DPCPX (Synonyms: PD 116948)

Name: DPCPX
Brand: MedChemExpress
SKU: HY-100937
Rating: 5.0 (9 reviews)

Cat. No.: HY-100937 Purity: 99.96%: Data Sheet
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DPCPX (PD 116948), a xanthine derivative, is a highly potent and selective Adenosine A1 receptor antagonist, with a K_i of 0.46 nM in ³H-CHA binding to A1 receptors in rat whole brain membranes.

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

CAS No. : 102146-07-6

Size	Stock	Quantity

Free Sample (0.1 - 0.2 mg)	Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 9 publication(s) in Google Scholar

Other Forms of DPCPX:

DPCPX-d₄ Get quote
DPCPX (Standard) Get quote

9 Publications Citing Use of MCE DPCPX

In Vivo Efficacy Study

Bio/Physico-chemical Assay

: DPCPX purchased from MedChemExpress. Usage Cited in: Mol Psychiatry. 2024 May 13. [Abstract]; DPCPX (4 mg/kg; i.g.; 14 d) blocked the 40 Hz light flicker's prosocial effect on social novelty preference in mice with 16p11.2 deletion.

: DPCPX purchased from MedChemExpress. Usage Cited in: Mol Psychiatry. 2024 May 13. [Abstract]; The A1R antagonist DPCPX (0.3 µM) significantly elevated the sEPSC frequency in mice with 16p11.2 deletion.

: DPCPX purchased from MedChemExpress. Usage Cited in: Mol Psychiatry. 2024 May 13. [Abstract]; DPCPX (0.3 µM), the A1R antagonist, blocked the reduction in sEPSC frequency induced by in-vitro application of adenosine in 16p11.2 deletion female mice.

: DPCPX purchased from MedChemExpress. Usage Cited in: Mol Psychiatry. 2024 May 13. [Abstract]; DPCPX (4 mg/kg; i.g.; 14 d) blocked the 40 Hz light flicker's effect on excitatory synapses with increasing VGLUT1⁺ boutons surrounding neurons in mice with 16p11.2 deletion.

: DPCPX purchased from MedChemExpress. Usage Cited in: Mol Psychiatry. 2024 May 13. [Abstract]; DPCPX (0.3 µM) blocked the 40 Hz light flicker's effect on sEPSCs, with significantly increased sEPSC frequency and amplitude.

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View All Adenosine Receptor Isoform Specific Products:

View All Isoforms

Adenosine A₁ receptor (A₁R) Adenosine A_2A receptor (A_2AR) Adenosine A_2B receptor (A_2BR) Adenosine A₃ receptor (A₃R)

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

Ki: 0.46 nM (³H-CHA binding to A1 receptors in rat whole brain membranes); 340 nM (³H-NECA binding to A2 receptors in rat striatal membranes)^[2].

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	1.52 nM Compound: DPCPX	Inverse agonist activity at human A1AR expressed in CHO cells assessed as increase in forskolin-stimulated cAMP production by alphascreen assay Inverse agonist activity at human A1AR expressed in CHO cells assessed as increase in forskolin-stimulated cAMP production by alphascreen assay	[PMID: 31306001]
CHO	EC₅₀	> 1000 nM Compound: DPCPX	Agonist activity at human A2B expressed in CHO cells assessed as stimulation of cAMP production by alphascreen assay Agonist activity at human A2B expressed in CHO cells assessed as stimulation of cAMP production by alphascreen assay	[PMID: 31306001]
CHO	IC₅₀	132 nM Compound: DPCPX	Antagonist activity at human A2AR expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP production by alphascreen assay Antagonist activity at human A2AR expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP production by alphascreen assay	[PMID: 31306001]
CHO	IC₅₀	43 nM Compound: DPCPX	Antagonist activity at human A2BR expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production by alphascreen assay Antagonist activity at human A2BR expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production by alphascreen assay	[PMID: 31306001]
CHO	IC₅₀	5 x 10^-10 M Compound: DPCPX	Displacement of [3H]DPCPX from human recombinant adenosine A1 receptor expressed in CHO cells Displacement of [3H]DPCPX from human recombinant adenosine A1 receptor expressed in CHO cells	[PMID: 26988801]
CHO	IC₅₀	5 x 10^-10 M Compound: DPCPX	Displacement of [3H]DPCPX from human recombinant adenosine receptor A1 expressed in CHO cells measured after 60 mins by scintillation counting method Displacement of [3H]DPCPX from human recombinant adenosine receptor A1 expressed in CHO cells measured after 60 mins by scintillation counting method	[PMID: 27876250]
HCT-116	IC₅₀	> 10 μM Compound: DPCPX	Cytotoxicity against human HCT-116 cells assessed as cell viability incubated for 72 to 96 hrs by MTT assay Cytotoxicity against human HCT-116 cells assessed as cell viability incubated for 72 to 96 hrs by MTT assay	[PMID: 35707146]
HEK293	IC₅₀	261 nM Compound: DPCPX	Inhibitory activity against membranes from HEK293 cells stably expressing the human A2a receptor (hA2a) Inhibitory activity against membranes from HEK293 cells stably expressing the human A2a receptor (hA2a)	[PMID: 10476879]
Huh-7	CC₅₀	> 8.26 μM Compound: GNF-Pf-2224	NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7) NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)	[PMID: 18579783]
PC-3	IC₅₀	> 10 μM Compound: DPCPX	Cytotoxicity against human PC-3 cells assessed as cell viability incubated for 72 to 96 hrs by MTT assay Cytotoxicity against human PC-3 cells assessed as cell viability incubated for 72 to 96 hrs by MTT assay	[PMID: 35707146]
ScN2a	EC₅₀	> 25 μM Compound: DPCPX	Reduction of PrPSC accumulation in ScN2a cells Reduction of PrPSC accumulation in ScN2a cells	[PMID: 17201410]
WI-38	IC₅₀	> 10 μM Compound: DPCPX	Cytotoxicity against human WI-38 cells assessed as cell viability incubated for 72 to 96 hrs by MTT assay Cytotoxicity against human WI-38 cells assessed as cell viability incubated for 72 to 96 hrs by MTT assay	[PMID: 35707146]

In Vivo

DPCPX (PD 116948) ( 0.1, 0.3 and 1.0 mg/kg i.v. ) produces significant dose-related increases (P<0.05) in urine volume and in urinary sodium, potassium and chloride excretion^[3].

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

Molecular Weight

304.39

Formula

C₁₆H₂₄N₄O₂

CAS No.

102146-07-6

Appearance

Solid

Color

White to off-white

SMILES

O=C(N1CCC)N(CCC)C2=C(N=C(C3CCCC3)N2)C1=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 : 10 mg/mL (32.85 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	3.2853 mL	16.4263 mL	32.8526 mL
5 mM	0.6571 mL	3.2853 mL	6.5705 mL
10 mM	0.3285 mL	1.6426 mL	3.2853 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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: ≥ 1 mg/mL (3.29 mM); Clear solution

This protocol yields a clear solution of ≥ 1 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 (10.0 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: 15% Cremophor EL 85% Saline
Solubility: 20 mg/mL (65.71 mM); Suspended solution; Need ultrasonic

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: 99.96%

Select Batch:

Data Sheet (274 KB) SDS (396 KB)

COA (247 KB) HNMR (241 KB) LCMS (97 KB)

Handling Instructions (2659 KB)

References

[1]. S J Haleen, et al. PD 116,948, a Highly Selective A1 Adenosine Receptor Antagonist. Life Sci. 1987 Feb 9;40(6):555-61. [Content Brief]

[2]. R F Bruns, et al. Binding of the A1-selective Adenosine Antagonist 8-cyclopentyl-1,3-dipropylxanthine to Rat Brain Membranes. Naunyn Schmiedebergs Arch Pharmacol. 1987 Jan;335(1):59-63. [Content Brief]

[3]. POSTER COMMUNICATIONS Part II. Br J Pharmacol. 1989 Jul; 97(Suppl): 496P–535P.

Animal Administration

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

References

[1]. S J Haleen, et al. PD 116,948, a Highly Selective A1 Adenosine Receptor Antagonist. Life Sci. 1987 Feb 9;40(6):555-61. [Content Brief]

[2]. R F Bruns, et al. Binding of the A1-selective Adenosine Antagonist 8-cyclopentyl-1,3-dipropylxanthine to Rat Brain Membranes. Naunyn Schmiedebergs Arch Pharmacol. 1987 Jan;335(1):59-63. [Content Brief]

[3]. POSTER COMMUNICATIONS Part II. Br J Pharmacol. 1989 Jul; 97(Suppl): 496P–535P.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.2853 mL	16.4263 mL	32.8526 mL	82.1315 mL
	5 mM	0.6571 mL	3.2853 mL	6.5705 mL	16.4263 mL
	10 mM	0.3285 mL	1.6426 mL	3.2853 mL	8.2131 mL
	15 mM	0.2190 mL	1.0951 mL	2.1902 mL	5.4754 mL
	20 mM	0.1643 mL	0.8213 mL	1.6426 mL	4.1066 mL
	25 mM	0.1314 mL	0.6571 mL	1.3141 mL	3.2853 mL
	30 mM	0.1095 mL	0.5475 mL	1.0951 mL	2.7377 mL

DPCPX Related Classifications

Cardiovascular 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:

DPCPX102146-07-6PD 116948PD116948PD-116948Adenosine ReceptorP1 receptorInhibitorinhibitorinhibit

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DPCPX (Synonyms: PD 116948)

Customer Review

Other Forms of DPCPX:

DPCPX Related Antibodies

9 Publications Citing Use of MCE DPCPX

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Adenosine Receptor Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

DPCPX Related Classifications

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