LU AA33810 | CAS# 304008-29-5 | NPY Y5 receptor antagonist

MedKoo Cat#: 574371 | Name: LU AA33810

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Description:

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

LU AA33810 is a neuropeptide Y (NPY) Y5 receptor antagonist with affinity for Y5 over Y1, Y2 and Y4 receptors. LU AA33810 also binds human 5-HT2B and 5-HT1A receptors and exerts anxiolytic- and antidepressant-like effects.

Chemical Structure

LU AA33810

CAS#304008-29-5

Theoretical Analysis

MedKoo Cat#: 574371

Name: LU AA33810

CAS#: 304008-29-5

Chemical Formula: C19H25N3O2S3

Exact Mass: 423.1109

Molecular Weight: 423.61

Elemental Analysis: C, 53.87; H, 5.95; N, 9.92; O, 7.55; S, 22.70

Price and Availability

Size	Price	Availability
5mg	USD 285.00	2 Weeks
10mg	USD 450.00	2 Weeks
25mg	USD 850.00	2 Weeks

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Synonym

LU AA33810, LU-AA33810

IUPAC/Chemical Name

N-[[trans-4-[(4,5-Dihydro[1]benzothiepino[5,4-d]thiazol-2-yl)amino]cyclohexyl]methyl]methanesulfonamide

InChi Key

UWSBTSAJZMIHBL-HDJSIYSDSA-N

InChi Code

InChI=1S/C19H25N3O2S3/c1-27(23,24)20-12-13-6-8-14(9-7-13)21-19-22-18-15-4-2-3-5-16(15)25-11-10-17(18)26-19/h2-5,13-14,20H,6-12H2,1H3,(H,21,22)/t13-,14-

SMILES Code

CS(=O)(NC[C@H]1CC[C@H](NC2=NC3=C(CCSC4=CC=CC=C43)S2)CC1)=O

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

>3 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:

Lu AA33810 is a potent and selective antagonist of neuropeptide Y5 receptor with a Ki of 1.5 nM for the human receptor.

In vitro activity:

This study identified a novel Y(5) receptor-selective antagonist, Lu AA33810 [N-[[trans-4-[(4,5-dihydro[1]-benzothiepino[5,4-d]thiazol-2-yl)amino]cyclohexyl]methyl]-methanesulfonamide], that bound to cloned rat Y(5) receptors (K(i) = 1.5 nM) and antagonized NPY-evoked cAMP and calcium mobilization in vitro. Reference: J Pharmacol Exp Ther. 2009 Mar;328(3):900-11. https://pubmed.ncbi.nlm.nih.gov/19098165/

In vivo activity:

Lu AA33810 administered intraperitoneally at a single dose of 10 mg/kg both reversed depressive-like behavioral changes in the forced swim test (FST) and prevented degeneration of astrocytes in the mPFC. Reference: Psychopharmacology (Berl). 2017 Feb;234(4):631-645. https://pubmed.ncbi.nlm.nih.gov/27975125/

	Solvent	mg/mL	mM	comments
Solubility
	DMSO	42.4	100.00

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 423.61 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. Walker MW, Wolinsky TD, Jubian V, Chandrasena G, Zhong H, Huang X, Miller S, Hegde LG, Marsteller DA, Marzabadi MR, Papp M, Overstreet DH, Gerald CP, Craig DA. The novel neuropeptide Y Y5 receptor antagonist Lu AA33810 [N-[[trans-4-[(4,5-dihydro[1]benzothiepino[5,4-d]thiazol-2-yl)amino]cyclohexyl]methyl]-methanesulfonamide] exerts anxiolytic- and antidepressant-like effects in rat models of stress sensitivity. J Pharmacol Exp Ther. 2009 Mar;328(3):900-11. doi: 10.1124/jpet.108.144634. Epub 2008 Dec 19. PMID: 19098165. 2. Domin H, Szewczyk B, Pochwat B, Woźniak M, Śmiałowska M. Antidepressant-like activity of the neuropeptide Y Y5 receptor antagonist Lu AA33810: behavioral, molecular, and immunohistochemical evidence. Psychopharmacology (Berl). 2017 Feb;234(4):631-645. doi: 10.1007/s00213-016-4495-3. Epub 2016 Dec 14. PMID: 27975125; PMCID: PMC5263200. 3. Packiarajan M, Marzabadi MR, Desai M, Lu Y, Noble SA, Wong WC, Jubian V, Chandrasena G, Wolinsky TD, Zhong H, Walker MW, Wiborg O, Andersen K. Discovery of Lu AA33810: a highly selective and potent NPY5 antagonist with in vivo efficacy in a model of mood disorder. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5436-41. doi: 10.1016/j.bmcl.2011.06.124. Epub 2011 Jul 2. PMID: 21782428.

In vitro protocol:

In vivo protocol:

1. Domin H, Szewczyk B, Pochwat B, Woźniak M, Śmiałowska M. Antidepressant-like activity of the neuropeptide Y Y5 receptor antagonist Lu AA33810: behavioral, molecular, and immunohistochemical evidence. Psychopharmacology (Berl). 2017 Feb;234(4):631-645. doi: 10.1007/s00213-016-4495-3. Epub 2016 Dec 14. PMID: 27975125; PMCID: PMC5263200. 2. Packiarajan M, Marzabadi MR, Desai M, Lu Y, Noble SA, Wong WC, Jubian V, Chandrasena G, Wolinsky TD, Zhong H, Walker MW, Wiborg O, Andersen K. Discovery of Lu AA33810: a highly selective and potent NPY5 antagonist with in vivo efficacy in a model of mood disorder. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5436-41. doi: 10.1016/j.bmcl.2011.06.124. Epub 2011 Jul 2. PMID: 21782428.

1. Walker et al (2009) The novel neuropeptide Y Y5 receptor antagonist Lu AA33810 [N-[[trans-4-[(4,5-dihydro[1]benzothiepino[5,4-d]thiazol-2-yl)amino]cyclohexyl]methyl]-methanesulfonamide] exerts anxiolytic- and antidepressant-like effects J.Pharmacol.Exp.Ther. 328 900 PMID: 19098165