A selective agonist of M1 mAChRs (Ki = 9.91 µM); selective for M1 over M2-M5 mAChRs (Kis = 21.4-50 µM in CHO cells); increases calcium mobilization and activates the ERK signaling pathway (EC50 = 1.6 and 37 µM

VU0357017 (hydrochloride) – 10 mg

Brand:
Cayman
CAS:
1135242-13-5
Storage:
-20
UN-No:
Non-Hazardous - /

VU0357017 is an allosteric agonist of M1 muscarinic acetylcholine receptors (mAChRs; Ki = 9.91 µM in CHO cells).{40723} In vitro, it is selective for M1 over M2-M5 mAChRs (Kis = 21.4-50 µM in CHO cells). VU0357017 induces concentration-dependent increases in calcium mobilization and activates the ERK signaling pathway with EC50 values of 1.6 and 37 µM, respectively, in CHO cells expressing human recombinant M1 receptors.{37300} In vivo, VU0357017 crosses the blood-brain barrier and reverses scopolamine-induced deficits in contextual fear conditioning in rats when used at a dose of 10 mg/kg.{40724}  

 

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SKU: 11939 - 10 mg Category:

Description

A selective agonist of M1 mAChRs (Ki = 9.91 µM); selective for M1 over M2-M5 mAChRs (Kis = 21.4-50 µM in CHO cells); increases calcium mobilization and activates the ERK signaling pathway (EC50 = 1.6 and 37 µM, respectively, in CHO cells expressing human recombinant M1 receptors); reverses scopolamine-induced deficits in contextual fear conditioning in rats (10 mg/kg)

Formal name: 4-[[2-[(2-methylbenzoyl)amino]ethyl]amino]-1-piperidinecarboxylic acid, ethyl ester, monohydrochloride

Synonyms:  CID-25010775

Molecular weight: 369.9

CAS: 1135242-13-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Neuroscience|Behavioral Neuroscience|Learning & Memory

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