| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
AVN-492 is a highly specific, selective and orally bioavailable antagonist of the 5-HT6R with Ki of 91 pM. AVN-492 exhibits a binding affinity of over three orders of magnitude higher to 5-HT6R (Ki=91 pM) than it does to 5-HT2BR (Ki=170 nM), which is the only other target. Because of this, the compound AVN-492 demonstrated excellent 5-HT6R selectivity against all other subtypes of serotonin receptors and exhibited extreme specificity against all other receptor types, including adrenergic, GABAergic, dopaminergic, histaminergic, and others. In rodents, AVN-492 exhibits a good ADME profile both in vitro and in vivo, along with high oral bioavailability and good brain permeability. An extremely promising method for assessing the possible contribution of the 5-HT6 receptor to cognitive and neurodegenerative impairments is AVN-492. AVN-492 is a promising drug candidate undergoing Phase I trials to be tested for treating these kinds of illnesses.
| Targets |
5-HT6 Receptor ( Ki = 91 pM )
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| ln Vitro |
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| ln Vivo |
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| Enzyme Assay |
AVN-492 is dissolved to a concentration of 10 mM in 100% DMSO. After that, this DMSO solution is diluted 50 times using either MQ water or a pH-appropriate buffer. The MultiScreen 96-well plates are used for the Caco-2 permeability assay. Simply put, each well with a porous membrane bottom is seeded with Caco-2 cells (ATCC, Cat. No. HTB-37). The cells are grown in a CO2 thermostat at 37°C for 20–23 days, or until they reach total confluence. Every two to three days, the growth medium is swapped. Using Lucifer Yellow CH, a "leak test" is used to determine the physical integrity of the cell monolayer that has been established on the well-porous membrane. The permeability of AVN-492 (200μM) is assessed in both directions: from basal to apical and from apical to basal. The permeabilities of propranolol (which has a high permeability) and ranitidine (which has a low permeability) are only measured in the apical-to-basal direction. Verapamil (100 μM), a Pgp inhibitor, is used with or without Rhodamine 123 (30 μM) to measure its Pgp-dependent permeability. The apical-to-basal and basalto-apical permeabilities are also measured in the presence of verapamil in order to evaluate the Pgp pump's potential involvement in an AVN-492 efflux. LC/MS/MS API2000 is used to determine the concentrations of AVN-322 in donor and acceptor chambers.
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| Animal Protocol |
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| References |
| Molecular Formula |
C17H21N5O2S
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| Molecular Weight |
359.45
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| Exact Mass |
359.14
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| Elemental Analysis |
C, 56.81; H, 5.89; N, 19.48; O, 8.90; S, 8.92
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| CAS # |
1220646-23-0
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| Related CAS # |
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| Appearance |
Solid powder
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| SMILES |
CC1=C(C(=NC2=C(C(=NN12)NC)S(=O)(=O)C3=CC=CC=C3)C)N(C)C
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| InChi Key |
SNPPEHMSSOEYDH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H21N5O2S/c1-11-14(21(4)5)12(2)22-17(19-11)15(16(18-3)20-22)25(23,24)13-9-7-6-8-10-13/h6-10H,1-5H3,(H,18,20)
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| Chemical Name |
3-(benzenesulfonyl)-2-N,6-N,6-N,5,7-pentamethylpyrazolo[1,5-a]pyrimidine-2,6-diamine
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| Synonyms |
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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 |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3.75 mg/mL (10.43 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 37.5 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: ≥ 3.75 mg/mL (10.43 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 37.5 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 | 2.7820 mL | 13.9101 mL | 27.8203 mL | |
| 5 mM | 0.5564 mL | 2.7820 mL | 5.5641 mL | |
| 10 mM | 0.2782 mL | 1.3910 mL | 2.7820 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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