CPPHA

Cat. No.: HY-14612 Purity: 98.04%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

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	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 77	In-stock	Estimated Time of Arrival: December 31
Solid
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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mGluR1 mGluR2 mGluR3 mGluR4 mGluR5 mGluR6 mGluR7 mGluR8 mGluR

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

mGlu5 Receptor

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	< 1 μM Compound: 2, CPPHA	Activity at rat mGluR5 expressed in CHO cells assessed as potentiation of glutamate response by FLIPR assay Activity at rat mGluR5 expressed in CHO cells assessed as potentiation of glutamate response by FLIPR assay	[PMID: 17210250]
CHO	EC₅₀	0.25 μM Compound: 2, CPPHA	Activity at human mGluR5 expressed in CHO cells assessed as potentiation of glutamate response by FLIPR assay Activity at human mGluR5 expressed in CHO cells assessed as potentiation of glutamate response by FLIPR assay	[PMID: 17210250]
HEK293	IC₅₀	> 10000 nM Compound: CPPHA	Displacement of [3H]-MethoxyPEPy from human mGlu5 receptor expressed in HEK293 cell membranes after 8 hrs by micro beta scintillation counting analysis Displacement of [3H]-MethoxyPEPy from human mGlu5 receptor expressed in HEK293 cell membranes after 8 hrs by micro beta scintillation counting analysis	[PMID: 27994742]

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.

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

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
10 mM	0.2458 mL	1.2290 mL	2.4581 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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)

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

Purity: 98.04%

Select Batch:

Data Sheet (277 KB) SDS (459 KB)

COA (253 KB) HNMR (244 KB) RP-HPLC (248 KB) MS (68 KB)

Handling Instructions (2659 KB)

References

[1]. O'Brien JA, et al. A novel selective allosteric modulator potentiates the activity of native metabotropic glutamate receptor subtype 5 in rat forebrain. J Pharmacol Exp Ther. 2004 May;309(2):568-77. [Content Brief]

[2]. N-{4-Chloro-2-[(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl]phenyl}-2-hydroxybenzamide (CPPHA) acts through a novel site as a positive allosteric modulator of group 1 metabotropic glutamate receptors. Mol Pharmacol. 2008 Mar;73(3):909-18. [Content Brief]

[3]. Liu F, et al. The effect of mGlu5 receptor positive allosteric modulators on signaling molecules in brain slices. Eur J Pharmacol. 2006 May 1;536(3):262-8. [Content Brief]

[4]. Zhang Y, et al. Allosteric potentiators of metabotropic glutamate receptor subtype 5 have differential effects on different signaling pathways in cortical astrocytes. J Pharmacol Exp Ther. 2005 Dec;315(3):1212-9. [Content Brief]

Complete Stock Solution Preparation Table

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

CPPHA Related Classifications

Neurological Disease

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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