Ness0327

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MedKoo CAT#: 563390

CAS#: 494844-07-4

Description: Ness0327 is a potent cannabinoid CB1 receptor antagonist.


Price and Availability

Size Price Shipping out time Quantity
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Pricing updated 2020-10-30. Prices are subject to change without notice.

Ness0327 is not in stock, may be available through custom synthesis. For cost-effective reason, minimum 1 gram order is requested. The product will be characterized by NMR, HPLC and MS analysis. Purity (HPLC) is usually >98%. CoA, QC data, MSDS will be provided when product is successfully made. The estimated lead time is 2-3 months. Please send email to sales@medkoo.com to inquire quote.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 563390
Name: Ness0327
CAS#: 494844-07-4
Chemical Formula: C24H23Cl3N4O
Exact Mass: 488.0937
Molecular Weight: 489.82
Elemental Analysis: C, 58.85; H, 4.73; Cl, 21.71; N, 11.44; O, 3.27


Synonym: Ness0327; Ness-0327; Ness 0327;

IUPAC/Chemical Name: 8-chloro-1-(2,4-dichlorophenyl)-1,4,5,6-tetrahydro-N-1-piperidinyl-benzo[6,7]cyclohepta[1,2-c]pyrazole-3-carboxamide

InChi Key: NCXBPZJQQSNIRA-UHFFFAOYSA-N

InChi Code: InChI=1S/C24H23Cl3N4O/c25-16-7-9-18-15(13-16)5-4-6-19-22(24(32)29-30-11-2-1-3-12-30)28-31(23(18)19)21-10-8-17(26)14-20(21)27/h7-10,13-14H,1-6,11-12H2,(H,29,32)

SMILES Code: O=C(C1=NN(C2=CC=C(Cl)C=C2Cl)C3=C1CCCC4=CC(Cl)=CC=C43)NN5CCCCC5


Technical Data

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:
2934.99.03.00


References

1: Gomis-González M, Busquets-Garcia A, Matute C, Maldonado R, Mato S, Ozaita A. Possible Therapeutic Doses of Cannabinoid Type 1 Receptor Antagonist Reverses Key Alterations in Fragile X Syndrome Mouse Model. Genes (Basel). 2016 Aug 31;7(9). pii: E56. doi: 10.3390/genes7090056. PubMed PMID: 27589806; PubMed Central PMCID: PMC5042387.

2: Lee SH, Ledri M, Tóth B, Marchionni I, Henstridge CM, Dudok B, Kenesei K, Barna L, Szabó SI, Renkecz T, Oberoi M, Watanabe M, Limoli CL, Horvai G, Soltesz I, Katona I. Multiple Forms of Endocannabinoid and Endovanilloid Signaling Regulate the Tonic Control of GABA Release. J Neurosci. 2015 Jul 8;35(27):10039-57. doi: 10.1523/JNEUROSCI.4112-14.2015. PubMed PMID: 26157003; PubMed Central PMCID: PMC4495235.

3: Kim J, Watkins BA. Cannabinoid receptor antagonists and fatty acids alter endocannabinoid system gene expression and COX activity. J Nutr Biochem. 2014 Aug;25(8):815-23. doi: 10.1016/j.jnutbio.2014.03.012. Epub 2014 Apr 4. PubMed PMID: 24854955.

4: Kim J, Carlson ME, Watkins BA. Docosahexaenoyl ethanolamide improves glucose uptake and alters endocannabinoid system gene expression in proliferating and differentiating C2C12 myoblasts. Front Physiol. 2014 Mar 21;5:100. doi: 10.3389/fphys.2014.00100. eCollection 2014. PubMed PMID: 24711795; PubMed Central PMCID: PMC3968752.

5: Meye FJ, Trezza V, Vanderschuren LJ, Ramakers GM, Adan RA. Neutral antagonism at the cannabinoid 1 receptor: a safer treatment for obesity. Mol Psychiatry. 2013 Dec;18(12):1294-301. doi: 10.1038/mp.2012.145. Epub 2012 Oct 16. PubMed PMID: 23070073.

6: Chiba T, Ueno S, Obara Y, Nakahata N. A synthetic cannabinoid, CP55940, inhibits lipopolysaccharide-induced cytokine mRNA expression in a cannabinoid receptor-independent mechanism in rat cerebellar granule cells. J Pharm Pharmacol. 2011 May;63(5):636-47. doi: 10.1111/j.2042-7158.2011.01250.x. Epub 2011 Mar 28. PubMed PMID: 21492165.

7: Latek D, Kolinski M, Ghoshdastider U, Debinski A, Bombolewski R, Plazinska A, Jozwiak K, Filipek S. Modeling of ligand binding to G protein coupled receptors: cannabinoid CB1, CB2 and adrenergic β 2 AR. J Mol Model. 2011 Sep;17(9):2353-66. doi: 10.1007/s00894-011-0986-7. Epub 2011 Mar 2. PubMed PMID: 21365223.

8: Bertalovitz AC, Ahn KH, Kendall DA. Ligand Binding Sensitivity of the Extracellular Loop Two of the Cannabinoid Receptor 1. Drug Dev Res. 2010 Nov 1;71(7):404-411. PubMed PMID: 21170298; PubMed Central PMCID: PMC3003262.

9: Murineddu G, Ruiu S, Loriga G, Manca I, Lazzari P, Reali R, Pani L, Toma L, Pinna GA. Tricyclic pyrazoles. 3. Synthesis, biological evaluation, and molecular modeling of analogues of the cannabinoid antagonist 8-chloro-1-(2',4'-dichlorophenyl)-N-piperidin-1-yl-1,4,5,6-tetrahydrobenzo[6,7]cy clohepta[1,2-c]pyrazole-3-carboxamide. J Med Chem. 2005 Nov 17;48(23):7351-62. PubMed PMID: 16279795.

10: Tambaro S, Mongeau R, Dessi C, Pani L, Ruiu S. Modulation of ATP-mediated contractions of the rat vas deferens through presynaptic cannabinoid receptors. Eur J Pharmacol. 2005 Nov 21;525(1-3):150-3. Epub 2005 Nov 3. PubMed PMID: 16271359.

11: Ruiu S, Pinna GA, Marchese G, Mussinu JM, Saba P, Tambaro S, Casti P, Vargiu R, Pani L. Synthesis and characterization of NESS 0327: a novel putative antagonist of the CB1 cannabinoid receptor. J Pharmacol Exp Ther. 2003 Jul;306(1):363-70. Epub 2003 Mar 27. PubMed PMID: 12663689.