NPS-467
NPS-467 is a calcium-sensing receptor (CaR) activator and stereospecific agent with only its R-enantiomer active. NPS-467 increases the sensitivity of the CaR to activation by extracellular calcium. NPS-467 stimulates stanniocalcin (STC) secretion in trout and induces inhibition of gill calcium transport in trout. NPS-467 has no effect on serum calcitonin levels in trout.
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- CAS. Nr.: 148717-47-9
- Formel: C18H23NO
- Molecular Weight:269.38
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
NPS-467 (R-enantiomer) (0.25-2.0 mg/kg; i.p.; single dose) produces stereospecific, dose-dependent inhibition of gill calcium transport in fingerling rainbow trout via enhanced STC release, with an ED50 of 0.5 mg/kg, and this effect is fully blocked by fish STC antiserum[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Oncorhynchus mykiss (juvenile, 150-250 g)[1]
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Dosage:0.25 mg/kg; 0.5 mg/kg; 1.0 mg/kg; 2.0 mg/kg
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Administration:i.p.; single dose
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Result:Produced statistically significant stimulatory effects on STC secretion (P < 0.01-0.001).
Raised serum STC levels maximally to 2069 ng/mL, representing a 9-fold induction over controls; the response plateaued at doses above 2.5 mg/kg.
Achieved an ED50 of 0.44 mg/kg for STC secretion stimulation.
Induced a rapid response, with maximal 14-fold STC induction by 0.5 hours post-injection, which persisted for up to 4 hours.
Showed no statistically significant effects on serum CT levels at doses of 0.25, 0.5, 1.0, or 2.0 mg/kg.
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Animal Model:Oncorhynchus mykiss (fingerling, 1-2 g)[1]
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Dosage:0.25 mg/kg; 0.5 mg/kg; 1.0 mg/kg; 2.0 mg/kg
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Administration:i.p.; single dose
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Result:Produced consistent, dose-dependent inhibitory effects on GCAT across three experiments, with statistically significant reductions at all tested doses (P < 0.05-0.01).
Achieved an ED50 of 0.5 mg/kg (2.5 μmol/kg) for GCAT inhibition, which was similar to the ED50 for STC secretion stimulation.
Had its inhibitory effects on GCAT at 2.0 mg/kg completely neutralized by passive immunization with fish STC antiserum, with GCAT rates not significantly different from controls receiving nonimmune rabbit serum alone.
Chemical Information
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CAS. Nr. 148717-47-9
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Molecular Weight 269.38
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Formel C18H23NO
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SMILES
CC(NCCCC1=CC=CC=C1)C2=CC(OC)=CC=C2
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
NPS-467 Related Classifications
HY-182543 Related Classifications
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