SML2225
RO5263397
≥98% (HPLC), TAAR1 agonist, powder
Synonym(s):
(S)-4-(3-Fluoro-2-methyl-phenyl)-4,5-dihydro-oxazol-2-ylamine
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About This Item
Empirical Formula (Hill Notation):
C10H11FN2O
CAS Number:
Molecular Weight:
194.21
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
Product Name
RO5263397, ≥98% (HPLC)
assay
≥98% (HPLC)
form
powder
optical activity
[α]/D +77 to +88°, c = 1.0 in methanol
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
SMILES string
NC1=N[C@@H](C2=CC=CC(F)=C2C)CO1
InChI
1S/C10H11FN2O/c1-6-7(3-2-4-8(6)11)9-5-14-10(12)13-9/h2-4,9H,5H2,1H3,(H2,12,13)/t9-/m1/s1
InChI key
IOHOUWIYOVWGHV-SECBINFHSA-N
Biochem/physiol Actions
Orally available, potent and selective partial TAAR1 agonist with similar in vivo efficacy as the full agonist RO5256390.
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.
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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