製品番号: HY-14569

CDPPB

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

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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純度: 98.01%
CAS 番号: 781652-57-1
分子式: C₂₃H₁₆N₄O
分子量:364.40

保管条件:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

CDPPB 構造式

CAS 番号: 781652-57-1

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数量

Amount: USD 0.00

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
化学情報
Publications (1)
溶剤 & 溶解度
- 体外
- 体内
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target^[1]

mGluR5

27 nM (EC₅₀)

mGluR アイソフォーム固有の製品をすべて表示 :

Akt アイソフォーム固有の製品をすべて表示 :

ERK アイソフォーム固有の製品をすべて表示 :

Caspase アイソフォーム固有の製品をすべて表示 :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	10 nM 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 nM 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 nM 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 nM 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]

体外実験

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.

体内実験

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.

化学情報

CAS 番号 781652-57-1
性状 Solid
分子量 364.40
分子式 C₂₃H₁₆N₄O
Color White to off-white
SMILES

O=C(NC1=CC(C2=CC=CC=C2)=NN1C3=CC=CC=C3)C4=CC=CC(C#N)=C4
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (1)

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Psychopharmacology (Berl)

The role of mGluR5 on the therapeutic effects of ketamine in Wistar rats. [Abstract]

2024 Jul;241(7):1399-1415. PMID: 38459971

溶剤 & 溶解度

体外:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.7442 mL

13.7212 mL

27.4424 mL

5 mM

0.5488 mL

2.7442 mL

5.4885 mL

10 mM

0.2744 mL

1.3721 mL

2.7442 mL

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.

モル濃度計算機

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

Mass Mass

濃度濃度

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分子量分子量

希釈計算機

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体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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:

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Animal Weight (Per Animal) Animal Weight (Per Animal)
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%
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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).

Working solution concentration: 0.22 mg/mL

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

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COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
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OR (2659 KB)
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取扱説明書 (2659 KB)

参考文献

[1]. Kinney GG, et, al. A novel selective positive allosteric modulator of metabotropic glutamate receptor subtype 5 has in vivo activity and antipsychotic-like effects in rat behavioral models. J Pharmacol Exp Ther. 2005 Apr; 313(1):199-206. [Content Brief]

[2]. Guan DF, et al. The mGluR5 positive allosteric modulator CDPPB inhibits SO₂-induced protein radical formation and mitochondrial dysfunction through activation of Akt in mouse hippocampal HT22 cells. Cell Mol Neurobiol. 2015 May;35(4):573-83. [Content Brief]

[3]. Chen T, et al. Protective effects of mGluR5 positive modulators against traumatic neuronal injury through PKC-dependent activation of MEK/ERK pathway. Neurochem Res. 2012 May;37(5):983-90. [Content Brief]

[4]. Horio M, et al. Therapeutic effects of metabotropic glutamate receptor 5 positive allosteric modulator CDPPB on phencyclidine-induced cognitive deficits in mice. Fundam Clin Pharmacol. 2013 Oct;27(5):483-8.

[5]. Płoska A, et al. Neurochemical changes underlying cognitive impairment in olfactory bulbectomized rats and the impact of the mGlu5-positive allosteric modulator CDPPB. Brain Res. 2021 Oct 1;1768:147577. [Content Brief]

[6]. Doria JG, et al. The mGluR5 positive allosteric modulator, CDPPB, ameliorates pathology and phenotypic signs of a mouse model of Huntington's disease. Neurobiol Dis. 2015 Jan;73:163-73. [Content Brief]

[7]. Zhang L, et al. Post-stress Social Interaction and 3-Cyano-N-(1,3-Diphenyl-1H-Pyrazol-5-yl) Benzamide Treatment Attenuate Depressive-like Behavior Induced by Repeated Social Defeat Stress. Neuroscience. 2024 Feb 6;538:11-21. [Content Brief]

[8]. Miller-Rhodes P, et al. Sex-specific behavioral impairments produced by neonatal exposure to MK-801 are partially reversed by adolescent CDPPB treatment. Neurotoxicology and Teratology, 2022, 89: 107053.

[9]. Bellozi PMQ, et al. A positive allosteric modulator of mGluR5 promotes neuroprotective effects in mouse models of Alzheimer's disease. Neuropharmacology. 2019 Dec 1;160:107785. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

CDPPB

1 Cited Publications

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MedChemExpress（MCE）の使用を引用している文献 CDPPB

mGluR アイソフォーム固有の製品をすべて表示

Akt アイソフォーム固有の製品をすべて表示

ERK アイソフォーム固有の製品をすべて表示

Caspase アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (1)

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

CDPPB 関連分類

HY-14569 関連分類