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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 |
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 | 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 | ||||||||||||||||||||||||||||||||||||
DMSO
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