2. GPCR/G Protein Neuronal Signaling
  3. mAChR
  4. VU6008055

VU6008055 (AF98943) is a brain-penetrant, orally active and selective muscarinic acetylcholine receptor subtype 4 (mAChR4) activator with human EC50 values of 73.4 nM. VU6008055 potentiates mAChR4 receptor activity in the presence of acetylcholine, and exhibits no activity at mAChR1, mAChR3, or mAChR5. VU6008055 can be used for the research of schizophrenia, parkinson’s disease, alzheimer’s disease.

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

VU6008055

VU6008055 Chemical Structure

CAS No. : 2170551-59-2

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

VU6008055 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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Description

VU6008055 (AF98943) is a brain-penetrant, orally active and selective muscarinic acetylcholine receptor subtype 4 (mAChR4) activator with human EC50 values of 73.4 nM. VU6008055 potentiates mAChR4 receptor activity in the presence of acetylcholine, and exhibits no activity at mAChR1, mAChR3, or mAChR5. VU6008055 can be used for the research of schizophrenia, parkinson’s disease, alzheimer’s disease[1].

IC50 & Target[1]

mAChR4

73.4 nM (EC50)

In Vitro

VU6008055 potently potentiates acetylcholine-evoked calcium mobilization in CHO cells expressing human M4 with an EC50 of 73.4 nM and a maximum response of 91% of the acetylcholine maximum[1].
VU6008055 potently potentiates acetylcholine-evoked calcium mobilization in CHO cells expressing rat M4 with an EC50 of 19.5 nM and a maximum response of 81% of the acetylcholine maximum[1].
VU6008055 does not inhibit CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 15 μM and does not cause time-dependent CYP inhibition[1].
VU6008055 does not form reactive intermediates/metabolites in human liver microsomes[1].
VU6008055 (10 μM) has no significant inhibitory activity against cardiac ion channels[1].
VU6008055 (4 h) shows moderate metabolic turnover in human hepatocytes, with low to high turnover across other preclinical species, and forms two predominant metabolites (MT4, MT5) in humans[1].

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

VU6008055 Related Antibodies
Parmacokinetics
Species Dose Route T1/2 MRT CLplasma Vss Tmax Cmax AUC0-∞ F
Rat[1] 1 mg/kg i.v. 2.63 h 2.65 h 4.7 mL/min/kg 0.7 L/kg / / / /
Rat[1] 3 mg/kg p.o. / / / / 1.5 h 1695 ng/mL 14801 ng·h/mL >100 %
Rat[1] 30 mg/kg p.o. / / / / 3.0 h 8985 ng/mL 101444 ng·h/mL 89 %
Dog[1] 1 mg/kg i.v. 4.17 h 5.05 h 5.0 mL/min/kg 1.4 L/kg / / / /
Dog[1] 3 mg/kg p.o. / / / / 2.0 h 766 ng/mL 5920 ng·h/mL 54 %
Monkey[1] 1 mg/kg i.v. 4.54 h 3.16 h 5.0 mL/min/kg 0.9 L/kg / / / /
Monkey[1] 3 mg/kg p.o. / / / / 2.0 h 960 ng/mL 4696 ng·h/mL 44 %
Pig[1] 2 mg/kg i.v. 5.50 h 4.9 h 7.7 mL/min/kg 2.2 L/kg / / / /
Pig[1] 5 mg/kg p.o. / / / / 1.2 h 600 ng/mL 8000 ng·h/mL 50 %
In Vivo

VU6008055 (0.1-10 mg/kg; p.o.) dose-dependently blocks Amphetamine-induced hyperlocomotion in male Sprague-Dawley rats, with a minimum effective dose of 0.3 mg/kg and up to 63% reversal at 10 mg/kg[1].
VU6008055 (0.3-3 mg/kg; p.o.) attenuates MK-801 (HY-15084B)-induced hyperlocomotion in male Sprague-Dawley rats[1].
VU6008055 (3 mg/kg; p.o.; twice daily; 7 days) does not induce tolerance to its antipsychotic-like activity in male Sprague-Dawley rats, producing ~50.6% reversal of Amphetamine-induced hyperlocomotion[1].
VU6008055 (0.3-30 mg/kg; p.o.) only moderately disrupts conditioned avoidance responses in male Wistar-Han rats at a high dose of 30 mg/kg, with no significant effect at lower doses[1].
VU6008055 (1-10 mg/kg; p.o.) dose-dependently blocks Amphetamine-induced brain activation in male Sprague-Dawley rats[1].
VU6008055 (0.1-10 mg/kg; p.o.) dose-dependently increases high gamma power, an EEG marker of arousal, in awake male Sprague-Dawley rats[1].

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

Animal Model: Sprague-Dawley (male)[1]
Dosage: 0.1 mg/kg; 0.3 mg/kg; 0.56 mg/kg; 1 mg/kg; 3 mg/kg; 10 mg/kg
Administration: p.o.
Result: Produced a robust dose-dependent blockade of Amphetamine-induced hyperlocomotion, with mean reversal percentages of 8.1% (0.1 mg/kg), 33% (0.3 mg/kg), 26% (0.56 mg/kg), 51% (1 mg/kg), 44% (3 mg/kg), and 63% (10 mg/kg).
Reached mean unbound brain concentrations ranging from 0.71 nM (0.1 mg/kg) to 68.6 nM (10 mg/kg).
Animal Model: Sprague-Dawley (male)[1]
Dosage: 0.3 mg/kg; 1 mg/kg; 3 mg/kg
Administration: p.o.
Result: Attenuated MK-801-induced hyperlocomotion, with mean reversal percentages of 7.4% (0.3 mg/kg), 24.3% (1 mg/kg), and 49.1% (3 mg/kg).
Produced a statistically significant effect at the 3 mg/kg dose.
Animal Model: Sprague-Dawley (male)[1]
Dosage: 3 mg/kg
Administration: p.o.; twice daily; 7 days
Result: Produced a 50.6% attenuation of Amphetamine-induced hyperlocomotion after chronic dosing.
Showed similar magnitude of attenuation to the 45.7% reduction observed after a single acute dose of 3 mg/kg.
Animal Model: Wistar-Han (male)[1]
Dosage: 0.3 mg/kg; 1 mg/kg; 3 mg/kg; 10 mg/kg; 30 mg/kg
Administration: p.o.
Result: Had only a moderate effect on avoidance and escape responses at 30 mg/kg.
Did not significantly disrupt avoidance responses compared to vehicle controls at lower doses (0.3-10 mg/kg).
Animal Model: Sprague-Dawley (male)[1]
Dosage: 1 mg/kg; 10 mg/kg
Administration: p.o.
Result: Dose-dependently attenuated amphetamine-evoked increases in cerebral blood volume (CBV) in the caudate putamen, nucleus accumbens, prefrontal cortex, cingulate cortex, medial dorsal thalamic nucleus, and ventral posterior lateral/ventral posterior medial thalamic nuclei.
Produced no significant CBV responses when administered alone.
Animal Model: Sprague-Dawley (male)[1]
Dosage: 0.1 mg/kg; 0.3 mg/kg; 1 mg/kg; 3 mg/kg; 10 mg/kg
Administration: p.o.
Result: Produced a robust, dose-dependent increase in high gamma power (30-100 Hz) during wake periods.
Induced significant increases at 0.3 mg/kg (78-79, 80-100 Hz), 1 mg/kg (78-100 Hz), 3 mg/kg (89-100 Hz), and 10 mg/kg (80-100 Hz).
Molecular Weight

379.48

Formula

C20H21N5OS
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

CC1=NN=C(SC2=C3N=CN=C2NCC4=CC=C(C(C)(O)C)C=C4)C3=C1C
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 : 100 mg/mL (263.52 mM; Need ultrasonic; 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 2.6352 mL 13.1759 mL 26.3519 mL
5 mM 0.5270 mL 2.6352 mL 5.2704 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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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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
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 2.6352 mL 13.1759 mL 26.3518 mL 65.8796 mL
5 mM 0.5270 mL 2.6352 mL 5.2704 mL 13.1759 mL
10 mM 0.2635 mL 1.3176 mL 2.6352 mL 6.5880 mL
15 mM 0.1757 mL 0.8784 mL 1.7568 mL 4.3920 mL
20 mM 0.1318 mL 0.6588 mL 1.3176 mL 3.2940 mL
25 mM 0.1054 mL 0.5270 mL 1.0541 mL 2.6352 mL
30 mM 0.0878 mL 0.4392 mL 0.8784 mL 2.1960 mL
40 mM 0.0659 mL 0.3294 mL 0.6588 mL 1.6470 mL
50 mM 0.0527 mL 0.2635 mL 0.5270 mL 1.3176 mL
60 mM 0.0439 mL 0.2196 mL 0.4392 mL 1.0980 mL
80 mM 0.0329 mL 0.1647 mL 0.3294 mL 0.8235 mL
100 mM 0.0264 mL 0.1318 mL 0.2635 mL 0.6588 mL
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VU6008055 Related Classifications

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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:

VU60080552170551-59-2AF98943VU 6008055VU-6008055AF 98943AF-98943mAChRMuscarinic acetylcholine receptorM3 muscarinic receptorsM1 muscarinic receptorsparkinson’s diseasealzheimer’s diseaseM2 muscarinic receptorsSprague-Dawley ratsM5 muscarinic receptorsmuscarinic acetylcholine receptor subtype 4schizophreniaCHO cellsInhibitorinhibitorinhibit

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