assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear (Warmed)
storage temp.
-10 to -25°C
Quality Level
Biochem/physiol Actions
Orally active dopamine receptor D1-selective postive allosteric modulator (PAM) in vitro and in vivo.
UCM-1306 is an orally active dopamine receptor D1-selective postive allosteric modulator (PAM) void of D1 agonist activity. UCM-1306 potentiates dopamine (DA)-induced cAMP in the SK-N-MC neuroblastoma cell line with endogenous D1R (EC50/Emax = 60 nM/45% with [DA] = EC70; Emax = 55% with [DA] = 10 μM), but not D5R, by modulating DA affinity for the receptor, while displaying low binding competition against orthosteric ligands. UCM-1306 augments cocaine (20 mg/kg s.c.)-induced locomotion (1 mg/kg i.p.) and enhances L-DOPA (100-400 mg/kg i.p.) recovery of decreased locomotor activity in reserpinized (2.5 mg/kg s.c.) mice in vivo (30 mg/kg p.o.).
UCM-1306 is an orally active dopamine receptor D1-selective postive allosteric modulator (PAM) void of D1 agonist activity. UCM-1306 potentiates dopamine (DA)-induced cAMP in the SK-N-MC neuroblastoma cell line with endogenous D1R (EC50/Emax = 60 nM/45% with [DA] = EC70; Emax = 55% with [DA] = 10 μM), but not D5R, by modulating DA affinity for the receptor, while displaying low binding competition against orthosteric ligands. UCM-1306 augments cocaine (20 mg/kg s.c.)-induced locomotion (1 mg/kg i.p.) and enhances L-DOPA (100-400 mg/kg i.p.) recovery of decreased locomotor activity in reserpinized (2.5 mg/kg s.c.) mice in vivo (30 mg/kg p.o.).
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