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MedKoo Cat#: 561401 | Name: AVN-101 HCl
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

AVN-101 is a very potent 5-HT7 receptor antagonist, with slightly lesser potency toward 5-HT6, 5-HT2A, and 5HT-2C receptors. It is a milti-target drug candidate for the treatment of CNS disorders.

Chemical Structure

AVN-101 HCl
AVN-101 HCl
CAS#1061354-48-0 (HCl)

Theoretical Analysis

MedKoo Cat#: 561401

Name: AVN-101 HCl

CAS#: 1061354-48-0 (HCl)

Chemical Formula: C21H25ClN2

Exact Mass: 0.0000

Molecular Weight: 340.90

Elemental Analysis: C, 73.99; H, 7.39; Cl, 10.40; N, 8.22

Price and Availability

Size Price Availability Quantity
5mg USD 90.00 Ready to ship
10mg USD 150.00 Ready to ship
25mg USD 250.00 Ready to ship
50mg USD 450.00 Ready to ship
100mg USD 750.00 Ready to ship
200mg USD 1,250.00 Ready to ship
500mg USD 2,650.00 Ready to ship
1g USD 3,850.00 Ready to ship
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Related CAS #
1025725-91-0 (free base) 1061354-48-0 (HCl)
Synonym
AVN-101; AVN 101; AVN101;
IUPAC/Chemical Name
2,8-Dimethyl-5-phenethyl-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole hydrochloride
InChi Key
RKLJJDFIWWRTEJ-UHFFFAOYSA-N
InChi Code
InChI=1S/C21H24N2.ClH/c1-16-8-9-20-18(14-16)19-15-22(2)12-11-21(19)23(20)13-10-17-6-4-3-5-7-17;/h3-9,14H,10-13,15H2,1-2H3;1H
SMILES Code
CC1=CC2=C(N(CCC3=CC=CC=C3)C4=C2CN(C)CC4)C=C1.[H]Cl
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Biological target:
AVN-101 is a very potent 5-HT7 receptor antagonist, with slightly lesser potency toward 5-HT6, 5-HT2A, and 5HT-2C receptors.
In vitro activity:
When tested at a concentration of 1μM, AVN-101 rapidly metabolized by both the human (HLM) and rat (RLM) microsomes (Fig. 7 and Table 5). Ten probable metabolites have been structurally identified, M1-M10 (Fig. 8). M1, M2, M4-M6, M9, and M10 were found in quantifiable amounts only in reactions with human microsomes. M7 was identified only with rat microsomes, and M3, M8, and a few other unidentifiable metabolites were found in both the rat and human microsomes. By the end of a 30-min incubation time, the remaining amount of AVN-101 comprised only 2% and <1% for human and rat microsomes, respectively (Table 6). However, at 2μM the decomposition AVN-101 in human microsomes was substantially diminished; only 57% of the original AVN-101 was consumed by the end of 30-min incubation (Table 6). It seemed that at the higher concentration, AVN-101 might have inhibited some cytochromes(s) participating in the AVN-101metabolism. Reference: J Alzheimers Dis. 2016 May 25;53(2):583-620. https://www.ncbi.nlm.nih.gov/pmc/articles/pmid/27232215/
In vivo activity:
Similar to scopolamine, treatment of the Balb/c mice with MK-801, NMDA glutamate receptor antagonist, also produced anterograde amnesia (Fig. 25). Judging by the three measured parameters, latency to enter the dark compartment, time spent in the white compartment, and number of entries into the dark compartment, the AVN-101 dose-dependently prevented the MK-801-induced amnesic effect. It should be noted, that the MK-801-induced memory impairment model was less sensitive to AVN-101 than the scopolamine model, the anti-amnesic dose of AVN-101 being approximately 10-fold as high in the MK-801 model (0.5 mg/kg) as in the scopolamine model (0.05 mg/kg) of the amnesia. Memantine was not active in this model and the effect of the AVN-101was similar to that of SB-742457. It is reasonable to assume, that similar to the SB-742457, in the MK-801-induced amnesia model, it is 5-HT6 receptor blocking ability of the AVN-101, which is responsible for its efficacy. AVN-101 at a dose of 0.2 mg/kg given 25 min after the scopolamine, effectively reversed the scopolamine-induced amnesia manifested by increased time spent in the “platform”. Reference: J Alzheimers Dis. 2016 May 25;53(2):583-620. https://www.ncbi.nlm.nih.gov/pmc/articles/pmid/27232215/

Preparing Stock Solutions

The following data is based on the product molecular weight 340.90 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
1. Ivachtchenko AV, Lavrovsky Y, Okun I. AVN-101: A Multi-Target Drug Candidate for the Treatment of CNS Disorders. J Alzheimers Dis. 2016 May 25;53(2):583-620. doi: 10.3233/JAD-151146. PMID: 27232215; PMCID: PMC4969713.
In vivo protocol:
1. Ivachtchenko AV, Lavrovsky Y, Okun I. AVN-101: A Multi-Target Drug Candidate for the Treatment of CNS Disorders. J Alzheimers Dis. 2016 May 25;53(2):583-620. doi: 10.3233/JAD-151146. PMID: 27232215; PMCID: PMC4969713.
1: Ivachtchenko AV, Lavrovsky Y, Okun I. AVN-101: A Multi-Target Drug Candidate for the Treatment of CNS Disorders. J Alzheimers Dis. 2016 May 25;53(2):583-620. doi: 10.3233/JAD-151146. PubMed PMID: 27232215; PubMed Central PMCID: PMC4969713.