AVN-492
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MedKoo CAT#: 555161

CAS#: 1220646-23-0

Description: AVN-492 is a potent and selective 5-HT6R Antagonist. The affinity of AVN-492 to bind to 5-HT6R (Ki = 91 pM) was more than three orders of magnitude higher than that to bind to the only other target, 5-HT2BR, (Ki = 170 nM). AVN-492 demonstrates good in vitro and in vivo ADME profile with high oral bioavailability and good brain permeability in rodents.


Price and Availability

Size Price Shipping out time Quantity
50mg USD 450 2 Weeks
100mg USD 650 2 Weeks
200mg USD 950 2 Weeks
500mg USD 1750 2 Weeks
1g USD 2650 2 Weeks
2g USD 3850 2 Weeks
5g USD 6950 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2020-10-31. Prices are subject to change without notice.

AVN-492, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 555161
Name: AVN-492
CAS#: 1220646-23-0
Chemical Formula: C17H21N5O2S
Exact Mass: 359.1416
Molecular Weight: 359.448
Elemental Analysis: C, 56.81; H, 5.89; N, 19.48; O, 8.90; S, 8.92


Synonym: AVN-492; AVN 492; AVN492.

IUPAC/Chemical Name: N2,N6,N6,5,7-pentamethyl-3-(phenylsulfonyl)pyrazolo[1,5-a]pyrimidine-2,6-diamine

InChi Key: SNPPEHMSSOEYDH-UHFFFAOYSA-N

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)

SMILES Code: CNC1=NN2C(N=C(C)C(N(C)C)=C2C)=C1S(C3=CC=CC=C3)(=O)=O


Technical Data

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


Additional Information

In behavioral tests, AVN-492 shows anxiolytic effect in elevated plus-maze model, prevents an apomorphine-induced disruption of startle pre-pulse inhibition (the PPI model) and reverses a scopolamine- and MK-801-induced memory deficit in passive avoidance model. No anti-obesity effect of AVN-492 was found in a murine model. The data presented here strongly indicate that due to its high oral bioavailability, extremely high selectivity, and potency to block the 5-HT6 receptor, AVN-492 is a very promising tool for evaluating the role the 5-HT6 receptor might play in cognitive and neurodegenerative impairments. AVN-492 is an excellent drug candidate to be tested for treatment of such diseases, and is currently being tested in Phase I trials.


References

1: Ivachtchenko AV, Okun I, Aladinskiy V, Ivanenkov Y, Koryakova A, Karapetyan R,
Mitkin O, Salimov R, Ivashchenko A. AVN-492, A Novel Highly Selective 5-HT6R
Antagonist: Preclinical Evaluation. J Alzheimers Dis. 2017;58(4):1043-1063. doi:
10.3233/JAD-161262. PubMed PMID: 28550249.