2. GPCR/G Protein Neuronal Signaling PI3K/Akt/mTOR MAPK/ERK Pathway Stem Cell/Wnt Apoptosis Metabolic Enzyme/Protease
  3. mGluR Akt ERK Caspase Mitochondrial Metabolism
  4. CDPPB

CDPPB is a selective, orally active and brain-penetrant mGluR5 allosteric modulator. CDPPB increases AKT and ERK1/2 activation and augments the BDNF mRNA. CDPPB inhibits caspase-3 activation and mitochondrial dysfunction. CDPPB improves cognitive impairment, depression, and Huntington's disease.

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CDPPB

CDPPB Estructura química

No. CAS : 781652-57-1

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10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

CDPPB Related Antibodies

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mGluR1 mGluR2 mGluR3 mGluR4 mGluR5 mGluR6 mGluR7 mGluR8 mGluR

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Akt Akt1 Akt2 Akt3

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

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Descripciòn

CDPPB is a selective, orally active and brain-penetrant mGluR5 allosteric modulator. CDPPB increases AKT and ERK1/2 activation and augments the BDNF mRNA. CDPPB inhibits caspase-3 activation and mitochondrial dysfunction. CDPPB improves cognitive impairment, depression, and Huntington's disease[1][2][3][4][5][6][7][8][9].

IC50 & Target[1]

mGluR5

27 nM (EC50)

Cellular Effect
Cell Line Type Value Description References
CHO EC50
10 1
Compound: 8q
Effective concentration against metabotropic glutamate receptor 5 of human transfected into CHO cells
Effective concentration against metabotropic glutamate receptor 5 of human transfected into CHO cells
[PMID: 15537338]
CHO EC50
10 1
Compound: 8q
Effective concentration against metabotropic glutamate receptor 5 of human transfected into CHO cells
Effective concentration against metabotropic glutamate receptor 5 of human transfected into CHO cells
[PMID: 15537338]
CHO EC50
27 1
Compound: 6, CDPPB
Positive allosteric modulation of human mGluR5 stably expressed in CHO cells assessed as Ca2+ flux by FLIPR assay
Positive allosteric modulation of human mGluR5 stably expressed in CHO cells assessed as Ca2+ flux by FLIPR assay
[PMID: 24050755]
CHO EC50
27 1
Compound: 6, CDPPB
Positive allosteric modulation of human mGluR5 stably expressed in CHO cells assessed as Ca2+ flux by FLIPR assay
Positive allosteric modulation of human mGluR5 stably expressed in CHO cells assessed as Ca2+ flux by FLIPR assay
[PMID: 24050755]
CHO EC50
27 1
Compound: 6, CDPPB
Positive allosteric modulation of human mGluR5 stably expressed in CHO cells assessed as Ca2+ flux by FLIPR assay
Positive allosteric modulation of human mGluR5 stably expressed in CHO cells assessed as Ca2+ flux by FLIPR assay
[PMID: 24050755]
CHO EC50
98 1
Compound: 6, CDPPB
Positive allosteric modulation of rat mGluR5 stably expressed in CHO cells assessed as Ca2+ flux by FLIPR assay
Positive allosteric modulation of rat mGluR5 stably expressed in CHO cells assessed as Ca2+ flux by FLIPR assay
[PMID: 24050755]
CHO EC50
98 1
Compound: 6, CDPPB
Positive allosteric modulation of rat mGluR5 stably expressed in CHO cells assessed as Ca2+ flux by FLIPR assay
Positive allosteric modulation of rat mGluR5 stably expressed in CHO cells assessed as Ca2+ flux by FLIPR assay
[PMID: 24050755]
CHO EC50
98 1
Compound: 6, CDPPB
Positive allosteric modulation of rat mGluR5 stably expressed in CHO cells assessed as Ca2+ flux by FLIPR assay
Positive allosteric modulation of rat mGluR5 stably expressed in CHO cells assessed as Ca2+ flux by FLIPR assay
[PMID: 24050755]
HEK293 EC50
176 1
Compound: 1, CDPPB
Positive allosteric modulation of human mGluR5a transfected in HEK293 cells by calcium mobilization assay
Positive allosteric modulation of human mGluR5a transfected in HEK293 cells by calcium mobilization assay
[PMID: 23947773]
HEK293 EC50
176 1
Compound: 1, CDPPB
Positive allosteric modulation of human mGluR5a transfected in HEK293 cells by calcium mobilization assay
Positive allosteric modulation of human mGluR5a transfected in HEK293 cells by calcium mobilization assay
[PMID: 23947773]
HEK293 EC50
176 1
Compound: 1, CDPPB
Positive allosteric modulation of human mGluR5a transfected in HEK293 cells by calcium mobilization assay
Positive allosteric modulation of human mGluR5a transfected in HEK293 cells by calcium mobilization assay
[PMID: 23947773]
In Vitro

CDPPB (above 1 μM) exhibits agonist-like activity on CHO cells expressing mGluR5[1].
CDPPB (0.1 mM, 30 min) inhibits SO2-induced protein radical formation and mitochondrial dysfunction through activation of Akt in mouse hippocampal HT22 cells[2].
CDPPB (0.02-0.2 mM, 2 h before traumatic neuronal injury) suppresses the increase of LDH release and caspase-3 activation induced by traumatic neuronal injury in a dose-dependent manner[3].

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

CDPPB Related Antibodies
In Vivo

CDPPB (1-30 mg/kg, s.c., 20 min prior to Amphetamine injection (locomotor test) or 20 min after Amphetamine injection (PPI test)) suppresses Amphetamine-induced locomotor activity without affecting spontaneous locomotor activity and reverses Amphetamine-induced deficits in PPI in rats[1].
CDPPB (10 mg/kg/day, i.p., 14 days) improves Phencyclidine-induced cognitive deficits in mice[4].
CDPPB (5 mg/kg, i.p., 14 days) improves cognitive impairment and partially reverses the lesion-induced changes in eNOS and nNOS expressions in olfactory bulbectomized rats[5].
CDPPB (1.5 mg/kg, s.c., 18 weeks) ameliorates pathology and phenotypic signs of Huntington's disease mice[6].
CDPPB (20 mg/kg, p.o., single) attenuates depressive-like behavior induced by repeated social defeat stress in mice[7].
CDPPB (10 mg/kg, i.p., adolescence) reverses MK-801 (HY-15084B)-induced locomotor hyperactivity and anhedonia in mice[8].
CDPPB (1-5 mg/kg, i.p., 8 days) improves neuronal survival and prevents memory deficits in C57BL/6 mice injected intrahippocampally with Aβ. [9].

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

Animal Model: Male Sprague-Dawley rats (250–300 g at the time of surgery, age not specified in this context for this part) with olfactory bulbectomy[5]
Dosage: 2.5 or 5 mg/kg, dissolved in 0.5% methylcellulose
Administration: Intraperitoneal injection (i.p.), once daily for 14 days
Result: Reversed the cognitive impairment in the passive avoidance test at 5 mg/kg.
Partially abolished the lesion-induced increase in total eNOS protein in the prefrontal cortex.
Reversed the lesion - induced changes in both total eNOS protein and D/M ratio in the striatum.
Had no impact on the lesion - induced decrease in total nNOS protein in the hippocampus but counteracted the lesion - induced increase in total nNOS protein in the striatum.
Decreased DDAH1 expression in the hippocampus and striatum of lesioned animals and reduced RAGEs expression in the hippocampi of sham animals and in the striata of OB animals.
Peso molecular

364.40

Fòrmula

C23H16N4O
No. CAS
Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1=CC(C2=CC=CC=C2)=NN1C3=CC=CC=C3)C4=CC=CC(C#N)=C4
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvente y solubilidad
In Vitro: 

DMSO : 100 mg/mL (274.42 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 2.7442 mL 13.7212 mL 27.4424 mL
5 mM 0.5488 mL 2.7442 mL 5.4885 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.

  • Calculadora de molaridad

  • Calculadora de dilución

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
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: ≥ 5 mg/mL (13.72 mM); Clear solution

    This protocol yields a clear solution of ≥ 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 (50.0 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.
Pureza y Documentación
Referencias

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 2.7442 mL 13.7212 mL 27.4424 mL 68.6059 mL
5 mM 0.5488 mL 2.7442 mL 5.4885 mL 13.7212 mL
10 mM 0.2744 mL 1.3721 mL 2.7442 mL 6.8606 mL
15 mM 0.1829 mL 0.9147 mL 1.8295 mL 4.5737 mL
20 mM 0.1372 mL 0.6861 mL 1.3721 mL 3.4303 mL
25 mM 0.1098 mL 0.5488 mL 1.0977 mL 2.7442 mL
30 mM 0.0915 mL 0.4574 mL 0.9147 mL 2.2869 mL
40 mM 0.0686 mL 0.3430 mL 0.6861 mL 1.7151 mL
50 mM 0.0549 mL 0.2744 mL 0.5488 mL 1.3721 mL
60 mM 0.0457 mL 0.2287 mL 0.4574 mL 1.1434 mL
80 mM 0.0343 mL 0.1715 mL 0.3430 mL 0.8576 mL
100 mM 0.0274 mL 0.1372 mL 0.2744 mL 0.6861 mL
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CDPPB 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:

CDPPB781652-57-1mGluRAktERKCaspaseMitochondrial MetabolismMetabotropic glutamate receptorsPKBProtein kinase BExtracellular signal regulated kinasespositiveallostericmetabotropicglutamatereceptorsubtype5mGluR5antipsychoticInhibitorinhibitorinhibit

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Cat. No.:
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