1. GPCR/G Protein
    Neuronal Signaling
  2. mAChR
  3. VU 6008667

VU 6008667 

Cat. No.: HY-101281 Purity: 99.05% ee.: 98.87%
Handling Instructions

VU 6008667 is a selective negative allosteric modulator of M5 NAM with IC50s of 1.2 μM and 1.6 μM for human M5 and rat M5, respectively. High CNS penetration.

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

VU 6008667 Chemical Structure

VU 6008667 Chemical Structure

CAS No. : 2092923-21-0

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 174 In-stock
Estimated Time of Arrival: December 31
5 mg USD 180 In-stock
Estimated Time of Arrival: December 31
10 mg USD 330 In-stock
Estimated Time of Arrival: December 31
25 mg USD 750 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1350 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2250 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of VU 6008667:

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

VU 6008667 is a selective negative allosteric modulator of M5 NAM with IC50s of 1.2 μM and 1.6 μM for human M5 and rat M5, respectively. High CNS penetration[1].

IC50 & Target

IC50: 1.2 μM (Human M5); 1.6 μM (Rat M5)[1]

In Vivo

VU 6008667 (1 mg/kg)/PO (3 mg/kg, solution dose) displays a diminished elimination half-life (t1/2=2.3 hr) driven by a smaller volume (Vss=7.4 L/kg) and higher clearance (CLp=82 mL/min/kg), with moderate oral bioavailability (17% F)[1].

Animal Model: RAT (PK study)[1]
Dosage: 1 mg/kg; 3 mg/kg
Administration: oral adminstration
Result: Had a desired short half-life in rat (t1/2= 2.3 hr), with moderate oral bioavailability (17% F).
Molecular Weight

438.85

Formula

C₂₄H₁₇ClF₂N₂O₂

CAS No.

2092923-21-0

SMILES

O=C1C2=CC=CC=C2[[email protected]]3(C4=CC=C(Cl)C(C)=C4)N1CCN3C(C5=CC(F)=C(F)C=C5)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (227.87 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2787 mL 11.3934 mL 22.7868 mL
5 mM 0.4557 mL 2.2787 mL 4.5574 mL
10 mM 0.2279 mL 1.1393 mL 2.2787 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.70 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.70 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

VU 6008667VU6008667VU-6008667mAChRMuscarinic acetylcholine receptorCNSpenetrationpenetrateInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product name:
VU 6008667
Cat. No.:
HY-101281
Quantity:
MCE Japan Authorized Agent: