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AVN-101
🥰Excellent
Catalog No. T26690Cas No. 1061354-48-0
AVN-101 is a highly potent 5-HT7 receptor antagonist with a Ki value of 153 pM. AVN-101 also exhibits considerable affinity for histamine H1 (Ki value of 0.58 nM) and adrenergic α2A, α2B and α2C (Ki values ​​of 0.41-3.6 nM) receptors. AVN-101 has shown good oral bioavailability and brain-blood barrier permeability, low toxicity and reasonable efficacy in animal models of central nervous system diseases.
AVN-101
🥰Excellent
Purity: 99.73%
Catalog No. T26690Cas No. 1061354-48-0
AVN-101 is a highly potent 5-HT7 receptor antagonist with a Ki value of 153 pM. AVN-101 also exhibits considerable affinity for histamine H1 (Ki value of 0.58 nM) and adrenergic α2A, α2B and α2C (Ki values ​​of 0.41-3.6 nM) receptors. AVN-101 has shown good oral bioavailability and brain-blood barrier permeability, low toxicity and reasonable efficacy in animal models of central nervous system diseases.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $30 | In Stock | |
| 5 mg | $73 | In Stock | |
| 10 mg | $123 | In Stock | |
| 25 mg | $228 | In Stock | |
| 50 mg | $372 | In Stock | |
| 100 mg | $619 | In Stock | |
| 200 mg | $877 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $98 | In Stock |
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Purity:99.73%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | AVN-101 is a highly potent 5-HT7 receptor antagonist with a Ki value of 153 pM. AVN-101 also exhibits considerable affinity for histamine H1 (Ki value of 0.58 nM) and adrenergic α2A, α2B and α2C (Ki values ​​of 0.41-3.6 nM) receptors. AVN-101 has shown good oral bioavailability and brain-blood barrier permeability, low toxicity and reasonable efficacy in animal models of central nervous system diseases. |
| Targets&IC50 | α2:0.41-3.6 nM(Ki), H1:0.58 nM(Ki), 5-HT7:153 pM(Ki) |
| In vitro | METHODS: The ability of AVN-101 to block hERG channels was tested in single-cell patch clamp experiments using HEK cells stably expressing hERG potassium channels and measuring potassium currents. RESULTS Both AVN-101 and M1 blocked hERG channels with an IC50 score of 0.58 μM. [2] |
| In vivo | METHODS: AVN-101 (5 mg/kg) was evaluated in Wistar rats when administered by oral (PO) and intravenous (I.v) routes. AVN-101 was detected in plasma using LC-MS/MS. RESULTS The bioavailability of AVN-101 in rats (calculated based on AUC0 ⟶240 values) was 26.3% when injected intraperitoneally and 8.5% when administered orally. However, it should be noted that the drug elimination rate determined in the in vivo experiments, Kel = 0.0121 min-1 (i.v.), was significantly slower than that observed in rat microsomes (Kel = 0.335 min-1). [1] |
| Molecular Weight | 340.89 |
| Formula | C21H25ClN2 |
| Cas No. | 1061354-48-0 |
| Smiles | Cl.CN1CCC2=C(C1)C1=CC(C)=CC=C1N2CCC1=CC=CC=C1 |
| Relative Density. | no data available |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 60 mg/ml (176.01 mM)  | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
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Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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