| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| Targets |
PD 160170 is a potent and selective non-peptide antagonist of the neuropeptide Y1 receptor (NPY1-R). It exhibits high affinity binding to the NPY1 receptor with a Ki value of 48 nM. The compound shows remarkable selectivity over other NPY receptor subtypes, with Ki values greater than 10 μM for both Y2 and Y5 receptors, indicating more than 200-fold selectivity for Y1 over Y2/Y5. This selectivity profile makes PD 160170 a valuable tool for dissecting NPY1-R-mediated physiological functions from those mediated by other NPY receptor subtypes.
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| ln Vitro |
In vitro studies have characterized PD 160170 as a potent NPY1 receptor antagonist. The compound effectively blocks NPY-induced calcium mobilization and other downstream signaling events in cells expressing recombinant NPY1 receptors. Its antagonistic activity is mediated through competitive binding at the receptor orthosteric site. PD 160170 demonstrates functional antagonism in various cell-based assay systems, inhibiting NPY-mediated responses with potency consistent with its receptor binding affinity. The compound's activity has been validated in multiple in vitro pharmacological assays for NPY1 receptor antagonism.
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| ln Vivo |
In vivo pharmacological data for PD 160170 are limited as the compound is primarily a research tool. As a potent NPY1 receptor antagonist with favorable selectivity, it is expected to modulate NPY1-mediated physiological responses in animal models. NPY1 receptor antagonism in vivo is associated with effects on feeding behavior, anxiety-like behaviors, and cardiovascular parameters. PD 160170 may be used in preclinical studies to investigate the therapeutic potential of NPY1 receptor blockade in conditions such as obesity, anxiety disorders, and hypertension.
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| Enzyme Assay |
NPY1 receptor binding assays are typically performed using membrane preparations from cells expressing recombinant human NPY1 receptors. Radioligand binding studies utilize [125I]-labeled peptide YY (PYY) or NPY as the tracer. Membranes are incubated with varying concentrations of PD 160170 and a fixed concentration of radioligand in binding buffer (e.g., 50 mM HEPES, pH 7.4, containing 5 mM MgCl2, 1 mM CaCl2, and 0.1% BSA) for 60-120 minutes at room temperature. Non-specific binding is determined in the presence of 1 μM unlabeled NPY. Bound radioligand is separated by rapid filtration through glass fiber filters and counted by scintillation spectroscopy. Ki values are calculated from IC50 values using the Cheng-Prusoff equation.
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| Cell Assay |
Cellular assays for NPY1 receptor antagonism typically employ cell lines stably or transiently expressing recombinant human NPY1 receptors, such as CHO or HEK-293 cells. Cells are seeded in 96-well or 384-well plates and loaded with a calcium-sensitive fluorescent dye (e.g., Fluo-4 AM). After dye loading and washing, cells are pre-incubated with varying concentrations of PD 160170 for 10-30 minutes, followed by stimulation with an EC80 concentration of NPY or PYY. The increase in intracellular calcium concentration is measured using a fluorescence plate reader. Antagonist potency is determined by measuring the rightward shift of the agonist concentration-response curve or by calculating the percentage inhibition of the agonist response at a fixed agonist concentration.
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| Animal Protocol |
In vivo pharmacological characterization of NPY1 receptor antagonists typically involves rodent models. For studying feeding behavior, compounds are administered via intraperitoneal, subcutaneous, or oral routes to fasted animals, followed by measurement of food intake over several hours. For anxiety-related studies, compounds are tested in established behavioral paradigms such as the elevated plus maze or open field test. Cardiovascular effects can be assessed in anesthetized or conscious animals via telemetry. PD 160170, as a research compound, would be administered at doses determined from pharmacokinetic and tolerability studies, typically ranging from 0.1 to 10 mg/kg depending on the route of administration and the specific model used.
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| ADME/Pharmacokinetics |
Published pharmacokinetic data for PD 160170 are limited. As a small molecule with a molecular weight of 371.41 g/mol and moderate lipophilicity (LogP ~5.87), the compound is expected to have reasonable membrane permeability. It is soluble in DMSO and may be formulated for in vivo administration using appropriate vehicles. The compound is stable in powder form at -20°C for up to 3 years and in solution at -80°C for 6 months. For in vivo studies, typical formulations may include DMSO/PEG400/saline mixtures or other suitable vehicles to achieve desired exposure levels.
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| Toxicity/Toxicokinetics |
Toxicological data for PD 160170 are not extensively published in the open literature. As a research compound not approved for human use, standard preclinical toxicity assessments would be required prior to any clinical development. Based on its chemical structure as a nitro-containing quinoline derivative, potential toxicological concerns may include mutagenicity and general cytotoxicity, which would need to be evaluated through appropriate in vitro and in vivo genotoxicity and safety pharmacology studies. The compound should be handled with appropriate laboratory safety precautions.
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| Additional Infomation |
5-Nitro-6-(2-Prop-2-ylphenyl)sulfonyl-8-quinolinamine is a nitro compound belonging to the quinoline class of compounds.
PD 160170 is also known by synonyms including PD-160170, NCGC00092332-01, and BRD-K12079898-001-01-8. Its chemical name is 5-nitro-6-(2-propan-2-ylphenyl)sulfonylquinolin-8-amine with molecular formula C18H17N3O4S and molecular weight 371.41. NPY1 receptors are involved in the regulation of appetite, anxiety, stress responses, and cardiovascular function. PD 160170's high selectivity for NPY1 over Y2 and Y5 receptors makes it a useful tool for distinguishing Y1-mediated effects from those of other NPY receptor subtypes. |
| Molecular Formula |
C18H17N3O4S
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| Molecular Weight |
371.41
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| Exact Mass |
371.094
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| CAS # |
181468-88-2
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| PubChem CID |
9820766
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.379g/cm3
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| Boiling Point |
646.6ºC at 760mmHg
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| Flash Point |
344.8ºC
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| Vapour Pressure |
0mmHg at 25°C
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| Index of Refraction |
1.658
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| LogP |
5.866
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
26
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| Complexity |
613
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(C1=CC=CC=C1S(C1C=C(N)C2=NC=CC=C2C=1[N+]([O-])=O)(=O)=O)C
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| InChi Key |
YUVNGBZROXQYQH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H17N3O4S/c1-11(2)12-6-3-4-8-15(12)26(24,25)16-10-14(19)17-13(7-5-9-20-17)18(16)21(22)23/h3-11H,19H2,1-2H3
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| Chemical Name |
5-nitro-6-(2-propan-2-ylphenyl)sulfonylquinolin-8-amine
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| Synonyms |
PD160170PD-160170PD 160170
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6924 mL | 13.4622 mL | 26.9244 mL | |
| 5 mM | 0.5385 mL | 2.6924 mL | 5.3849 mL | |
| 10 mM | 0.2692 mL | 1.3462 mL | 2.6924 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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