N-PIPERIDINYL-[8-CHLORO-1-(2,4-DICHLOROPHENYL)-1,4,5,6-TETRAHYDROBENZO-[6,7]CYCLOHEPTAL[1,2-C]PYRAZOLE-3-CARBOXAMIDE

Product Name: N-PIPERIDINYL-[8-CHLORO-1-(2,4-DICHLOROPHENYL)-1,4,5,6-TETRAHYDROBENZO-[6,7]CYCLOHEPTAL[1,2-C]PYRAZOLE-3-CARBOXAMIDE
CAS No.: 494844-07-4
Chemical Name: N-PIPERIDINYL-[8-CHLORO-1-(2,4-DICHLOROPHENYL)-1,4,5,6-TETRAHYDROBENZO-[6,7]CYCLOHEPTAL[1,2-C]PYRAZOLE-3-CARBOXAMIDE
Synonyms: NESS 0327;NESS 0327 Exclusive;8-chloro-1-(2,4-dichlorophenyl)-N-piperidin-1-yl-5,6-dihydro-4H-benzo[2,3]cyclohepta[2,4-b]pyrazole-3-carboxamide;N-PIPERIDINYL-[8-CHLORO-1-(2,4-DICHLOROPHENYL)-1,4,5,6-TETRAHYDROBENZO-[6,7]CYCLOHEPTAL[1,2-C]PYRAZOLE-3-CARBOXAMIDE;N-PIPERIDINYL-[8-CHLORO-1-(2,4-DICHLOROPHENYL)-1,4,5,6-TETRAHYDROBENZO-[6,7]CYCLOHEPTAL[1,2-C]PYRAZOLE-3-CARBOXAMIDE;Benzo[6,7]cyclohepta[1,2-c]pyrazole-3-carboxamide, 8-chloro-1-(2,4-dichlorophenyl)-1,4,5,6-tetrahydro-N-1-piperidinyl-
CBNumber: CB9825071
Molecular Formula: C24H23Cl3N4O
Formula Weight: 489.82
MOL File: 494844-07-4.mol

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N-PIPERIDINYL-[8-CHLORO-1-(2,4-DICHLOROPHENYL)-1,4,5,6-TETRAHYDROBENZO-[6,7]CYCLOHEPTAL[1,2-C]PYRAZOLE-3-CARBOXAMIDE Property

storage temp.: Store at -20°C
solubility: ≤0.25mg/ml in ethanol;0.25mg/ml in DMSO;0.5mg/ml in dimethyl formamide
form: crystalline solid
color: White to off-white

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 10004184
Product name: NESS 0327
Purity: ≥98%
Packaging: 1mg
Price: $159
Updated: 2024/03/01

Cayman Chemical

Product number: 10004184
Product name: NESS 0327
Purity: ≥98%
Packaging: 5mg
Price: $398
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Cayman Chemical

Product number: 10004184
Product name: NESS 0327
Purity: ≥98%
Packaging: 10mg
Price: $636
Updated: 2024/03/01

Tocris

Product number: 5746
Product name: NESS0327
Purity: ≥98%(HPLC)
Packaging: 10
Price: $189
Updated: 2021/12/16

Tocris

Product number: 5746
Product name: NESS0327
Purity: ≥98%(HPLC)
Packaging: 50
Price: $795
Updated: 2021/12/16

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N-PIPERIDINYL-[8-CHLORO-1-(2,4-DICHLOROPHENYL)-1,4,5,6-TETRAHYDROBENZO-[6,7]CYCLOHEPTAL[1,2-C]PYRAZOLE-3-CARBOXAMIDE Chemical Properties,Usage,Production

Uses

NESS 0327 is a potent, selective CB1 receptor antagonist. Synthetic Cannabinoids

Biological Activity

ki: 0.35 pm and 21 nm for cb1 and cb2 receptor, respectively.ness 0327 is an extremely potent cannabinoid (cb) receptor antagonist.cannabinoid cb1 receptors are present in the central nervous system with the highest densities in the hippocampus, and to a lesser extent in some peripheral tissues. cannabinoid cb2 receptors are predominantly located in peripheral tissues. both receptors can negatively regulate adenylate cyclase and control the release of arachidonic acid.

in vitro

previous study found that ness 0327 exhibited a stronger selectivity for cb1 receptor compared with sr 141716a, showing a much higher affinity for cb1 receptor and a higher affinity for the cb2 receptor. affinity ratios demonstrated that ness 0327 was more than 60,000-fold selective for the cb1 receptor. ness 0327 alone did not produce concentration-dependent stimulation of guanosine 5'-o-(3-[35s]thio)-triphosphate binding in rat cerebella membranes. conversely, ness 0327 antagonized win 55,212-2-stimulated guanosine 5'-o-(3-[35s]thio)-triphosphate binding. in functional assay, ness 0327 could antagonize the inhibitory effects of win 55,212-2 on electrically evoked contractions in mouse isolated vas deferens preparations [1].

in vivo

in vivo studies showed that ness 0327 could antagonize the antinociceptive effect produced by win 55,212-2 in both tail-flick and hot-plate test, suggesting that ness 0327 was a novel cannabinoid antagonist with high selectivity for the cannabinoid cb1 receptor [1].

storage

Store at -20°C

References

[1] ruiu, s. ,pinna, g.a.,marchese, g., et al. synthesis and characterization of ness 0327: a novel putative antagonist of the cb1 cannabinoid receptor. journal of pharmacology and experimental therapeutics 306(1), 363-370 (2003).

N-PIPERIDINYL-[8-CHLORO-1-(2,4-DICHLOROPHENYL)-1,4,5,6-TETRAHYDROBENZO-[6,7]CYCLOHEPTAL[1,2-C]PYRAZOLE-3-CARBOXAMIDE Preparation Products And Raw materials

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494844-07-4, N-PIPERIDINYL-[8-CHLORO-1-(2,4-DICHLOROPHENYL)-1,4,5,6-TETRAHYDROBENZO-[6,7]CYCLOHEPTAL[1,2-C]PYRAZOLE-3-CARBOXAMIDERelated Search:

N-Aminopiperidine hydrochloride N-PIPERIDINYL-[8-CHLORO-1-(2,4-DICHLOROPHENYL)-1,4,5,6-TETRAHYDROBENZO-[6,7]CYCLOHEPTAL[1,2-C]PYRAZOLE-3-CARBOXAMIDE Rimonabant hydrochloride

NESS 0327

N-PIPERIDINYL-[8-CHLORO-1-(2,4-DICHLOROPHENYL)-1,4,5,6-TETRAHYDROBENZO-[6,7]CYCLOHEPTAL[1,2-C]PYRAZOLE-3-CARBOXAMIDE

8-chloro-1-(2,4-dichlorophenyl)-N-piperidin-1-yl-5,6-dihydro-4H-benzo[2,3]cyclohepta[2,4-b]pyrazole-3-carboxamide

NESS 0327 Exclusive

Benzo[6,7]cyclohepta[1,2-c]pyrazole-3-carboxamide, 8-chloro-1-(2,4-dichlorophenyl)-1,4,5,6-tetrahydro-N-1-piperidinyl-

N-PIPERIDINYL-[8-CHLORO-1-(2,4-DICHLOROPHENYL)-1,4,5,6-TETRAHYDROBENZO-[6,7]CYCLOHEPTAL[1,2-C]PYRAZOLE-3-CARBOXAMIDE

494844-07-4