2. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  3. Dopamine Receptor CCR
  4. PNU-177864

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

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PNU-177864 Chemical Structure

PNU-177864 Chemical Structure

CAS No. : 250266-51-4

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1 mg USD 98 In-stock
5 mg USD 200 In-stock
10 mg USD 290 In-stock
25 mg USD 590 In-stock
50 mg USD 830 In-stock
100 mg USD 1150 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of PNU-177864:

PNU-177864 Related Antibodies

Top Publications Citing Use of Products

View All Dopamine Receptor Isoform Specific Products:

View All Isoforms
Dopamine Receptor D1 Receptor D2 Receptor D3 Receptor D4 Receptor D5 Receptor

View All CCR Isoform Specific Products:

View All Isoforms
CCR1 CCR2 CCR3 CCR4 CCR5 CCR6 CCR7 CCR8 CCR9

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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

 

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.

PNU-177864 Related Antibodies
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 Cmax (μg/mL) Tmax (h) C24 (μg/mL) t1/2 (h) AUC0-24 (μg•h/mL) AUC0-∞ (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.
Molecular Weight

402.43

Formula

C18H21F3N2O3S
CAS No.
Appearance

Solid

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4849 mL 12.4245 mL 24.8490 mL
5 mM 0.4970 mL 2.4849 mL 4.9698 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)

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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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    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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Purity & Documentation
References

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.

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 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:

PNU-177864250266-51-4PNU177864PNU 177864Dopamine ReceptorCCRCC chemokine receptorD3-receptorcationicamphiphilicphospholipidosisCADantischizophrenicmyopathyInhibitorinhibitorinhibit

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