2. GPCR/G Protein Neuronal Signaling
  3. mAChR
  4. VU6000918

VU6000918 is a muscarinic acetylcholine (M4) positive allosteric modulator, with an EC50 of 19 nM for hM4.

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

VU6000918 Chemical Structure

VU6000918 Chemical Structure

CAS No. : 2101737-32-8

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Customer Review

Based on 1 publication(s) in Google Scholar

VU6000918 Related Antibodies

Top Publications Citing Use of Products

View All mAChR Isoform Specific Products:

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mAChR1 mAChR2 mAChR3 mAChR4 mAChR5

  • Biological Activity

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Description

VU6000918 is a muscarinic acetylcholine (M4) positive allosteric modulator, with an EC50 of 19 nM for hM4[1].

IC50 & Target

EC50: 19 nM (hM4)[1].
In Vitro

VU6000918 demonstrates statistically significant AHL reversal (18%) from a low oral dose of 0.03 mg/kg and reaches maximal reversal (74%) from a 3 mg/kg dose, with a resulting in vivo plasma EC50 of 74 nM (0.66 nM unbound) based on terminal concentrations measured in the study animals (1.5 hr post-administration of 17j)[1].

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

VU6000918 Related Antibodies
Molecular Weight

389.42

Formula

C18H17F2N5OS
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=C(N)C2=C(C)C(C)=NN=C2S1)NC3CN(C4=CC=CC(F)=C4F)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 : 125 mg/mL (320.99 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 2.5679 mL 12.8396 mL 25.6792 mL
5 mM 0.5136 mL 2.5679 mL 5.1358 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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  • Dilution Calculator

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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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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g

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(per animal)

μL

Number of animals

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 2.5679 mL 12.8396 mL 25.6792 mL 64.1980 mL
5 mM 0.5136 mL 2.5679 mL 5.1358 mL 12.8396 mL
10 mM 0.2568 mL 1.2840 mL 2.5679 mL 6.4198 mL
15 mM 0.1712 mL 0.8560 mL 1.7119 mL 4.2799 mL
20 mM 0.1284 mL 0.6420 mL 1.2840 mL 3.2099 mL
25 mM 0.1027 mL 0.5136 mL 1.0272 mL 2.5679 mL
30 mM 0.0856 mL 0.4280 mL 0.8560 mL 2.1399 mL
40 mM 0.0642 mL 0.3210 mL 0.6420 mL 1.6050 mL
50 mM 0.0514 mL 0.2568 mL 0.5136 mL 1.2840 mL
60 mM 0.0428 mL 0.2140 mL 0.4280 mL 1.0700 mL
80 mM 0.0321 mL 0.1605 mL 0.3210 mL 0.8025 mL
100 mM 0.0257 mL 0.1284 mL 0.2568 mL 0.6420 mL
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VU6000918 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.

Keywords:

VU60009182101737-32-8VU 6000918VU-6000918mAChRMuscarinic acetylcholine receptorM4PAMhyperlocomotionP-gpInhibitorinhibitorinhibit

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