2. GPCR/G Protein Neuronal Signaling
  3. Neuropeptide FF Receptor Opioid Receptor
  4. NPFF1-R antagonist 1

NPFF1-R antagonist 1 (compound 8b), a piperidine analogue, is a potent neuropeptide FF (NPFF) receptor antagonist. NPFF1-R antagonist 1 is 15-fold selective for the NPFF1-R subtype, with Ki values of 211 nM and 3270 nM for NPFF1-R and NPFF2-R, respectively.

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NPFF1-R antagonist 1

NPFF1-R antagonist 1 Chemical Structure

CAS No. : 3057753-40-6

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Based on 1 publication(s) in Google Scholar

NPFF1-R antagonist 1 Related Antibodies

Top Publications Citing Use of Products

View All Neuropeptide FF Receptor Isoform Specific Products:

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NPFFR1 NPFFR2

View All Opioid Receptor Isoform Specific Products:

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μ Opioid Receptor/MOR κ Opioid Receptor/KOR δ Opioid Receptor/DOR NOP Receptor/ORL1

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Description

NPFF1-R antagonist 1 (compound 8b), a piperidine analogue, is a potent neuropeptide FF (NPFF) receptor antagonist. NPFF1-R antagonist 1 is 15-fold selective for the NPFF1-R subtype, with Ki values of 211 nM and 3270 nM for NPFF1-R and NPFF2-R, respectively[1].

IC50 & Target

NPFF1-R

211 ± 54 nM (Ki)

NPFF2-R

3270 ±639 nM (Ki)

κ Opioid Receptor/KOR

1390 ± 147 nM (Ki)

δ Opioid Receptor/DOR

1540 ± 132 nM (Ki)

μ Opioid Receptor/MOR

3560 ± 364 nM (Ki)

In Vitro

NPFF1-R antagonist 1 (compound 8b) shows some off target binding at the opioid receptors (DOR, KOR, and MOR), with Ki values of 1540 ± 132, 1390 ± 147, and 3560 ± 364 nM, respectively[1].
NPFF1-R antagonist 1 (0-10 μM) fails to inhibit cAMP stimulation, dose-dependently reverses NPFF inhibition of forskolin (HY-15371)-induced cAMP accumulation[1].

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

NPFF1-R antagonist 1 Related Antibodies
Molecular Weight

560.77

Formula

C37H44N4O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(CN1CCC(CC2=CC=CC=C2)CC1)NCC3(CCN(CC4=CC=CC=C4)CC3)NC5=C(C=CC=C6)C6=CC=C5
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 4.29 mg/mL (7.65 mM; ultrasonic and warming and heat to 60°C; 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 1.7833 mL 8.9163 mL 17.8326 mL
5 mM 0.3567 mL 1.7833 mL 3.5665 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 (sealed storage, away from moisture and light). 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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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 (sealed storage, away from moisture and light). 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 1.7833 mL 8.9163 mL 17.8326 mL 44.5816 mL
5 mM 0.3567 mL 1.7833 mL 3.5665 mL 8.9163 mL
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NPFF1-R antagonist 1 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:

NPFF1-R antagonist 13057753-40-6Neuropeptide FF ReceptorOpioid ReceptorCHO cellsNPFFcAMPInhibitorinhibitorinhibit

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