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

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
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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].

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

Formula

C17H17FN4O2S
CAS No.
Appearance

Solid

Color

Light yellow to yellow

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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: ≥99.0%

COA (249 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7746 mL 13.8731 mL 27.7462 mL 69.3654 mL
5 mM 0.5549 mL 2.7746 mL 5.5492 mL 13.8731 mL
10 mM 0.2775 mL 1.3873 mL 2.7746 mL 6.9365 mL
15 mM 0.1850 mL 0.9249 mL 1.8497 mL 4.6244 mL
20 mM 0.1387 mL 0.6937 mL 1.3873 mL 3.4683 mL
25 mM 0.1110 mL 0.5549 mL 1.1098 mL 2.7746 mL
30 mM 0.0925 mL 0.4624 mL 0.9249 mL 2.3122 mL
40 mM 0.0694 mL 0.3468 mL 0.6937 mL 1.7341 mL
50 mM 0.0555 mL 0.2775 mL 0.5549 mL 1.3873 mL
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  • 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.

Keywords:

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

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