1. GPCR/G Protein
    Neuronal Signaling
  2. mAChR
  3. VU0152099

VU0152099 

Cat. No.: HY-119226
Handling Instructions

VU0152099 is a potent, selective and brain-penetrant mAChR M4 positive allosteric modulator with an EC50 of 0.4 µM for rat M4 receptor. VU0152099 is inactive for other mAChR subtypes or other GPCRs. VU0152099 has no agonist activity but potentiated responses of M4 to acetylcholine.

For research use only. We do not sell to patients.

VU0152099 Chemical Structure

VU0152099 Chemical Structure

CAS No. : 612514-42-8

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Description

VU0152099 is a potent, selective and brain-penetrant mAChR M4 positive allosteric modulator with an EC50 of 0.4 µM for rat M4 receptor. VU0152099 is inactive for other mAChR subtypes or other GPCRs. VU0152099 has no agonist activity but potentiated responses of M4 to acetylcholine[1].

In Vitro

VU0152099 (30 µM) induces a dose-dependent leftward shift of the acetylcholine (ACh) concentration response curve (CRC) with maximal shifts of 30-fold observed with 30 µM. VU0152099 dose-dependently potentiates the response to an EC20 concentration of ACh with EC50 values of 1.2 µM, and increases the maximal response to ACh to approximately 130%. VU0152099 is a potent positive allosteric modulator that enhance the response of the M4 receptor to the endogenous agonist ACh[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

VU0152099 (56.6 mg/kg; i.p.; once) reverses Amphetamine-induced hyperlocomotion in rats[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Sprague-Dawley rats (270-300 g) injected with Amphetamine[1]
Dosage: 56.6 mg/kg
Administration: i.p.; once
Result: Reversed Amphetamine-induced hyperlocomotion in rats.
Molecular Weight

355.41

Formula

C₁₈H₁₇N₃O₃S

CAS No.
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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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VU0152099
Cat. No.:
HY-119226
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