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SML1936

Ro 64-6198

≥98% (HPLC), nociceptin receptor ORL-1 (ORL1) agonist , powder

Synonym(s):

(1S,3aS)-8-(2,3,3a,4,5,6-Hexahydro-1H-phenalen-1-yl)-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one, 8-[(1S,3aS)-2,3,3a,4,5,6-Hexahydro-1H-phenalen-1-yl]-1-phenyl-1,3,8-Triazaspiro[4.5]decan-4-one, Ro64-6198

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About This Item

Empirical Formula (Hill Notation):
C26H31N3O
CAS Number:
280783-56-4
Molecular Weight:
401.54
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
MFCD04113242
Assay:
≥98% (HPLC)
Form:
powder
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Product Name

Ro 64-6198, ≥98% (HPLC)

Quality Segment

100

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

SMILES string

O=C1C2(CCN([C@]3([H])C4=CC=CC5=C4[C@](CCC5)([H])CC3)CC2)N(C6=CC=CC=C6)CN1

InChI

1S/C26H31N3O/c30-25-26(29(18-27-25)21-9-2-1-3-10-21)14-16-28(17-15-26)23-13-12-20-7-4-6-19-8-5-11-22(23)24(19)20/h1-3,5,8-11,20,23H,4,6-7,12-18H2,(H,27,30)/t20-,23-/m0/s1

InChI key

JLFMYEAXZNPWBK-REWPJTCUSA-N

Biochem/physiol Actions

A brain-penetrant, nonpeptidic, high-affinity, reversible, selective nociceptin receptor ORL-1 (ORL1) agonist that elicits anxiolytic-like effects in vivo.
Ro 64-6198 is a brain-penetrant, nonpeptidic, high-affinity (Ki = 0.389 nM against 0.1 nM OFQ for binding human ORL1) nociceptin/orphanin FQ (N/OFQ) receptor ORL-1 (KOR-3, NOP) agonist (EC50 = 38.9 nM by GTPγS binding assay; IC50 = 32.4 nM against forskolin-stimulated cellular cAMP accumulation) with >100-fold selectivity over other opioid receptor family members (Ki = 46.8 nM/μ, 89.1 nM/k, 1.38 μM/δ) and no significant affinity toward 48 other receptors and ion channels (IC50 >1 μM). Ro 64-6198 elicits ORL1-dependent anxiolytic-like effects in several rat models of spontaneous and conditioned anxiety states (0.3-3.2 mg/kg i.p) without antipanic, anticonvulsant, sedative, amnestic activity, or signs of tolerance to its anxiolytic-like effects following chronical dosing.

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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