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

CPPHA is potent and selective positive allosteric modulator (PAM) of the mGluR5 and mGluR1 (metabotropic glutamate receptor). CPPHA can potentiate responses of mGluR5 and mGluR1 to activation of these receptors. CPPHA is developed for the research of central nervous system disorders.

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

CPPHA Chemical Structure

CPPHA Chemical Structure

CAS No. : 693288-97-0

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 77 In-stock
Solution
10 mM * 1 mL in DMSO USD 77 In-stock
Solid
1 mg USD 28 In-stock
5 mg USD 70 In-stock
10 mg USD 130 In-stock
50 mg USD 390 In-stock
100 mg USD 660 In-stock
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CPPHA Related Antibodies

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  • Biological Activity

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Description

CPPHA is potent and selective positive allosteric modulator (PAM) of the mGluR5 and mGluR1 (metabotropic glutamate receptor). CPPHA can potentiate responses of mGluR5 and mGluR1 to activation of these receptors. CPPHA is developed for the research of central nervous system disorders[1][2].

IC50 & Target[1]

mGlu5 Receptor

 

In Vitro

CPPHA alone has no agonist activity[1].
CPPHA causes concentration-dependent potentiation of the response of human mGluR5 CHO cells to agonists[1].
CPPHA potentiates threshold response to glutamate in fluorometric Ca2+ assays 7- to 8-fold with EC50 values in the 400 to 800 nM range[1].
CPPHA (20 μM; 15 minutes) potentiates the response to a subthreshold concentration of DHPG (HY-12598A) on ERK and cyclic-AMP responsive element-binding protein (CREB) activity, as well as NMDA receptor subunit NR1 phosphorylation in cortical and hippocampal slices[3].

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

CPPHA Related Antibodies

Western Blot Analysis[3]

Cell Line: Rat hippocampal cells
Concentration: 20 μM
Incubation Time: 15 minutes
Result: Potentiated the DHPG (20 μM)-induced increase in phosphorylation of ERK and CREB, approaching levels seen with 100 μM DHPG alone.
Molecular Weight

406.82

Formula

C22H15ClN2O4
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1N(C(C2=CC=CC=C21)=O)CC3=CC(Cl)=CC=C3NC(C4=CC=CC=C4O)=O
Shipping

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

DMSO : 100 mg/mL (245.81 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 2.4581 mL 12.2904 mL 24.5809 mL
5 mM 0.4916 mL 2.4581 mL 4.9162 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

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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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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% Corn Oil

    Solubility: ≥ 2.5 mg/mL (6.15 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4581 mL 12.2904 mL 24.5809 mL 61.4522 mL
5 mM 0.4916 mL 2.4581 mL 4.9162 mL 12.2904 mL
10 mM 0.2458 mL 1.2290 mL 2.4581 mL 6.1452 mL
15 mM 0.1639 mL 0.8194 mL 1.6387 mL 4.0968 mL
20 mM 0.1229 mL 0.6145 mL 1.2290 mL 3.0726 mL
25 mM 0.0983 mL 0.4916 mL 0.9832 mL 2.4581 mL
30 mM 0.0819 mL 0.4097 mL 0.8194 mL 2.0484 mL
40 mM 0.0615 mL 0.3073 mL 0.6145 mL 1.5363 mL
50 mM 0.0492 mL 0.2458 mL 0.4916 mL 1.2290 mL
60 mM 0.0410 mL 0.2048 mL 0.4097 mL 1.0242 mL
80 mM 0.0307 mL 0.1536 mL 0.3073 mL 0.7682 mL
100 mM 0.0246 mL 0.1229 mL 0.2458 mL 0.6145 mL
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CPPHA 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:

CPPHA693288-97-0mGluRMetabotropic glutamate receptorsmetabotropicglutamatereceptorcentralnervoussystemdisordersInhibitorinhibitorinhibit

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