| Size | Price | Stock | Qty |
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| 5mg |
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| Other Sizes |
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H1PVAT is a novel inhibitor of poliovirus serotypes (PV-1, PV-2, PV-3), inhibiting early stage of the viral replication. H1PVAT interacts with viral capsid directly and protects PV against heat inactivation. H1PVAT was identified as a potent and selective inhibitor of the in vitro replication of all three poliovirus serotypes, whereas no activity was observed against other enteroviruses.
| ln Vitro |
With dose-dependent inhibition, H1PVAT (10-218 nM; 24-48 hours) suppresses the replication of the poliovirus strain Sabin, with EC50s of 10 nM (PV-1), 26 nM (PV-2), and 218 nM (PV-3), respectively [1]. When H1PVAT is administered only before infection, intracellular viral RNA levels are reduced (>99.9%) and early viral replication is inhibited (30 minutes before PV-1 infection or 1 hour after infection; 7 hours) [1]. With 50% thermal inactivation temperatures rising to 52.6°C and 50.8°C, H1PVAT (50 μM; 2 min) shields PV against thermal inactivation, indicating a direct interaction between the viral capsid and H1PVAT [1].
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| References |
| Molecular Formula |
C19H14N5OF3S
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|---|---|
| Molecular Weight |
417.408
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| Exact Mass |
417.087
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| CAS # |
351438-49-8
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| PubChem CID |
3462414
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Index of Refraction |
1.674
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| LogP |
4.29
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
29
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| Complexity |
660
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
FITXCLRWDSMQLY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H14F3N5OS/c20-19(21,22)16-8-13(15-2-1-7-29-15)25-17-9-14(26-27(16)17)18(28)24-12-5-3-11(10-23)4-6-12/h1-7,9,13,16,25H,8H2,(H,24,28)
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| Chemical Name |
N-(4-cyanophenyl)-5-thiophen-2-yl-7-(trifluoromethyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-2-carboxamide
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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 | 2.3957 mL | 11.9786 mL | 23.9573 mL | |
| 5 mM | 0.4791 mL | 2.3957 mL | 4.7915 mL | |
| 10 mM | 0.2396 mL | 1.1979 mL | 2.3957 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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