AC-263093
AC-263093 (AC-093 hydrochloride) is a NPFFR2 agonist and a NPFFR1 functional antagonist, with pKi values of 6.9 and 7.0, respectively. AC-263093 selectively activates NPFFR2 (and inhibits NPFFR1) coupled to Gai/o proteins, thereby inhibiting adenylyl cyclase to reduce cAMP production. AC-263093 can be used for research on depression and anxiety-like disorders, inflammatory and neuropathic pain, and opioid tolerance.
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- CAS No.: 849335-02-0
- Formule: C8H9Br2ClN4
- Masse moléculaire:356.44
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Help & FAQs
Activité biologique
Description
IC50 & Target
[3]|
NPFF1-R 3320 nM (Ki) |
NPFF2-R 1296 nM (Ki) |
In Vitro
AC-263093 (AC-093 hydrochloride) (1 μM; 15 min) inhibits Forskolin (HY-15371)-stimulated cAMP production in mRPTCs (mouse renal proximal tubule cells)[1].
AC-263093 (0.1 μM; 30 min) attenuates the stimulation of intracellular cAMP concentration by Fenoldopam (HY-B0735A) in hRPTCs (human renal proximal tubule cells)[1].
AC-263093 binds to human NPFFR2 and NPFFR1 with Ki values of 1296 nM and 3320 nM, respectively, and in a cAMP functional assay, it has a pEC50 of 5.2 for NPFFR2 with an efficacy of 78%[3].
AC-263093 is a full agonist of the recombinant human FF2 receptor in NIH-3T3 cells with a pEC50 of 5.9, and shows very low intrinsic efficacy at the human FF1 receptor (12% at 6 μM)[3].
AC-263093 has full efficacy at recombinant human FF2 receptors in HEK-293T cells, with a pEC50 of 5.2, and shows only weak agonist activity at human FF1 receptors (23% at 30 μM)[3].
AC-263093 binds human NPFFR1 and NPFFR2 with approximately equal affinity in radioligand binding assays (pKi = 7.0 and 6.9, respectively)[5].
AC-263093 (5 µM) functionally inhibits NPFFR1 in NIH/3T3 cells transfected with NPFFR1, completely abolishing 1 µM NPAF-induced β-galactosidase activity[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
AC-263093 (20 mg/kg; i.p.; once daily; 20 days) increased immobility time in the tail suspension test, induced anhedonic responses to sucrose, elicited anxiety-like behavior in the elevated plus maze, and decreased hippocampal GR and MR protein levels in wild-type C57BL/6 mouse models[2].
AC-263093 (10 mg/kg; i.p.; single administration; 15 min before formalin injection) selectively reduces formalin-induced phase 2 flinching behavior in rats[3].
AC-263093 (1-10 mg/kg; i.p.; single administration) dose- and time-dependently attenuated thermal hyperalgesia in the Carrageenan (HY-125474)-induced inflammatory thermal hyperalgesia model in SD rats[3].
AC-263093 (1-30 mg/kg; i.p.; single administration) dose-dependently reversed SNL-induced mechanical hypersensitivity in rats[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (male)[2]
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Dosage:30 mg/kg
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Administration:i.p.; single dose; 1 h before behavioral tests
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Result:Prominently up-regulated blood CORT and ACTH levels.
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Animal Model:C57BL/6 (male)[2]
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Dosage:20 mg/kg
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Administration:i.p.; once daily; for 20 consecutive days
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Result:After 20 days of AC-263093 administration, TST immobility time was enhanced, whereas FST immobility time was not altered.
Chronic AC-263093-exposed mice showed an anhedonic response to sucrose solution, with lower sucrose consumption and lower sucrose/water consumption ratio than control.
In the EPM, chronic AC-263093-exposed mice displayed anxiety-like behavior, with changes in time spent in open arms, time spent in closed arms, and open-arm entries.
Persistently increased serum CORT and decreased hippocampal GR and MR protein levels compared with control.
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Animal Model:Sprague-Dawley (male, 150-300 g)[3]
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Dosage:10 mg/kg
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Administration:i.p.; single dose; 15 min before formalin injection
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Result:Intraperitoneal administration of 10 mg/kg AC-263093 selectively inhibited flinching behavior in phase 2 (11-60 min) of the formalin test.
The phase 2 value obtained was 213.3 flinches.
Chemical Information
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CAS No. 849335-02-0
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Masse moléculaire 356.44
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Formule C8H9Br2ClN4
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SMILES
BrC1=CC=C(/C=N/NC(N)=N)C=C1Br.Cl
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Synonyms
AC-093 hydrochloride
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
AC-263093 Related Classifications
HY-123893 Related Classifications
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