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Triptonine B

Cat No.:V34199 Purity: ≥98%
Triptonine B is a sesquiterpene pyridine alkaloid that can inhibit HIV replication in H9 lymphocytes with EC50 of <0.10 μg/mL.
Triptonine B
Triptonine B Chemical Structure CAS No.: 168009-85-6
Product category: Natural Products
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
1mg
100mg
Other Sizes
Official Supplier of:
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Product Description
Triptonine B is a sesquiterpene pyridine alkaloid that can inhibit HIV replication in H9 lymphocytes with EC50 of <0.10 μg/mL.
Triptonine B is a natural sesquiterpenoid pyridine alkaloid found in the roots of Tripterygium wilfordii Hook. f. It exhibits potent anti-HIV activity with an EC₅0 value of <0.10 microg/mL and an in vitro therapeutic index value of >1000. The compound inhibits HIV replication in H9 lymphocytes. Triptonine B is a sesquiterpene pyridine alkaloid with a molecular weight of 967.87 and a molecular formula of C4₆H4₉NO22.
Biological Activity I Assay Protocols (From Reference)
Targets
Triptonine B targets HIV, exhibiting potent activity against HIV replication. It targets enzymatic active sites or protein interfaces involved in the HIV life cycle. Resistance arises via amino acid substitutions that reduce inhibitor binding affinity. The compound's mechanism of action involves inhibition of HIV replication, though the specific viral target has not been fully elucidated. As a sesquiterpenoid pyridine alkaloid, it may interact with viral enzymes or proteins essential for HIV replication.
ln Vitro
In vitro studies demonstrate that Triptonine B is a potent inhibitor of HIV replication. In H9 lymphocytes, the compound inhibits HIV replication with an EC₅0 value of <0.10 microg/mL. The compound exhibits a high therapeutic index of >1000, indicating a favorable selectivity profile. Its in vitro activity is assessed using HIV-infected cell lines, with viral replication measured by p24 antigen production or reverse transcriptase activity. The compound's potency and selectivity make it a promising lead for anti-HIV drug development.
ln Vivo
In vivo activity of Triptonine B has not been extensively characterized in the available literature. As a potent anti-HIV compound with a high therapeutic index in vitro, the compound has potential for in vivo efficacy. However, detailed in vivo studies, including animal models of HIV infection, are not reported. The compound is primarily used as a research tool for studying anti-HIV activity.
Enzyme Assay
In vitro antiviral assays for Triptonine B involve measuring its inhibition of HIV replication in susceptible cell lines such as H9 lymphocytes. Cells are infected with HIV and treated with varying concentrations of the compound. Viral replication is quantified by measuring p24 antigen levels in culture supernatants using ELISA or by measuring reverse transcriptase activity. EC₅0 values are calculated from dose-response curves. Cytotoxicity is assessed in parallel to determine the therapeutic index (TI = CC₅0/EC₅0).
Cell Assay
Cellular assays for Triptonine B are conducted using HIV-susceptible cell lines such as H9 lymphocytes. Cells are infected with HIV-1 and treated with varying concentrations of the compound for 3-7 days. Viral replication is measured by p24 antigen ELISA or reverse transcriptase activity in culture supernatants. Cytotoxicity is assessed using MTT or similar assays to determine the CC₅0. The therapeutic index is calculated as the ratio of CC₅0 to EC₅0. The compound's effects on cell viability and viral replication are compared to control treatments.
Animal Protocol
In vivo animal studies for Triptonine B are limited, as the compound is primarily used as a research tool. For in vivo efficacy studies, animal models of HIV infection (e.g., humanized mouse models) could be employed. Infected animals would be treated with the compound via oral or intraperitoneal administration at various doses. Viral load would be measured in plasma, and CD4+ T-cell counts would be monitored. However, specific in vivo study protocols and results are not extensively reported in the available literature.
ADME/Pharmacokinetics
Pharmacokinetic properties of Triptonine B have not been extensively characterized. The compound has a molecular weight of 967.87 and a molecular formula of C4₆H4₉NO22. It has low aqueous solubility (0.025 g/L at 25degC). The compound is stable when stored as directed on the vial and kept tightly sealed for up to 24 months at 2-8degC. Detailed PK parameters such as half-life, bioavailability, and volume of distribution are not reported in the available literature.
Toxicity/Toxicokinetics
Toxicological data for Triptonine B are limited. The compound is not intended for human therapeutic use and is supplied for research purposes only. In cell-based assays, the compound exhibits potent anti-HIV activity with a high therapeutic index (>1000), suggesting low cytotoxicity. The compound is derived from Tripterygium wilfordii, a plant known for its toxic components, so caution should be exercised. Standard safety precautions should be followed when handling this compound.
References

[1]. Sesquiterpene alkaloids from Tripterygium hypoglaucum and Tripterygium wilfordii: a new class of potent anti-HIV agents. J Nat Prod. 2000 Mar;63(3):357-61.

Additional Infomation
Triptonine B is a natural sesquiterpenoid pyridine alkaloid from Tripterygium wilfordii with potent anti-HIV activity (EC₅0 <0.10 microg/mL). It has a high therapeutic index of >1000. The compound is not an FDA-approved drug and has no clinical indications. It is available in high purity (≥98%) and is typically stored at 2-8degC or -20degC. The compound is used as a research tool for studying anti-HIV activity.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C45H55NO22
Molecular Weight
961.911700000001
Exact Mass
961.321
CAS #
168009-85-6
Appearance
White to off-white solid
Density
1.4±0.1 g/cm3
Boiling Point
1003.3±65.0 °C at 760 mmHg
Flash Point
560.6±34.3 °C
Vapour Pressure
0.0±0.3 mmHg at 25°C
Index of Refraction
1.580
LogP
1.51
SMILES
CC(=O)OC[C@@]12[C@@H]([C@@H](C3[C@H]([C@@]42[C@](C)([C@H]([C@@H]([C@@H]1OC(=O)C)OC(=O)C5=COC=C5)OC(=O)[C@@](C)(CCC6=C(C=CC=N6)C(=O)OC[C@]3(C)O4)OC(=O)C7=COC=C7)O)OC(=O)C)OC(=O)C)OC(=O)C
HS Tariff Code
2934.99.9001
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)
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
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
(e.g. IP/IV/IM/SC)
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution 50 μL Tween 80 850 μL Saline)
*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 : PEG300Tween 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).
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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)]
*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.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO 100 μLPEG300 200 μL castor oil 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol 100 μL Cremophor 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH 400 μLPEG300 50 μL Tween 80 450 μL 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).
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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders


Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.0396 mL 5.1980 mL 10.3960 mL
5 mM 0.2079 mL 1.0396 mL 2.0792 mL
10 mM 0.1040 mL 0.5198 mL 1.0396 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:
  • To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.
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.

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