Cat. No.: HY-103406

PNU-177864

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PNU-177864 is a potent, selective, orally active dopamine D₃ receptor antagonist. PNU-177864 induces phospholipid metabolism in vivo and has anti-schizophrenia activity.

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

CAS No.: 250266-51-4
Formula: C₁₈H₂₁F₃N₂O₃S
Molecular Weight:402.43

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Data Sheet (277 KB)

PNU-177864 Chemical Structure

CAS No.: 250266-51-4

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Price

Stock

Quantity

Sample (0.1mg)

In-stock

(In Japan)

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

PNU-177864 is a potent, selective, orally active dopamine D₃ receptor antagonist. PNU-177864 induces phospholipid metabolism in vivo and has anti-schizophrenia activity^[1]^[2]^[3].

IC₅₀ & Target

CCR5

All Dopamine Receptor Isoforms :

All CCR Isoforms :

In Vitro

PNU-177864 (1-10 μM, 30 min) reduces CCR5 expression in THP1, reduces inflammation^[1].

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

In Vivo

PNU-177864 (0-200 mg/kg,p.o., once daily for 2 weeks) can cause significant phospholipidosis and associated myopathy under certain conditions in rats, with plasma levels increasing throughout 24 hours at high doses. It remains high and almost unchanged over the dosing interval, but it has no obvious toxicity at lower doses^[2].
PNU-177864 (0-200 mg/kg, p.o., once daily for 2 weeks) in rats and dogs is the accumulation of phospholipids in epididymal epithelial cells^[3].
Pharmacokinetic analysis of oral PNU-177864 in rats^[2]

Treatment (mg/kg/day)	Day	C_max (μg/mL)	T_max (h)	C₂₄ (μg/mL)	t_1/2 (h)	AUC_0-24 (μg•h/mL)	AUC_0-∞ (ng•h/mL)
12.5	1	0.88	4-8	0.167	6.5	13.2	15.1
12.5	6	nc	nc	0.23	nc	nc	nc
12.5	14	1.25	2-8	0.237	7.1	18.4	nc
50	1	3.64	8	1.84	16	63.9	117
50	6	nc	nc	2.74	nc	nc	nc
50	14	5.7	4-8	2.50	13.7	104	nc
200	1	6.9	8-24	6.8	/	133	nc
200	6	nc	nc	14.3	nc	nc	nc
200	11	15.9	0-8	11.06	/	306	nc

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

Animal Model:

Male and female Sprague-Dawley rats (8-9-week-old)^[1]
Dosage:

12.5 mg/kg, 50 mg/kg (for 2 weeks), or 200 mg/kg; 8 mg/kg, 25 mg/kg, or 80 mg/kg (for 4 weeks)
Administration:

Oral gavage; daily; for 2-4 weeks
Result:

Induced phospholipidosis in unusual target organs in dogs or rats including epididymis, pituitary, and hair follicles.

Animal Model:

Male and Female Sprague–Dawley rats^[2]^[3]
Dosage:

0, 12.5, 50, 200 mg/kg/day, 2 weeks; 0, 8, 25, 80 mg/kg/day, 4 weeks; 0, 200 mg/kg/day, 9 days
Administration:

Oral
Result:

Showed lymphoid tissue (lymph nodes, foamy macrophages in the white medulla of the spleen or Peyer's patches), alveolar macrophages, epididymal epithelial cells, peripheral blood lymphocytes, lymphocytes and plasma cells all show changes consistent with phospholipidosis.
Showed morphological changes in the affected tissues show obvious, clear vacuoles or foamy appearance in the cytoplasm of plasma cells, lymphocytes or epithelial cells and macrophages. After the recovery period, no histological and electron microscopic signs of phospholipidosis were found except in the epididymis.
Showed multifocal to extensive myocyte degeneration in skeletal muscle, with accumulation of phospholipids observed under light microscopy.

Animal Model:

9–10-month-old beagle dogs^[3]
Dosage:

0, 2, 10, 50 mg/kg/day, 2 weeks; 0, 0.5, 4, 32 mg/kg/day, 4 weeks
Administration:

Oral
Result:

Showed lymphoid tissue (lymph nodes, foamy macrophages in the white medulla of the spleen or Peyer's patches), alveolar macrophages, epididymal epithelial cells, and peripheral blood lymphocytes showed changes consistent with phospholipidosis. After the recovery period, no histological and electron microscopic signs of phospholipidosis were found except in the epididymis.
Showed no histological changes were found in the epididymal epithelial cells; sperm density and morphology were normal histologically; the dogs had normal sperm concentration, morphology, and motility.

Chemical Information

CAS No. 250266-51-4
Appearance Solid
Molecular Weight 402.43
Formula C₁₈H₂₁F₃N₂O₃S
Color White to off-white
SMILES

O=S(C1=CC=C(OC(F)(F)F)C=C1)(NC2=CC=C(CCNCCC)C=C2)=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 : 57.14 mg/mL (141.99 mM; adjust pH to 5 with HCl; 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

2.4849 mL

12.4245 mL

24.8490 mL

5 mM

0.4970 mL

2.4849 mL

4.9698 mL

10 mM

0.2485 mL

1.2425 mL

2.4849 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, 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

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 5 mg/mL (12.42 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 5 mg/mL (12.42 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Liana Basova , et al. Dopamine and its receptors play a role in the modulation of CCR5 expression in innate immune cells following exposure to Methamphetamine: Implications to HIV infection. PLoS One.2018 Jun 26;13(6):e0199861. [Content Brief]

[2]. Vonderfecht SL, et al. Myopathy related to administration of a cationic amphiphilic drug and the use of multidose drug distribution analysis to predict its occurrence. Toxicol Pathol. 2004 May-Jun;32(3):318-25. [Content Brief]

[3]. Rudmann DG, et al. Epididymal and systemic phospholipidosis in rats and dogs treated with the dopamine D3 selective antagonist PNU-177864. Toxicol Pathol. 2004 May-Jun;32(3):326-32. [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, 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.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.4849 mL	12.4245 mL	24.8490 mL	62.1226 mL
	5 mM	0.4970 mL	2.4849 mL	4.9698 mL	12.4245 mL
	10 mM	0.2485 mL	1.2425 mL	2.4849 mL	6.2123 mL
	15 mM	0.1657 mL	0.8283 mL	1.6566 mL	4.1415 mL
	20 mM	0.1242 mL	0.6212 mL	1.2425 mL	3.1061 mL
	25 mM	0.0994 mL	0.4970 mL	0.9940 mL	2.4849 mL
	30 mM	0.0828 mL	0.4142 mL	0.8283 mL	2.0708 mL
	40 mM	0.0621 mL	0.3106 mL	0.6212 mL	1.5531 mL
	50 mM	0.0497 mL	0.2485 mL	0.4970 mL	1.2425 mL
	60 mM	0.0414 mL	0.2071 mL	0.4142 mL	1.0354 mL
	80 mM	0.0311 mL	0.1553 mL	0.3106 mL	0.7765 mL
	100 mM	0.0248 mL	0.1242 mL	0.2485 mL	0.6212 mL

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PNU-177864

MCE Bioactive Compound Library

All Dopamine Receptor Isoforms

All CCR Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

PNU-177864 Related Classifications

Cat. No.: HY-103406