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NPFF1-R antagonist 1 (compound 8b) is a piperidine analog and an effective neuropeptide FF (NPFF) receptor antagonist. It exhibits 15-fold selectivity 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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| 50 mg | Inquiry | Inquiry | Inquiry |
| Description | NPFF1-R antagonist 1 (compound 8b) is a piperidine analog and an effective neuropeptide FF (NPFF) receptor antagonist. It exhibits 15-fold selectivity for the NPFF1-R subtype, with Ki values of 211 nM and 3270 nM for NPFF1-R and NPFF2-R, respectively. |
| Targets&IC50 | κ opioid receptor:1390 ± 147 nM (Ki), NPFF1R:211 ± 54 nM (Ki), NPFF2R:3270 ±639 nM (Ki), δ opioid receptor:1540 ± 132 nM (Ki), μ opioid receptor:3560 ± 364 nM (Ki) |
| In vitro | NPFF1-R antagonist 1 (compound 8b) exhibits off-target binding at the opioid receptors (DOR, KOR, and MOR), with K i values of 1540 ± 132, 1390 ± 147, and 3560 ± 364 nM, respectively. At concentrations of 0-10 μM, NPFF1-R antagonist 1 does not inhibit cAMP stimulation but dose-dependently reverses the NPFF-induced inhibition of forskolin-induced cAMP accumulation. |
| Formula | C37H44N4O |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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