 119.4 min, respectively [ 4]. In adult beagle dogs, stampidine does not elevate ALT, AST, or Alk levels; it also does not produce anemia, thrombocytopenia, neutropenia, or lymphopenia (suggesting hematological toxicity), increases in BUN or creatinine, or electrolyte changes (suggesting nephrotoxicity or metabolic abnormalities)[4].
Stampidine (50-100 mg/kg; p.o.) exhibits potent antiretroviral activity in chronically feline immunodeficiency virus (FIV)-infected cats. Stampidine (100 mg/kg; p.o.) shows the average plasma Cmax, AUC, half-life (t1/2), and mean residence time (MRT) values of 15.4 µM, 23.1 µM·h, 108.6 min and 119.4 min, respectively, in dogs. Stampidine does not cause anemia. |
| Enzyme Assay |
The antiviral activity of stampidine can be assessed using in vitro cell-based antiviral assays. HIV-1-infected cells (e.g., MT-4 cells or PBMCs) are treated with increasing concentrations of stampidine. Viral replication is measured by quantifying p24 antigen production or by using a reporter gene assay. IC50 values are determined from dose-response curves.
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| Cell Assay |
Stampidine's antiviral activity is evaluated in vitro using HIV-1-infected cell lines such as MT-4 cells or primary human PBMCs. Cells are infected with HIV-1 at a defined multiplicity of infection and treated with increasing concentrations of stampidine. Viral replication is assessed by measuring p24 antigen or by using a luciferase reporter assay. Activity against drug-resistant HIV-1 isolates is also assessed.
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| Animal Protocol |
Animal/Disease Models: SPF male or female domestic cat (2.9-6.2 kg), chronic FIV infection [3]
Doses: 50 mg/kg, 100 mg/kg Route of Administration: Oral (oral bolus dose) Experimental Results: Demonstrated effective Antiretroviral activity. Animal/Disease Models: Male Beagle (10-12 kg) [4] Doses: 100 mg/kg (pharmacokinetic/PK/PK analysis) Route of Administration: Oral Experimental Results: Estimated mean plasma Cmax and AUC values were 15.4 µM and 23.1 µM, respectively ·h. The mean elimination half-life (t1/2) and mean residence time (MRT) were 108.6 minutes and 119.4 minutes, respectively. Stampidine is administered orally in preclinical studies. In FIV-infected cats, stampidine (50-100 mg/kg; p.o.) exhibits potent antiretroviral activity. In dogs, stampidine (100 mg/kg; p.o.) shows favorable pharmacokinetic properties. Efficacy is assessed by measuring viral load and clinical parameters. |
| ADME/Pharmacokinetics |
Stampidine has a molecular formula of C20H23BrN3O8P and a molecular weight of 544.29. In dogs, stampidine (100 mg/kg; p.o.) shows average plasma Cmax of 15.4 µM, AUC of 23.1 µM·h, half-life of 108.6 min, and MRT of 119.4 min. Stampidine does not cause anemia.
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| Toxicity/Toxicokinetics |
The toxicity profile of stampidine is favorable. Stampidine does not cause anemia. Specific LD50 values and organ-specific toxicity data are not extensively detailed in standard reference sources, but the compound is described as having an improved pharmacological profile.
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| References | |
| Additional Infomation |
Stampidine (CAS# 217178-62-6) is an antiviral agent that inhibits HIV-1 replication by targeting reverse transcriptase. It has demonstrated broad-spectrum antiviral effects, including activity against drug-resistant HIV strains. Stampidine has shown strong activity in preclinical studies and is a promising candidate for HIV therapy. It also shows potential anticancer properties.
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| Molecular Formula |
C20H23BRN3O8P
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| Molecular Weight |
544.2948
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| Exact Mass |
543.041
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| CAS # |
217178-62-6
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| PubChem CID |
469782
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| Appearance |
White to off-white solid powder
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| LogP |
2.806
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
33
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| Complexity |
873
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| Defined Atom Stereocenter Count |
3
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| SMILES |
CC1=CN(C(=O)NC1=O)[C@H]2C=C[C@H](O2)COP(=O)(N[C@H](C)C(=O)OC)OC3=CC=C(C=C3)Br
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| InChi Key |
VPABMVYNSQRPBD-AOJMVMDXSA-N
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| InChi Code |
InChI=1S/C20H23BrN3O8P/c1-12-10-24(20(27)22-18(12)25)17-9-8-16(31-17)11-30-33(28,23-13(2)19(26)29-3)32-15-6-4-14(21)5-7-15/h4-10,13,16-17H,11H2,1-3H3,(H,23,28)(H,22,25,27)/t13-,16+,17-,33?/m1/s1
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| Chemical Name |
methyl (2R)-2-[[(4-bromophenoxy)-[[(2S,5R)-5-(5-methyl-2,4-dioxopyrimidin-1-yl)-2,5-dihydrofuran-2-yl]methoxy]phosphoryl]amino]propanoate
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| Synonyms |
HI-113; HI 113; Stampidine
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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) |
DMSO : ~100 mg/mL (~183.73 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.83 mg/mL (1.52 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 8.3 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of 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. Solubility in Formulation 2: ≥ 0.83 mg/mL (1.52 mM) (saturation unknown) 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. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 8.3 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. View More
Solubility in Formulation 3: ≥ 0.83 mg/mL (1.52 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8373 mL | 9.1863 mL | 18.3726 mL | |
| 5 mM | 0.3675 mL | 1.8373 mL | 3.6745 mL | |
| 10 mM | 0.1837 mL | 0.9186 mL | 1.8373 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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