NPY5RA972 | CAS#439861-56-0 | Y Y5 antagonist

MedKoo Cat#: 562517 | Name: NPY5RA972

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Description:

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

NPY5RA972 is a neuropeptide Y Y5 antagonist.

Chemical Structure

NPY5RA972

CAS#439861-56-0

Theoretical Analysis

MedKoo Cat#: 562517

Name: NPY5RA972

CAS#: 439861-56-0

Chemical Formula: C21H25N3O2

Exact Mass: 351.1947

Molecular Weight: 351.45

Elemental Analysis: C, 71.77; H, 7.17; N, 11.96; O, 9.10

Price and Availability

Size	Price	Availability	Quantity
10mg	USD 345.00	2 Weeks
50mg	USD 1,100.00	2 Weeks

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Related CAS #

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Synonym

NPY5RA972; NPY-5-RA-972; NPY 5 RA 972;

IUPAC/Chemical Name

N-[4-Methyl-9-(1-methylethyl)-9H-carbazol-3-yl]-4-morpholinecarboxamide

InChi Key

ZNFMHLDBJPAFEQ-UHFFFAOYSA-N

InChi Code

InChI=1S/C21H25N3O2/c1-14(2)24-18-7-5-4-6-16(18)20-15(3)17(8-9-19(20)24)22-21(25)23-10-12-26-13-11-23/h4-9,14H,10-13H2,1-3H3,(H,22,25)

SMILES Code

O=C(N1CCOCC1)NC2=C(C)C3=C(C=C2)N(C(C)C)C4=C3C=CC=C4

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:

NPY5RA-972 is an orally active, central nervous system (CNS) penetrating, potent and selective NPY Y5 receptor antagonist.

In vitro activity:

TBD

In vivo activity:

This compound is central nervous system (CNS) penetrant, and an oral dose of 10 mg/kg NPY5RA-972 to rats produced concentrations in cerebrospinal fluid that greatly exceeded the in vitro IC(50) (inhibitory concentration 50%). Indeed, at doses to rats as low as 1 mg/kg, NPY5RA-972 inhibited feeding induced by intracerebroventricular (ICV) administration of a selective NPY Y5 agonist ([cPP(1-7),NPY(19-23),Ala(31),Aib(32),Gln(34)]-hPP). Reference: Diabetes. 2002 Aug;51(8):2441-9. https://pubmed.ncbi.nlm.nih.gov/12145156/

Preparing Stock Solutions

The following data is based on the product molecular weight 351.45 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. Turnbull AV, Ellershaw L, Masters DJ, Birtles S, Boyer S, Carroll D, Clarkson P, Loxham SJ, McAulay P, Teague JL, Foote KM, Pease JE, Block MH. Selective antagonism of the NPY Y5 receptor does not have a major effect on feeding in rats. Diabetes. 2002 Aug;51(8):2441-9. doi: 10.2337/diabetes.51.8.2441. PMID: 12145156. 2. Block MH, Boyer S, Brailsford W, Brittain DR, Carroll D, Chapman S, Clarke DS, Donald CS, Foote KM, Godfrey L, Ladner A, Marsham PR, Masters DJ, Mee CD, O'Donovan MR, Pease JE, Pickup AG, Rayner JW, Roberts A, Schofield P, Suleman A, Turnbull AV. Discovery and optimization of a series of carbazole ureas as NPY5 antagonists for the treatment of obesity. J Med Chem. 2002 Aug 1;45(16):3509-23. doi: 10.1021/jm011125x. PMID: 12139462.

In vitro protocol:

TBD

In vivo protocol:

1: Li P, Tiwari HK, Lin WY, Allison DB, Chung WK, Leibel RL, Yi N, Liu N. Genetic association analysis of 30 genes related to obesity in a European American population. Int J Obes (Lond). 2014 May;38(5):724-9. doi: 10.1038/ijo.2013.140. Epub 2013 Jul 31. PubMed PMID: 23900445; PubMed Central PMCID: PMC3909018. 2: Morris MJ, Gannan E, Stroud LM, Beck-Sickinger AG, O'Brien TJ. Neuropeptide Y suppresses absence seizures in a genetic rat model primarily through effects on Y receptors. Eur J Neurosci. 2007 Feb;25(4):1136-43. PubMed PMID: 17331209. 3: Gabriele B, Salerno G, Mancuso R, Costa M. Efficient synthesis of ureas by direct palladium-catalyzed oxidative carbonylation of amines. J Org Chem. 2004 Jul 9;69(14):4741-50. PubMed PMID: 15230597. 4: Turnbull AV, Ellershaw L, Masters DJ, Birtles S, Boyer S, Carroll D, Clarkson P, Loxham SJ, McAulay P, Teague JL, Foote KM, Pease JE, Block MH. Selective antagonism of the NPY Y5 receptor does not have a major effect on feeding in rats. Diabetes. 2002 Aug;51(8):2441-9. PubMed PMID: 12145156. 5: Block MH, Boyer S, Brailsford W, Brittain DR, Carroll D, Chapman S, Clarke DS, Donald CS, Foote KM, Godfrey L, Ladner A, Marsham PR, Masters DJ, Mee CD, O'Donovan MR, Pease JE, Pickup AG, Rayner JW, Roberts A, Schofield P, Suleman A, Turnbull AV. Discovery and optimization of a series of carbazole ureas as NPY5 antagonists for the treatment of obesity. J Med Chem. 2002 Aug 1;45(16):3509-23. PubMed PMID: 12139462.