LY320135 | CAS#176977-56-3 | CB1 Receptor Antagonist |MedKoo

MedKoo Cat#: 532158 | Name: LY320135

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

LY320135 is a selective antagonist for the brain CB1 receptor. LY320135 has a greater than 70-fold higher affinity for the CB1 than the peripheral CB2 receptor. The Ki values for LY320135 at the CB1 and CB2 receptors were 224 nM and > 10 microM, respectively.

Chemical Structure

LY320135

CAS#176977-56-3

Theoretical Analysis

MedKoo Cat#: 532158

Name: LY320135

CAS#: 176977-56-3

Chemical Formula: C24H17NO4

Exact Mass: 383.1158

Molecular Weight: 383.40

Elemental Analysis: C, 75.19; H, 4.47; N, 3.65; O, 16.69

Price and Availability

Size	Price	Availability	Quantity
10mg	USD 350.00	2 weeks
25mg	USD 750.00	2 weeks

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Synonym

LY320135; LY 320135; LY-320135.

IUPAC/Chemical Name

4-[6-methoxy-2-(4-methoxyphenyl)1-benzofuran-3-carbonyl]benzonitrile

InChi Key

RYNSGDFWBJWWSZ-UHFFFAOYSA-N

InChi Code

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

SMILES Code

N#CC1=CC=C(C(C2=C(C3=CC=C(OC)C=C3)OC4=C2C=CC(OC)=C4)=O)C=C1

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

LY320135 is a potent and selective antagonist of CB1 receptor, with a Ki of 141 nM. LY320135 also binds to 5-HT2 and muscarinic receptors with Kis of 6.4 μM and 2.1 μM.

In vitro activity:

LY320135 is a selective antagonist for the brain CB1 receptor, having greater than 70-fold higher affinity for the CB1 than the peripheral CB2 receptor. The Ki values for LY320135 at the CB1 and CB2 receptors, transfected and stably expressed in cell lines, were 224 nM and > 10 microM, respectively. Reference: J Pharmacol Exp Ther. 1998 Jan;284(1):291-7. https://pubmed.ncbi.nlm.nih.gov/9435190/

In vivo activity:

The inhibitory effect of methanandamide on cyclic AMP accumulation was prevented by incubation of the rat arteries with pertussis toxin and was significantly reduced by LY320135, a selective CB1 antagonist, but not by SR 144528, a CB2-selective antagonist. Reference: Br J Pharmacol. 1999 Oct;128(3):597-604. https://pubmed.ncbi.nlm.nih.gov/10516638/

	Solvent	mg/mL	mM
Solubility
	DMF	25.0	65.21
	DMSO	25.0	65.21
	DMSO:PBS (pH 7.2) (1:1)	0.5	1.30
	Ethanol	0.2	0.52

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 383.40 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Ledgerwood CJ, Greenwood SM, Brett RR, Pratt JA, Bushell TJ. Cannabidiol inhibits synaptic transmission in rat hippocampal cultures and slices via multiple receptor pathways. Br J Pharmacol. 2011 Jan;162(1):286-94. doi: 10.1111/j.1476-5381.2010.01015.x. PMID: 20825410; PMCID: PMC3012422. 2. Felder CC, Joyce KE, Briley EM, Glass M, Mackie KP, Fahey KJ, Cullinan GJ, Hunden DC, Johnson DW, Chaney MO, Koppel GA, Brownstein M. LY320135, a novel cannabinoid CB1 receptor antagonist, unmasks coupling of the CB1 receptor to stimulation of cAMP accumulation. J Pharmacol Exp Ther. 1998 Jan;284(1):291-7. PMID: 9435190. 3. Landucci E, Scartabelli T, Gerace E, Moroni F, Pellegrini-Giampietro DE. CB1 receptors and post-ischemic brain damage: studies on the toxic and neuroprotective effects of cannabinoids in rat organotypic hippocampal slices. Neuropharmacology. 2011 Mar;60(4):674-82. doi: 10.1016/j.neuropharm.2010.11.021. Epub 2010 Dec 3. PMID: 21130785. 4. Holland M, John Challiss RA, Standen NB, Boyle JP. Cannabinoid CB1 receptors fail to cause relaxation, but couple via Gi/Go to the inhibition of adenylyl cyclase in carotid artery smooth muscle. Br J Pharmacol. 1999 Oct;128(3):597-604. doi: 10.1038/sj.bjp.0702842. PMID: 10516638; PMCID: PMC1571683.

In vitro protocol:

In vivo protocol:

1. Landucci E, Scartabelli T, Gerace E, Moroni F, Pellegrini-Giampietro DE. CB1 receptors and post-ischemic brain damage: studies on the toxic and neuroprotective effects of cannabinoids in rat organotypic hippocampal slices. Neuropharmacology. 2011 Mar;60(4):674-82. doi: 10.1016/j.neuropharm.2010.11.021. Epub 2010 Dec 3. PMID: 21130785. 2. Holland M, John Challiss RA, Standen NB, Boyle JP. Cannabinoid CB1 receptors fail to cause relaxation, but couple via Gi/Go to the inhibition of adenylyl cyclase in carotid artery smooth muscle. Br J Pharmacol. 1999 Oct;128(3):597-604. doi: 10.1038/sj.bjp.0702842. PMID: 10516638; PMCID: PMC1571683.

1: Felder CC, Joyce KE, Briley EM, Glass M, Mackie KP, Fahey KJ, Cullinan GJ, Hunden DC, Johnson DW, Chaney MO, Koppel GA, Brownstein M. LY320135, a novel cannabinoid CB1 receptor antagonist, unmasks coupling of the CB1 receptor to stimulation of cAMP accumulation. J Pharmacol Exp Ther. 1998 Jan;284(1):291-7. PubMed PMID: 9435190.