VU0467154
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MedKoo CAT#: 530355

CAS#: 1451993-15-9

Description: VU0467154 is a potent and selective M4 PAM. VU0467154 exhibits robust APD-like and cognitive enhancing activity in rodents. Selective M4 PAMs could provide a therapeutic strategy for the treatment of HD.


Price and Availability

Size Price Shipping out time Quantity
10mg USD 150 Same day
25mg USD 250 Same day
50mg USD 450 Same day
100mg USD 850 Same day
200mg USD 1450 Same day
500mg USD 3250 Same day
Inquire bulk and customized quantity

Pricing updated 2020-10-20. Prices are subject to change without notice.

VU0467154, purity > 98%, is in stock. The same day shipping out after order is received. Note: the estimated shipping out time for order > 2g may be 2 weeks.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 530355
Name: VU0467154
CAS#: 1451993-15-9
Chemical Formula: C17H15F3N4O3S2
Exact Mass: 444.0538
Molecular Weight: 444.4472
Elemental Analysis: C, 45.94; H, 3.40; F, 12.82; N, 12.61; O, 10.80; S, 14.43


Synonym: VU0467154, VU-0467154, VU 0467154

IUPAC/Chemical Name: 5-Amino-3,4-dimethyl-N-[[4-[(trifluoromethyl)sulfonyl]phenyl]methyl]thieno[2,3-c]pyridazine-6-carboxamide

InChi Key: UDSFKIFLJPECRN-UHFFFAOYSA-N

InChi Code: InChI=1S/C17H15F3N4O3S2/c1-8-9(2)23-24-16-12(8)13(21)14(28-16)15(25)22-7-10-3-5-11(6-4-10)29(26,27)17(18,19)20/h3-6H,7,21H2,1-2H3,(H,22,25)

SMILES Code: O=C(C1=C(N)C2=C(C)C(C)=NN=C2S1)NCC3=CC=C(S(=O)(C(F)(F)F)=O)C=C3


Technical Data

Appearance:
Yellow solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Certificate of Analysis:

Safety Data Sheet (SDS):

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


References

1: Gould RW, Nedelcovych MT, Gong X, Tsai E, Bubser M, Bridges TM, Wood MR, Duggan ME, Brandon NJ, Dunlop J, Wood MW, Ivarsson M, Noetzel MJ, Daniels JS, Niswender CM, Lindsley CW, Conn PJ, Jones CK. State-dependent alterations in sleep/wake architecture elicited by the M4 PAM VU0467154 - Relation to antipsychotic-like drug effects. Neuropharmacology. 2016 Mar;102:244-53. doi: 10.1016/j.neuropharm.2015.11.016. PubMed PMID: 26617071; PubMed Central PMCID: PMC4809053.

2: Wood MR, Noetzel MJ, Poslusney MS, Melancon BJ, Tarr JC, Lamsal A, Chang S, Luscombe VB, Weiner RL, Cho HP, Bubser M, Jones CK, Niswender CM, Wood MW, Engers DW, Brandon NJ, Duggan ME, Conn PJ, Bridges TM, Lindsley CW. Challenges in the development of an M(4) PAM in vivo tool compound: The discovery of VU0467154 and unexpected DMPK profiles of close analogs. Bioorg Med Chem Lett. 2016 Nov 30. pii: S0960-894X(16)31260-4. doi: 10.1016/j.bmcl.2016.11.086. [Epub ahead of print] PubMed PMID: 27939174.

3: Bubser M, Bridges TM, Dencker D, Gould RW, Grannan M, Noetzel MJ, Lamsal A, Niswender CM, Daniels JS, Poslusney MS, Melancon BJ, Tarr JC, Byers FW, Wess J, Duggan ME, Dunlop J, Wood MW, Brandon NJ, Wood MR, Lindsley CW, Conn PJ, Jones CK. Selective activation of M4 muscarinic acetylcholine receptors reverses MK-801-induced behavioral impairments and enhances associative learning in rodents. ACS Chem Neurosci. 2014 Oct 15;5(10):920-42. doi: 10.1021/cn500128b. PubMed PMID: 25137629; PubMed Central PMCID: PMC4324418.

4: Pancani T, Foster DJ, Moehle MS, Bichell TJ, Bradley E, Bridges TM, Klar R, Poslusney M, Rook JM, Daniels JS, Niswender CM, Jones CK, Wood MR, Bowman AB, Lindsley CW, Xiang Z, Conn PJ. Allosteric activation of M4 muscarinic receptors improve behavioral and physiological alterations in early symptomatic YAC128 mice. Proc Natl Acad Sci U S A. 2015 Nov 10;112(45):14078-83. doi: 10.1073/pnas.1512812112. PubMed PMID: 26508634; PubMed Central PMCID: PMC4653197.