VU0453595

VU0453595 is a highly selective, systemically active M1 positive allosteric modulator (PAM, EC50=2140 nM) for the research of schizophrenia.

Product information

CAS Number: 1432436-13-9

Molecular Weight: 322.34

Formula: C18H15FN4O

Chemical Name: 6-{[2-fluoro-4-(1-methyl-1H-pyrazol-4-yl)phenyl]methyl}-5H,6H,7H-pyrrolo[3,4-b]pyridin-5-one

Smiles: CN1C=C(C=N1)C1C=C(F)C(CN2CC3=NC=CC=C3C2=O)=CC=1

InChiKey: LIZQOZALTSDKFU-UHFFFAOYSA-N

InChi: InChI=1S/C18H15FN4O/c1-22-9-14(8-21-22)12-4-5-13(16(19)7-12)10-23-11-17-15(18(23)24)3-2-6-20-17/h2-9H,10-11H2,1H3

Technical Data

Appearance: Solid Power

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

Solubility: DMSO : 100 mg/mL (310.23 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

Application of M1 PAM VU0453595 (3 μM) induces a transient increase in excitability of medium spiny neurons (MSNs).

In Vivo:

VU0453595 potentiates M1-mediated muscarinic long-term depression (mLTD). VU0453595 (1-10 mg/kg; i.p.) reverses behavioral deficits induced by repeated phencyclidine (PCP) administration.

References:

1. Lv X, Dickerson JW, Rook JM, Lindsley CW, Conn PJ, Xiang Z. M(1) muscarinic activation induces long-lasting increase in intrinsic excitability of striatal projection neurons. Neuropharmacology. 2017 May 15;118:209-222.
2. Panarese JD, Cho HP, Adams JJ, Nance KD, Garcia-Barrantes PM, Chang S, Morrison RD, Blobaum AL, Niswender CM, Stauffer SR, Conn PJ, Lindsley CW. Further optimization of the M1 PAM VU0453595: Discovery of novel heterobicyclic core motifs with improved CNS penetration. Bioorg Med Chem Lett. 2016 Aug 1;26(15):3822-5.
3. Ghoshal A, Rook JM, Dickerson JW, Roop GN, Morrison RD, Jalan-Sakrikar N, Lamsal A, Noetzel MJ, Poslusney MS, Wood MR, Melancon BJ, Stauffer SR, Xiang Z, Daniels JS, Niswender CM, Jones CK, Lindsley CW, Conn PJ. Potentiation of M1 Muscarinic Receptor Reverses Plasticity Deficits and Negative and Cognitive Symptoms in a Schizophrenia Mouse Model. Neuropsychopharmacology. 2016 Jan;41(2):598-610.

Products are for research use only. Not for human use.