RO5263397

RO5263397

Biochem/physiol Actions

RO5256390 is an orally available partial agonist that targets trace amine-associated receptor 1 (TAAR1) with high affinity (Ki in nM = 0.9/mouse, 4.1/human, 9.1/rat, 24/monkey TARR1), potency (EC50 in nM/relative efficacy with respect to β-phenylethylamine = 1.3/0.59/mouse, 17/0.81/human, 47/0.76/rat, 251/0.85/monkey TARR1-dependent cellular cAMP production), and selectivity (by a 112-receptor/channel/transporter and a 42-enzyme panel), without agonistic activity toward mouse TAAR4-expressing cells even at a high concentration of 30 μM. When applied via oral administration (0.003-1 mg/kg), RO5256390 exhibits similar in vivo efficacy as the full agonist RO5256390 in blocking psychostimulants-induced hyperlocomotion in mice.

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Code Description Colour Manufacturer Storage Temp. Solubility Form Assay Price Quantity
3575991 RO5263397 white to beige SIGMA-ALDRICH 2-8°C DMSO: 2 mg/mL, clear
£501.43 (exc VAT) per 25MG
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3575992 RO5263397 white to beige SIGMA-ALDRICH 2-8°C DMSO: 2 mg/mL, clear
£124.24 (exc VAT) per 5MG
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