2. Neuronal Signaling
  3. Amyloid-β
  4. AZD4694

AZD4694 (NAV4694), a fluorinated β-amyloid (Aβ) plaque neuroimaging PET radioligand, shows high affinity for Aβ fibrils (Kd = 2.3 nM).

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AZD4694 Chemical Structure

AZD4694 Chemical Structure

CAS No. : 1054629-49-0

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Based on 1 publication(s) in Google Scholar

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Description

AZD4694 (NAV4694), a fluorinated β-amyloid (Aβ) plaque neuroimaging PET radioligand, shows high affinity for Aβ fibrils (Kd = 2.3 nM)[1].

IC50 & Target

Kd: 2.3 nM (Aβ)
In Vivo

Administration of unlabeled AZD4694 to rat showed that it has a pharmacokinetic profile consistent with good PET radioligands, it quickly entered and rapidly cleared from normal rat brain tissue[1].
AZD4694 (4 mL/kg; intravenous injection) inhibits [3H]AZD2184 binding (1 nM) in a concentration-dependent manner, with a Ki of 23.1 nM, in postmortem brain sections from AD patients[1].

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

Animal Model: Male Sprague–Dawley rats (275-300 g)[1]
Dosage: 4 mL/kg
Administration: I.v.
Result: Inhibited [3H]AZD2184 binding in a concentration-dependent manner, with a Ki of 23.1 nM, in postmortem brain sections from AD patients.
Clinical Trial
Molecular Weight

258.25

Formula

C14H11FN2O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OC1=CC=C(OC(C2=CC=C(NC)N=C2F)=C3)C3=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (387.22 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 3.8722 mL 19.3611 mL 38.7222 mL
5 mM 0.7744 mL 3.8722 mL 7.7444 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (9.68 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (9.68 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
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 3.8722 mL 19.3611 mL 38.7222 mL 96.8054 mL
5 mM 0.7744 mL 3.8722 mL 7.7444 mL 19.3611 mL
10 mM 0.3872 mL 1.9361 mL 3.8722 mL 9.6805 mL
15 mM 0.2581 mL 1.2907 mL 2.5815 mL 6.4537 mL
20 mM 0.1936 mL 0.9681 mL 1.9361 mL 4.8403 mL
25 mM 0.1549 mL 0.7744 mL 1.5489 mL 3.8722 mL
30 mM 0.1291 mL 0.6454 mL 1.2907 mL 3.2268 mL
40 mM 0.0968 mL 0.4840 mL 0.9681 mL 2.4201 mL
50 mM 0.0774 mL 0.3872 mL 0.7744 mL 1.9361 mL
60 mM 0.0645 mL 0.3227 mL 0.6454 mL 1.6134 mL
80 mM 0.0484 mL 0.2420 mL 0.4840 mL 1.2101 mL
100 mM 0.0387 mL 0.1936 mL 0.3872 mL 0.9681 mL
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AZD4694 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:

AZD46941054629-49-0NAV4694AZD 4694AZD-4694NAV 4694NAV-4694Amyloid-ββ-amyloid peptideAβAbetaplaqueneuroimagingPETradioligandfibrilsInhibitorinhibitorinhibit

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