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PIPE-359

Chemical Structure : PIPE-359

CAS No.: 2401785-66-6

PIPE-359 (PIPE359)

Catalog No.: PC-20509Not For Human Use, Lab Use Only.

PIPE-359 (PIPE359) is a potent, selective and brain-penetrant antagonist of muscarinic acetylcholine receptor subtype 1 (M1 mAChR) with IC50 of 1.8 nM and Ki of 0.14 nM (hM1R).

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

PIPE-359 (PIPE359) is a potent, selective and brain-penetrant antagonist of muscarinic acetylcholine receptor subtype 1 (M1 mAChR) with IC50 of 1.8 nM and Ki of 0.14 nM (hM1R).
PIPE-359 exhibited good-to-excellent selectivities versus the hM2R, hM3R, and hM4R in both functional and binding settings.
PIPE-359 (30 mg/kg po qd) exhibited robust efficacy in mouse myelin oligodendrocyte glycoprotein (MOG)-induced experimental autoimmune encephalitis (EAE), a preclinical model for multiple sclerosis.

Physicochemical Properties

M.Wt 467.56
Formula C22H21N5O3S2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N#CC1=CN=C(N2C3CN(C(CCS(=O)(C4=C(SC=N5)C5=CC=C4)=O)=O)CC2CC3)C=C1

References

1. Thomas O Schrader, et al. ACS Med Chem Lett. 2020 Dec 24;12(1):155-161.

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