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Merck
CN

L5295

LY 320135

≥98% (HPLC)

Synonym(s):

4-[6-Methoxy-2-(4-methoxyphenyl)benzofuran-3-carbonyl]benzonitrile, LY320135, [6-Methoxy-2-(4-methoxyphenyl)benzo[b]furan-3-yl](4-cyanophenyl)methanone

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About This Item

Empirical Formula (Hill Notation):
C24H17NO4
CAS Number:
176977-56-3
Molecular Weight:
383.40
MDL number:
MFCD00945878
UNSPSC Code:
12352200
PubChem Substance ID:
329817622
NACRES:
NA.77

Key Documents

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Quality Level

100

Assay

≥98% (HPLC)

form

powder

color

orange

solubility

DMSO: ≥10 mg/mL

originator

Eli Lilly

storage temp.

2-8°C

SMILES string

COc1ccc(cc1)-c2oc3cc(OC)ccc3c2C(=O)c4ccc(cc4)C#N

InChI

1S/C24H17NO4/c1-27-18-9-7-17(8-10-18)24-22(20-12-11-19(28-2)13-21(20)29-24)23(26)16-5-3-15(14-25)4-6-16/h3-13H,1-2H3

InChI key

RYNSGDFWBJWWSZ-UHFFFAOYSA-N

Biochem/physiol Actions

LY320135 is a potent CB1 receptor antagonist/inverse agonist (Ki = 141 nM) with greater than 70-fold selectivity over CB2 receptors (Ki > 10 μM).
LY320135 is a potent CB1 receptor antagonist/inverse agonist (Ki = 141 nM) with greater than 70-fold selectivity over CB2 receptors (Ki > 10 μM). Structurally dissimilar from SR 141716A and AM 251. Shows weak binding to both 5-HT2 (Ki = 6.4 μM) and muscarinic receptors (Ki = 2.1 μM)

Features and Benefits

This compound is featured on the Cannabinoid Receptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
This compound was developed by Eli Lilly. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Pictograms

Skull and crossbones
GHS06

Signal Word

Danger

Hazard Statements

H301

Hazard Classifications

Acute Tox. 3 Oral

Storage Class Code

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Regulatory Information

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Certificates of Analysis (COA)

Lot/Batch Number
0000321719
0000321719
0000142108
070M4621V
0000142108

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K M Kampa-Schittenhelm et al.
EBioMedicine, 54, 102678-102678 (2020-04-10)
Overriding the differentiation blockage in acute myeloid leukemia (AML) is the most successful mode-of-action in leukemia therapy - now curing the vast majority of patients with acute promyelocytic leukemia (APL) using all-trans retinoic acid (ATRA)-based regimens. Similar approaches in other
Xinwen Zhang et al.
Neuropharmacology, 128, 269-281 (2017-10-25)
Monoacylglycerol lipase (MGL) hydrolyzes 2-arachidonoylglycerol to arachidonic acid and glycerol. Inhibition of MGL may attenuate neuroinflammation by enhancing endocannabinoid signaling and decreasing prostaglandin (PG) production. Almost half of HIV infected individuals are afflicted with HIV-associated neurocognitive disorder (HAND), a neuroinflammatory
Elham Khajehali et al.
Molecular pharmacology, 88(2), 368-379 (2015-06-06)
CB1 cannabinoid receptors (CB1Rs) are attractive therapeutic targets for numerous central nervous system disorders. However, clinical application of cannabinoid ligands has been hampered owing to their adverse on-target effects. Ligand-biased signaling from, and allosteric modulation of, CB1Rs offer pharmacological approaches

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