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| 1mg |
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| Other Sizes |
| Targets |
Bis-T-23 targets HIV-1 integrase, an enzyme essential for the replication of the HIV virus. It acts as an inhibitor of this enzyme. It also targets dynamin, a GTPase involved in endocytosis and other cellular processes. By promoting dynamin oligomerization and inhibiting its GTPase activity, Bis-T-23 modulates cellular trafficking and signaling.
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| ln Vitro |
Via its 0.18 μM dose, Bis-T-23 (AG1717) inhibits HIV-1 integrase [2]. The binding of integrase to substrate DNA is inhibited by AG1717 (2 μM)[2].
In vitro, Bis-T-23 inhibits HIV-1 integrase activity. It also inhibits phosphatidylserine-induced dynamin 1 GTPase activity with an IC50 of 1.7 µM. It promotes actin-dependent dynamin oligomerization. These activities demonstrate its ability to modulate both viral replication and cellular trafficking processes. |
| ln Vivo |
Bis-T-23 (1 ng) targets the oligomerization of the actin kinase dynein in podocytes to promote proper GFB activity [1]. Bis-T-23 (ip; 20, 40 mg/kg) improves proteinuria by altering actin dynamics [1]. Bis-T-23 (ip; 20, 40 mg/kg) relieves or avoids proteinuria in numerous hereditary and chronic glomerular disease models in wild animals
In vivo, Bis-T-23 has been studied for its potential in the treatment of HIV and chronic kidney diseases (CKD). By inhibiting HIV-1 integrase, it may prevent viral replication. Its effects on dynamin may be relevant to kidney disease. However, specific details of in vivo efficacy studies are not extensively detailed in the available literature. |
| Enzyme Assay |
The in vitro enzyme assay for Bis-T-23 measures its ability to inhibit HIV-1 integrase activity. These cell-free assays use purified integrase and a DNA substrate. The compound's inhibitory potency is determined by measuring the reduction in integration activity. Its effects on dynamin GTPase activity can be assessed using similar assays with purified dynamin.
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| Cell Assay |
In vitro cellular assays for Bis-T-23 assess its effects on HIV replication and cellular trafficking. HIV-infected cells are treated with Bis-T-23, and viral replication is measured. Its effects on dynamin-mediated endocytosis and other cellular processes can also be assessed. These assays demonstrate the compound's functional activity in a relevant cellular context.
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| Animal Protocol |
Animal/Disease Models: zebrafish[1]
Doses: 1 ng Route of Administration: Injection Experimental Results:Promotes the oligomerization of zebrafish Dyn2. Increases the number of focal adhesions (FA) and stress fibers in cultured podocytes. In vivo animal studies for Bis-T-23 have been conducted in models of HIV infection and chronic kidney disease to evaluate its efficacy. However, specific details of these studies are not extensively detailed in the available literature. It is a research compound and is not approved for clinical use. |
| ADME/Pharmacokinetics |
Specific pharmacokinetic data for Bis-T-23 are not extensively detailed in the available literature. As a small molecule, its pharmacokinetic properties would be important for its in vivo efficacy. However, specific parameters such as half-life and bioavailability are not provided. It is intended for research use only.
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| Toxicity/Toxicokinetics |
Specific toxicity data for Bis-T-23 are not extensively detailed in the available literature. As an HIV integrase inhibitor and dynamin modulator, its toxicity profile is likely related to its mechanism of action. However, its potential for treating HIV and CKD suggests a manageable safety profile. It is intended for research purposes only.
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| References |
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| Additional Infomation |
Bis-T-23 (AG1717) is a tyrphostin derivative and an HIV-I integrase inhibitor. It promotes actin-dependent dynamin oligomerization and inhibits dynamin 1 GTPase activity. It can be used for the research of HIV and chronic kidney diseases (CKD). It is not approved for clinical use and is intended for research purposes only.
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| Molecular Formula |
C23H20N4O8
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| Molecular Weight |
480.426905632019
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| Exact Mass |
480.128
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| CAS # |
171674-76-3
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| PubChem CID |
5468833
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
1.1
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| Hydrogen Bond Donor Count |
8
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
35
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| Complexity |
834
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(/C(/C#N)=C/C1C=C(C(=C(C=1)O)O)O)NCCCNC(/C(/C#N)=C/C1C=C(C(=C(C=1)O)O)O)=O
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| InChi Key |
AAPVOSBVTLGGOU-VHUAAIQRSA-N
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| InChi Code |
InChI=1S/C23H20N4O8/c24-10-14(4-12-6-16(28)20(32)17(29)7-12)22(34)26-2-1-3-27-23(35)15(11-25)5-13-8-18(30)21(33)19(31)9-13/h4-9,28-33H,1-3H2,(H,26,34)(H,27,35)/b14-4+,15-5+
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| Chemical Name |
(E)-2-cyano-N-[3-[[(E)-2-cyano-3-(3,4,5-trihydroxyphenyl)prop-2-enoyl]amino]propyl]-3-(3,4,5-trihydroxyphenyl)prop-2-enamide
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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 | 2.0815 mL | 10.4073 mL | 20.8147 mL | |
| 5 mM | 0.4163 mL | 2.0815 mL | 4.1629 mL | |
| 10 mM | 0.2081 mL | 1.0407 mL | 2.0815 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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