1. Anti-infection
  2. Reverse Transcriptase HIV
  3. Stampidine

Stampidine is a nucleoside reverse transcriptase inhibitor (NRTI) with potent and broad-spectrum anti-HIV activity. Stampidine inhibits the laboratory HIV-1 strain HTLVIIIB (B-envelope subtype) and primary clinical isolates with IC50s of 1 nM and 2 nM, respectively. Stampidine also inhibits NRTI-resistant primary clinical isolates and NNRTI-resistant clinical isolates with IC50s of 8.7 nM and 11.2 nM, respectively.

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Stampidine Chemical Structure

Stampidine Chemical Structure

CAS No. : 217178-62-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 440 In-stock
Solution
10 mM * 1 mL in DMSO USD 440 In-stock
Solid
5 mg USD 400 In-stock
10 mg USD 680 In-stock
25 mg USD 1350 In-stock
50 mg USD 2150 In-stock
100 mg USD 3500 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

Stampidine is a nucleoside reverse transcriptase inhibitor (NRTI) with potent and broad-spectrum anti-HIV activity. Stampidine inhibits the laboratory HIV-1 strain HTLVIIIB (B-envelope subtype) and primary clinical isolates with IC50s of 1 nM and 2 nM, respectively. Stampidine also inhibits NRTI-resistant primary clinical isolates and NNRTI-resistant clinical isolates with IC50s of 8.7 nM and 11.2 nM, respectively[1].

IC50 & Target

IC50: 1 nM (HTLVIIIB), 2 nM (primary clinical isolates), 8.7 nM (NRTI-resistant primary clinical isolates), 11.2 nM (NRTI-resistant primary clinical isolates)[1]

In Vitro

Stampidine (7.8-1,000 μM; 24 hours) is not cytotoxic to genital tract epithelial cells[2].
Stampidine has no effect on sperm motility in cervical mucus[2].

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

In Vivo

Stampidine (50-100 mg/kg; p.o.) exhibits potent antiretroviral activity in chronically feline immunodeficiency virus (FIV)-infected cats[3].
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[4].
Stampidine does not cause anemia, thrombocytopenia, neutropenia, or lymphopenia suggestive of hematologic toxicity, elevations of BUN or creatinine or electrolyte disturbances suggestive of renal toxicity or metabolic abnormalities, elevations of ALT, AST, Alk in adult beagle dogs[4].

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

Animal Model: SPF male or female domestic cats (2.9- 6.2 kg), with chronically FIV-infected[3]
Dosage: 50 mg/kg, 100 mg/kg
Administration: Oral administration (oral bolus dose)
Result: Exhibited potent antiretroviral activity.
Animal Model: Male beagle dogs (10-12 kg)[4]
Dosage: 100 mg/kg (Pharmacokinetic Analysis)
Administration: Oral administration
Result: The estimated average plasma Cmax and AUC values were 15.4 µM and 23.1 µM·h, respectively. The average elimination half-life (t1/2) and mean residence time (MRT) were 108.6 min and 119.4 min, respectively.
Molecular Weight

544.29

Formula

C20H23BrN3O8P

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1=O)N(C=C1C)[C@](C=C2)([H])O[C@@H]2CO[P](OC(C=C3)=CC=C3Br)(N[C@@H](C)C(OC)=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (183.73 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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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: ≥ 0.83 mg/mL (1.52 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 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: ≥ 0.83 mg/mL (1.52 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8373 mL 9.1863 mL 18.3726 mL 45.9314 mL
5 mM 0.3675 mL 1.8373 mL 3.6745 mL 9.1863 mL
10 mM 0.1837 mL 0.9186 mL 1.8373 mL 4.5931 mL
15 mM 0.1225 mL 0.6124 mL 1.2248 mL 3.0621 mL
20 mM 0.0919 mL 0.4593 mL 0.9186 mL 2.2966 mL
25 mM 0.0735 mL 0.3675 mL 0.7349 mL 1.8373 mL
30 mM 0.0612 mL 0.3062 mL 0.6124 mL 1.5310 mL
40 mM 0.0459 mL 0.2297 mL 0.4593 mL 1.1483 mL
50 mM 0.0367 mL 0.1837 mL 0.3675 mL 0.9186 mL
60 mM 0.0306 mL 0.1531 mL 0.3062 mL 0.7655 mL
80 mM 0.0230 mL 0.1148 mL 0.2297 mL 0.5741 mL
100 mM 0.0184 mL 0.0919 mL 0.1837 mL 0.4593 mL
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Stampidine Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    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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