1. GPCR/G Protein
    Neuronal Signaling
  2. mAChR
  3. VU0467485

VU0467485  (Synonyms: AZ13713945)

Cat. No.: HY-120184 Purity: 97.03%
COA Handling Instructions

VU0467485 (AZ13713945) is a potent, selective, and orally bioavailable muscarinic acetylcholine receptor 4 (M4) positive allosteric modulator (PAM). VU0467485 (AZ13713945) potentiates activity of ACh at M4 with EC50s of 26.6 nM and 78.8 nM at rat and human M4 receptors, respectively. VU0467485 (AZ13713945) shows selectivity for M4 over human and rat M1/2/3/5. VU0467485 (AZ13713945) displays moderate to high CNS penetration. VU0467485 (AZ13713945) has antipsychotic-like activity.

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

VU0467485 Chemical Structure

VU0467485 Chemical Structure

CAS No. : 1451994-10-7

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10 mM * 1 mL in DMSO USD 222 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

VU0467485 (AZ13713945) is a potent, selective, and orally bioavailable muscarinic acetylcholine receptor 4 (M4) positive allosteric modulator (PAM). VU0467485 (AZ13713945) potentiates activity of ACh at M4 with EC50s of 26.6 nM and 78.8 nM at rat and human M4 receptors, respectively. VU0467485 (AZ13713945) shows selectivity for M4 over human and rat M1/2/3/5. VU0467485 (AZ13713945) displays moderate to high CNS penetration. VU0467485 (AZ13713945) has antipsychotic-like activity[1].

In Vivo

VU0467485 (1-10 mg/kg; p.o.) has antipsychotic-like activity in an amphetamine-induced hyperlocomotion (AHL) rat model[1].
VU0467485 (3 mg/kg; p.o.) treatment displays that the Cmax, AUCo-inf and elimination t1/2 were 1.2 μM, 3.8 μM•h and 4.2 hours, respectively[1].

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

Animal Model: Sprague Dawley rats (amphetamine-induced hyperlocomotion rat model) [1]
Dosage: 1, 3, 10 mg/kg
Administration: Oral administration
Result: Dose-dependently reverses AHL.
Animal Model: Male sprague Dawley rats[1]
Dosage: Oral administration (Pharmacokinetic Analysis)
Administration: 3 mg/kg
Result: The Cmax, AUCo-inf and elimination t1/2 were 1.2 μM, 3.8 μM•h and 4.2 hours, respectively.
Molecular Weight

360.41

Formula

C17H17FN4O2S

CAS No.
SMILES

O=C(C1=C(N)C2=C(C)C(C)=NN=C2S1)NCC3=CC=C(OC)C(F)=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 20 mg/mL (55.49 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7746 mL 13.8731 mL 27.7462 mL
5 mM 0.5549 mL 2.7746 mL 5.5492 mL
10 mM 0.2775 mL 1.3873 mL 2.7746 mL
*Please refer to the solubility information to select the appropriate solvent.
Purity & Documentation

Purity: ≥99.0%

References
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