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

CPPHA 

Cat. No.: HY-14612 Purity: 95.01%
Handling Instructions

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
10 mM * 1 mL in DMSO USD 77 In-stock
Estimated Time of Arrival: December 31
5 mg USD 70 In-stock
Estimated Time of Arrival: December 31
10 mg USD 130 In-stock
Estimated Time of Arrival: December 31
50 mg USD 390 In-stock
Estimated Time of Arrival: December 31
100 mg USD 660 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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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].

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

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.

693288-97-0

SMILES

O=C1N(CC2=CC(Cl)=CC=C2NC(C3=CC=CC=C3O)=O)C(C4=CC=CC=C41)=O

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 (245.81 mM; Need ultrasonic)

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
10 mM 0.2458 mL 1.2290 mL 2.4581 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 2.5 mg/mL (6.15 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

CPPHAmGluRMetabotropic glutamate receptorsmetabotropicglutamatereceptorcentralnervoussystemdisordersInhibitorinhibitorinhibit

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CPPHA
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