- AVN-492
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- $44.00
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2026-08-08
- CAS:1220646-23-0
- Purity: 99.81%
- Supply Ability: 10g
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| | AVN-492 Basic information |
| Product Name: | AVN-492 | | Synonyms: | AVN-492;AVN-492; AVN 492; AVN492;1220646-23-0;CS-2812;Pyrazolo[1,5-a]pyrimidine-2,6-diamine, N2,N6,N6,5,7-pentamethyl-3-(phenylsulfonyl)-;N2,N6,N6,5,7-Pentamethyl-3-(phenylsulfonyl)pyrazolo[1,5-a]pyrimidine-2,6-diamine;inhibit,5-HT Receptor,Inhibitor,AVN-492,Serotonin Receptor,AVN 492,5-hydroxytryptamine Receptor;3-(benzenesulfonyl)-N2,5,N6,N6,7-pentamethylpyrazolo[1,5-a]pyrimidine-2,6-diamine;AVN-492, 10 mM in DMSO | | CAS: | 1220646-23-0 | | MF: | C17H21N5O2S | | MW: | 359.45 | | EINECS: | | | Product Categories: | API | | Mol File: | 1220646-23-0.mol |  |
| | AVN-492 Chemical Properties |
| density | 1.31±0.1 g/cm3(Predicted) | | storage temp. | Keep in dark place,Sealed in dry,Store in freezer, under -20°C | | solubility | DMSO:62.5(Max Conc. mg/mL);173.88(Max Conc. mM) DMF:25.0(Max Conc. mg/mL);69.55(Max Conc. mM) DMF:PBS (pH 7.2) (1:20):0.04(Max Conc. mg/mL);0.11(Max Conc. mM) Ethanol:1.0(Max Conc. mg/mL);2.78(Max Conc. mM) | | form | A crystalline solid | | pka | 1.04±0.30(Predicted) | | color | White to light yellow |
| | AVN-492 Usage And Synthesis |
| Uses | AVN-492 is a very specific and highly-selective antagonist with picomolar affinity to 5-HT6R (Ki=91 pM). | | in vivo | In rats, the plasma, brain, and CSF concentrations of the PO administered AVN-492 are dose-dependent. The drug concentration curves for the plasma and brain are of hyperbolic shape and at all doses the brain-plasma ratio is near 11%. The drug concentration in CSF, however, is nearly linearly dependent on the dose, reaching 50% of the plasma level at 10mg/kg. In mice, the plasma and brain concentrations of AVN-492, given IV at a dose of 2 mg/kg, decreased with time but at both time points, 15 min and 60 min, the brain/plasma ratio (mean±SEM) is nearly the same, at 13.2±0.7% and 9.0±1.5%, respectively. This indicates that the steady-state concentration gradient of AVN-492 is established by at least 15 min after the drug administration[1]. | | IC 50 | 5-HT6 Receptor: 91 pM (Ki) | | References | [1] Ivachtchenko AV, et al. AVN-492, A Novel Highly Selective 5-HT6R Antagonist: Preclinical Evaluation. J Alzheimers Dis. 2017;58(4):1043-1063. DOI:10.3233/JAD-161262 |
| | AVN-492 Preparation Products And Raw materials |
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