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

VU0467485  (Synonyms: AZ13713945)

Cat. No.: HY-120184 Purity: ≥99.0%
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.

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VU0467485 Chemical Structure

VU0467485 Chemical Structure

CAS No. : 1451994-10-7

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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].

MedChemExpress (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

Appearance

Solid

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%

COA (249 KB)

Handling Instructions (2659 KB)
References
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VU0467485 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Keywords:

VU04674851451994-10-7AZ13713945VU 0467485VU-0467485AZ 13713945AZ-13713945mAChRMuscarinic acetylcholine receptorselectiveorallybioavailableallostericmodulatorAchCNSpenetrationantipsychotic-likeactivityInhibitorinhibitorinhibit

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