NPY5RA972
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 562517

CAS#: 439861-56-0

Description: NPY5RA972 is a neuropeptide Y Y5 antagonist.


Chemical Structure

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NPY5RA972
CAS# 439861-56-0

Theoretical Analysis

MedKoo Cat#: 562517
Name: NPY5RA972
CAS#: 439861-56-0
Chemical Formula: C21H25N3O2
Exact Mass: 351.19
Molecular Weight: 351.450
Elemental Analysis: C, 71.77; H, 7.17; N, 11.96; O, 9.10

Price and Availability

Size Price Availability Quantity
10mg USD 345 2 Weeks
50mg USD 1100 2 Weeks
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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:
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.

Recalculate based on batch purity %
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. 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.

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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.