2. GPCR/G Protein
  3. Bombesin Receptor
  4. PD 168368

PD 168368 is a potent, competitive, and selective neuromedin B receptor (NMB-R) antagonist with the Ki of 15–45 nM. PD 168368 is neuromedin B receptor (NMBR; IC50=96 nM) / gastrin-releasing peptide receptor (GRPR IC50=3500 nM) antagonist. PD 168368 also is a mixed FPR1/FPR2/FPR3 agonist with EC50s of 0.57, 0.24, and 2.7 nM, respectively.

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PD 168368 Chemical Structure

PD 168368 Chemical Structure

CAS No. : 204066-82-0

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5 mg USD 300 In-stock
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Based on 1 publication(s) in Google Scholar

PD 168368 Related Antibodies

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  • Purity & Documentation

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Description

PD 168368 is a potent, competitive, and selective neuromedin B receptor (NMB-R) antagonist with the Ki of 15–45 nM[1]. PD 168368 is neuromedin B receptor (NMBR; IC50=96 nM) / gastrin-releasing peptide receptor (GRPR IC50=3500 nM) antagonist[2]. PD 168368 also is a mixed FPR1/FPR2/FPR3 agonist with EC50s of 0.57, 0.24, and 2.7 nM, respectively[3].

In Vitro

PD 168368 (PD168368) is highly active and stimulated [Ca2+]I release in human neutrophils with EC50 values in the nanomolar range[3].
PD 168368 (PD168368) suppresses migration and invasion of the human breast cancer cell line MDA-MB-231. PD 168368 reduces epithelial-mesenchymal transition (EMT) of breast cancer cells by E-cadherin upregulation and vimentin downregulation. PD 168368 (5 μM) inhibits migration and invasiveness in breast cancer cells[4].
PD 168368 (10 μM) suppresses the activation of mTOR/p70S6K/4EBP1 and AKT/GSK-3β pathways in breast cancer cells[4].

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

PD 168368 Related Antibodies

Cell Viability Assay[4]

Cell Line: Human breast cancer cell line MDA-MB-231
Concentration: 5 μM
Incubation Time: 24 hours
Result: Clearly decreased the migratory ability of MDA-MB-231 cells in a Boyden chamber migration assay.

Cell Viability Assay[4]

Cell Line: MDA-MB-231 cells
Concentration: 10 μM
Incubation Time: 0, 0.5, 1, 2, 4, 8, and 16 hours
Result: Decreased phosphorylation levels of mTOR, p70S6K, 4EBP1, AKT and GSK-3β in a time-dependent manner.
In Vivo

PD 168368 (PD168368) potently inhibits in vivo metastasis of breast cancer. PD 168368 (1.2 mg/kg; intraperitoneal injection for 30 days) inhibits metastasis of breast cancer in mice[4].

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

Animal Model: Female BALB/c-nude mice (age 8-10 weeks) bearing MDA-MB-231 xenograft model[4]
Dosage: 1.2 mg/kg
Administration: Intraperitoneal injection for 30 days
Result: No metastatic tumor nodules were observed in lungs of PD 168368-treated mice compared to PEG-injected mice.
Molecular Weight

554.64

Formula

C31H34N6O4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C([C@](C)(CC1=CNC2=C1C=CC=C2)NC(NC3=CC=C(C=C3)[N+]([O-])=O)=O)NCC4(CCCCC4)C5=NC=CC=C5
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 30 mg/mL (54.09 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

DMF : 10 mg/mL (18.03 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8030 mL 9.0149 mL 18.0297 mL
5 mM 0.3606 mL 1.8030 mL 3.6059 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.

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: ≥99.0%

COA (256 KB)

Handling Instructions (2659 KB)
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
DMF / DMSO 1 mM 1.8030 mL 9.0149 mL 18.0297 mL 45.0743 mL
5 mM 0.3606 mL 1.8030 mL 3.6059 mL 9.0149 mL
10 mM 0.1803 mL 0.9015 mL 1.8030 mL 4.5074 mL
15 mM 0.1202 mL 0.6010 mL 1.2020 mL 3.0050 mL
DMSO 20 mM 0.0901 mL 0.4507 mL 0.9015 mL 2.2537 mL
25 mM 0.0721 mL 0.3606 mL 0.7212 mL 1.8030 mL
30 mM 0.0601 mL 0.3005 mL 0.6010 mL 1.5025 mL
40 mM 0.0451 mL 0.2254 mL 0.4507 mL 1.1269 mL
50 mM 0.0361 mL 0.1803 mL 0.3606 mL 0.9015 mL
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PD 168368 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:

PD 168368204066-82-0PD168368PD-168368Bombesin ReceptorNMBNMBRGRPRgastrinreleasingpeptideneuromedin BBB1BB2FPR1FPR2FPR3Inhibitorinhibitorinhibit

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