| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Targets |
T-00127-HEV1 targets phosphatidylinositol 4-kinase III beta (PI4KB), a host factor essential for the replication of enteroviruses such as poliovirus. PI4KB is involved in the formation of replication organelles that are required for viral RNA synthesis. By inhibiting PI4KB, T-00127-HEV1 blocks viral replication.
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| ln Vitro |
Compared to other chemical candidates, T-00127_HEV1 exhibited greater action against poliovirus (PV) (EC50 of 0.77 μM) (EC50 1.7 to 4.7 μM). In contrast to AN-12-H5 (108% activity [no inhibition]), GW5074 and T-00127_HEV1 virtually entirely block PI4KB activity at 10 μM (3% and 5% forming activity, respectively) [1].
T-00127-HEV1 is a PI4KB inhibitor with an IC50 of 60 nM. It exhibits potent anti-poliovirus activity with an EC50 of 0.77 μM. At 10 μM concentration, T-00127-HEV1 almost completely inhibits PI4KB kinase activity, retaining only 5% residual activity. The compound is more potent than other tested candidates in inhibiting poliovirus replication. |
| ln Vivo |
Specific in vivo efficacy data for T-00127-HEV1 are not extensively detailed in standard reference sources. As an inhibitor of a host factor essential for enterovirus replication, it is expected to show antiviral activity in animal models of enterovirus infection. Studies in mouse models of poliovirus or other enterovirus infections would be required to evaluate its in vivo efficacy.
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| Enzyme Assay |
The inhibitory activity of T-00127-HEV1 against PI4KB can be assessed using in vitro kinase assays. Recombinant PI4KB enzyme is incubated with its substrate (phosphatidylinositol) and ATP in the presence of varying concentrations of T-00127-HEV1. The amount of phosphatidylinositol 4-phosphate produced is measured using a suitable detection method (e.g., ELISA, radiometric, or mass spectrometry) to determine the IC50.
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| Cell Assay |
The antiviral activity of T-00127-HEV1 is evaluated in vitro using cell lines infected with enteroviruses such as poliovirus. Cells (e.g., HeLa or Vero cells) are infected with virus at a defined multiplicity of infection and treated with increasing concentrations of T-00127-HEV1. Viral replication is assessed by measuring cytopathic effect (CPE) or by quantifying viral RNA or infectious virus particles (plaque assay). The EC50 for inhibition of viral replication is determined.
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| Animal Protocol |
T-00127-HEV1 would be evaluated in animal models of enterovirus infection, such as transgenic mice expressing the human poliovirus receptor (PVR-Tg mice) infected with poliovirus. The compound would be administered via oral, intraperitoneal, or intravenous routes at various doses. Survival rates, clinical signs of paralysis, and viral loads in target organs (e.g., spinal cord, brain) would be monitored to assess efficacy.
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| ADME/Pharmacokinetics |
T-00127-HEV1 has a molecular weight of 411.49 and molecular formula C22H29N5O3. It is a purine derivative. Specific pharmacokinetic parameters such as half-life, bioavailability, and plasma protein binding are not extensively detailed in standard reference sources.
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| Toxicity/Toxicokinetics |
The toxicity profile of T-00127-HEV1 is not extensively documented. As a PI4KB inhibitor, potential toxicities may include effects on cellular lipid metabolism and membrane trafficking, as PI4KB is involved in these processes. Specific LD50 values and organ-specific toxicity data are not readily available.
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| References | |
| Additional Infomation |
T-00127-HEV1 (CAS# 900874-91-1) is also known as T-00127_HEV1. It is a PI4KB inhibitor with an IC50 of 60 nM and exhibits potent anti-poliovirus activity with an EC50 of 0.77 μM. The compound is a research tool for studying enterovirus replication and host-targeted antiviral strategies.
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| Molecular Formula |
C22H29N5O3
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| Molecular Weight |
411.497
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| Exact Mass |
411.227
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| CAS # |
900874-91-1
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| PubChem CID |
4904109
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| Appearance |
White to light yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Index of Refraction |
1.623
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| LogP |
1.52
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
30
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| Complexity |
535
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
RITGMCAEZVMEQO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H29N5O3/c1-15-13-20(23-7-8-26-9-11-30-12-10-26)27-22(24-15)21(16(2)25-27)17-5-6-18(28-3)19(14-17)29-4/h5-6,13-14,23H,7-12H2,1-4H3
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| Chemical Name |
3-(3,4-dimethoxyphenyl)-2,5-dimethyl-N-(2-morpholin-4-ylethyl)pyrazolo[1,5-a]pyrimidin-7-amine
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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 : ~50 mg/mL (~121.51 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.08 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 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL 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: ≥ 2.5 mg/mL (6.08 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4301 mL | 12.1507 mL | 24.3013 mL | |
| 5 mM | 0.4860 mL | 2.4301 mL | 4.8603 mL | |
| 10 mM | 0.2430 mL | 1.2151 mL | 2.4301 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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