1. GPCR/G Protein
  2. mGluR

ADX88178 

Cat. No.: HY-18654 Purity: 98.59%
Handling Instructions

ADX88178 is a potent positive allosteric modulator for metabotropic glutamate receptor 4 (mGluR4) with EC50 of 4 nM for human mGluR4.

For research use only. We do not sell to patients.
ADX88178 Chemical Structure

ADX88178 Chemical Structure

CAS No. : 1235318-89-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 395 In-stock
1 mg USD 132 In-stock
5 mg USD 396 In-stock
10 mg USD 600 In-stock
50 mg USD 1800 In-stock
100 mg USD 2520 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

ADX88178 is a potent positive allosteric modulator for metabotropic glutamate receptor 4 (mGluR4) with EC50 of 4 nM for human mGluR4.

IC50 & Target

EC50: 4 nM (human mGluR4)[1]

In Vitro

ADX88178 is developed as a potent and selective mGluR4 positive allosteric modulator. ADX88178 is used as a novel radioligand for imaging of metabotropic glutamate receptor subtype 4 (mGluR4). ADX88178 potentiates glutamate-mediated activation of human mGluR4 with EC50 values of 4 nM without significant effects on other mGluRs (EC50 > 30 μM)[1]. ADX88178 is novel potent, selective, and brain-penetrant positive allosteric modulator of the mGlu4. Microglia are pretreated with 1, 10 or 100 nM ADX88178 or 100 nM LAP4 for 30 min followed by LPS treatment for 24 h prior to collecting culture supernatant for ELISA measurement of TNFα levels. The pre-treatment with ADX88178 and LAP4 both significantly attenuate LPS-induced TNFα levels. As little as 1 nM of ADX88178 is sufficient to inhibit TNFα, and is as effective at concentrations of 10 and 100 nM[2].

In Vivo

In mice, ADX88178 (1-30 mg/kg p.o.) dose-dependently increases the number of open-arm entries. Specifically, at 3, 10, and 30 mg/kg ADX88178, there are 5-, 7-, and almost 13-fold increases in the number of open-arm entries, respectively, when compared with the vehicle-treated controls. Also, ADX88178 dose-dependently increases the time spent in the open arms. Specifically, at 3, 10, and 30 mg/kgADX88178, there are 8-, 12-, and 24-fold increases in the time spent in the open arms when compared with the vehicle-treated controls. In rats, ADX88178 (10-100 mg/kg p.o.) dose-dependently increases the number of open-arm entries in the rat EPM test. Specifically, at 10, 30, and 100 mg/kg ADX88178, there are 5-, 8-, and more than 10-fold increases in the number of open-arm entries, respectively, when compared with the vehicle-treated controls. Also, ADX88178 dose-dependently increases the time spent in the open arms. Specifically, at 10, 30, and 100 mg/kg ADX88178, there are 7.5-, 11-, and 13-fold increases in time spent in the open arms when compared with the vehicle-treated controls[3].

References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 3.6720 mL 18.3601 mL 36.7202 mL
5 mM 0.7344 mL 3.6720 mL 7.3440 mL
10 mM 0.3672 mL 1.8360 mL 3.6720 mL
Please refer to the solubility information to select the appropriate solvent.
Cell Assay
[2]

ADX88178 is dissolved in DMSO and stored, and then diluted with appropriate medium before use[2].

After adhesion to the chamber slides, microglia from WT and mGlu4 KO microglia pre-treated with 1 nM, 10 nM, 100 nM ADX88178, or 100 nM L-AP4. Each treatment is performed in quadruplicate. Thirty minutes after treatment with ADX88178 or L-AP4, 100 ng/mL LPS is added to the cultures and the cells are incubated at 37 °C for an additional 24 h. At the end of the 24 h treatment period, media is collected and analyzed for TNFα, and the cells are for iNOS and MHC II expression by immunocytochemistry[2].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[3]

ADX88178 is prepared in 1% carboxymethyl cellulose (CMC)[3].

Mice and Rats[3] Male mice (n=8-10/group) are treated orally (p.o.) via gavage with vehicle [1% carboxymethyl cellulose (CMC)], ADX88178 (1, 3, 10 and 30 mg/kg) or Diazepam (1.5 mg/kg). Male rats (n=10/group) are treated p.o. with vehicle (1% CMC), ADX88178 (10, 30, and 100 mg/kg), or Diazepam (3 mg/kg). After 60 minutes, animals are individually placed in the center of the maze (facing one of the closed arms) and left to explore for 5 minutes. A terminal blood sample is collected from all ADX88178-treated animals at the end of the experiment, and plasma is analyzed for the pharmacokinetic studies. The number of open-arm and closed-arm entries, as well as the time (seconds) spent in the open arms of the maze, is analyzed by one-way analysis of variance followed by Dunnett’s test.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

272.33

Formula

C₁₂H₁₂N₆S

CAS No.

1235318-89-4

SMILES

CC1=C(C2=CNN=C2)N=C(NC3=NC=CC(C)=N3)S1

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 50 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
ADX88178
Cat. No.:
HY-18654
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