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

VU0467485 (Synonyms: AZ13713945)

Cat. No.: HY-120184 Purity: >99.0%
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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.

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VU0467485 Chemical Structure

VU0467485 Chemical Structure

CAS No. : 1451994-10-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 444 In-stock
Estimated Time of Arrival: December 31
5 mg USD 560 In-stock
Estimated Time of Arrival: December 31
10 mg USD 950 In-stock
Estimated Time of Arrival: December 31
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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].

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.

1451994-10-7

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
References

Purity: >99.0%

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Keywords:

VU0467485AZ13713945VU 0467485VU-0467485AZ 13713945AZ-13713945mAChRMuscarinic acetylcholine receptorselectiveorallybioavailableallostericmodulatorAchCNSpenetrationantipsychotic-likeactivityInhibitorinhibitorinhibit

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VU0467485
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