2. GPCR/G Protein Neuronal Signaling
  3. mGluR
  4. ADX71743

ADX71743 is a highly selective, noncompetitive and brain-penetrant metabotropic glutamate receptor 7 negative allosteric modulator (mGlu7 NAM). ADX71743 can cross the blood-brain barrier (BBB) and possesses anxiolytic activity..

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ADX71743

ADX71743 構造式

CAS 番号 : 1431641-29-0

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 413 在庫あり
Solution
10 mM * 1 mL in DMSO USD 413 在庫あり
Solid
1 mg $150 在庫あり
5 mg $376 在庫あり
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ADX71743 関連抗体

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製品説明

ADX71743 is a highly selective, noncompetitive and brain-penetrant metabotropic glutamate receptor 7 negative allosteric modulator (mGlu7 NAM). ADX71743 can cross the blood-brain barrier (BBB) and possesses anxiolytic activity.[1][2].

IC50 & Target[1]

mGlu7

 

体外実験

ADX71743 has an IC50 of 300 nM in-house cell lines. Pretreatment of ADX71743 (3 μM; for 20 min) before high-frequency stimulation (HFS) results in an almost complete blockade of LTP induction[1].
ADX71743 (0.1, 10 μM) reverses L-AP4-induced depression of synaptic transmission and results in a concentration-dependent reversal of the L-AP4-induced depression. 0.1 μM ADX71743 reverses the effects of L-AP4 by 11% and 10 μM results in a 20% reversal[2].
ADX71743 can against an EC80 of glutamate (IC50 of 22 nM) as well as against an EC80 of L-AP4 (IC50 of 125 nM)[2].

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

ADX71743 関連抗体
体内実験

ADX71743 (50, 100, 150 mg/kg; SC) results in robust reductions in numbers of buried marbles to near maximal levels at lower doses (50 and 100 mg/kg)[2].
ADX71743 (12.5, 100 mg/kg for mice and 100 mg/kg for rat; SC) has a T1/2 of 0.68, 0.40 hours, a Cmax of 1380, 12766 ng/ml of 12.5 mg/kg and 100 mg/kg in mice[2].
ADX71743 (12.5 and 100 mg/kg, subcutaneous injection, single dose) demonstrates bioavailability in C57Bl6/J mice, penetrates the blood-brain barrier (CSF/plasma concentration ratio was 5.3% at Cmax), shows linear increases in plasma exposure with increasing dose, and is cleared rapidly (half-life approximately 0.5 hours); similar pharmacokinetic characteristics are observed in Sprague-Dawley rats (100 mg/kg, subcutaneous injection, single dose), with a plasma Cmax of 16800 ng/ml and a half-life of 1.5 hours[3].

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

Animal Model: Adult male C57Bl6/J mice (24-30 g)[2]
Dosage: 50, 100, 150 mg/kg
Administration: SC
Result: Resulted in robust reductions in numbers of buried marbles to near maximal levels at lower doses (50 and 100 mg/kg).
Animal Model: Adult male C57Bl6/J mice (24-30 g) and Sprague-Dawley rats (250-350 g)[2]
Dosage: 12.5, 100 mg/kg for mice and 100 mg/kg for rat (Pharmacokinetic Analysis)
Administration: SC
Result: Had a T1/2 of 0.68, 0.40 hours, a Cmax of 1380, 12766 ng/ml of 12.5 mg/kg and 100 mg/kg in mice.
Had a T1/2 of 1.5 hours, a Cmax of 16800 ng/ml of 100 mg/kg in rat.
分子量

269.34

分子式

C17H19NO2
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O=C1C2=C(OC(CC)=N2)CC(C3=C(C=C(C)C=C3)C)C1
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 100 mg/mL (371.28 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 3.7128 mL 18.5639 mL 37.1278 mL
5 mM 0.7426 mL 3.7128 mL 7.4256 mL
10 mM 0.3713 mL 1.8564 mL 3.7128 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)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

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体積 （開始）

V1

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C2

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体積 （終了）

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体内:

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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (9.28 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 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: ≥ 2.5 mg/mL (9.28 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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mg/kg

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(per animal)

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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.
純度とドキュメンテーション

純度: 99.46%

COA (247 KB) HNMR (162 KB) LCMS (102 KB)

取扱説明書 (2659 KB)
参考文献

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 3.7128 mL 18.5639 mL 37.1278 mL 92.8195 mL
5 mM 0.7426 mL 3.7128 mL 7.4256 mL 18.5639 mL
10 mM 0.3713 mL 1.8564 mL 3.7128 mL 9.2819 mL
15 mM 0.2475 mL 1.2376 mL 2.4752 mL 6.1880 mL
20 mM 0.1856 mL 0.9282 mL 1.8564 mL 4.6410 mL
25 mM 0.1485 mL 0.7426 mL 1.4851 mL 3.7128 mL
30 mM 0.1238 mL 0.6188 mL 1.2376 mL 3.0940 mL
40 mM 0.0928 mL 0.4641 mL 0.9282 mL 2.3205 mL
50 mM 0.0743 mL 0.3713 mL 0.7426 mL 1.8564 mL
60 mM 0.0619 mL 0.3094 mL 0.6188 mL 1.5470 mL
80 mM 0.0464 mL 0.2320 mL 0.4641 mL 1.1602 mL
100 mM 0.0371 mL 0.1856 mL 0.3713 mL 0.9282 mL
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ADX71743 Related Classifications

  • Molarity Calculator

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The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

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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:

ADX717431431641-29-0ADX 71743ADX-71743mGluRMetabotropic glutamate receptorsbrain-penetrantbbbmetabotropicglutamatereceptorNAManxiolytic-likeInhibitorinhibitorinhibit

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製品番号:
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