Slv319 - CAS 362519-49-1
Catalog number: B0084-112540
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C23H20Cl2N4O2S
Molecular Weight:
487.399
COA:
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Targets:
Cannabinoid Receptor
Description:
Slv319 is a potent antagonist of CB1 recceptor (Ki = 7.8 nM) used for the treatment of neuroinflammatory disorders, cognitive disorders, septic shock, obesity, psychosis, addiction and gastrointestinal disorders, as well as inhibits CP 55,940-induced hypotension and WIN 55,212-2-induced hypothermia in vivo.
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-112540 25 mg $298 In stock
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Brife Description:
CB1 recceptor antagonist
Purity:
98%
Appearance:
Solid Powder
Synonyms:
Slv319; Slv 319; Slv-319; 3-(4-Chlorophenyl)-N-[(4-chlorophenyl)sulfonyl]-4,5-dihydro-N'-methyl-4-phenyl-1H-pyrazole-1-carboximidamide; CHEMBL158784
Solubility:
Soluble in DMSO.
Storage:
Store in a cool and dry place and at 0-4 ℃ for short term (days to weeks) or -66 ℃ for long term (months to years).
MSDS:
Inquire
Shelf Life:
2 years
InChIKey:
AXJQVVLKUYCICH-UHFFFAOYSA-N
InChI:
InChI=1S/C23H20Cl2N4O2S/c1-26-23(28-32(30,31)20-13-11-19(25)12-14-20)29-15-21(16-5-3-2-4-6-16)22(27-29)17-7-9-18(24)10-8-17/h2-14,21H,15H2,1H3,(H,26,28)
Canonical SMILES:
CN=C(NS(=O)(=O)C1=CC=C(C=C1)Cl)N2CC(C(=N2)C3=CC=C(C=C3)Cl)C4=CC=CC=C4
1.Pooled sample strategy in conjunction with high-resolution liquid chromatography-mass spectrometry-based background subtraction to identify toxicological markers in dogs treated with ibipinabant.
Zhang H1, Patrone L, Kozlosky J, Tomlinson L, Cosma G, Horvath J. Anal Chem. 2010 May 1;82(9):3834-9. doi: 10.1021/ac100287a.
Metabolomics with chromatography-mass spectrometry is often challenging and relies on statistical tools to discern changes in a metabolome. A pooled sample strategy was proposed, consisting of (1) identification of potential marker candidates by detecting changes of metabolites in a few pooled samples between treated and control groups and (2) validation of markers of statistically significant changes with a large set of individual samples. This strategy was enabled by applying a thorough background subtraction approach based on high-resolution mass spectrometry. In a proof-of-principle study, plasma samples were generated and pooled in a 6-week investigational study to identify potential toxicological markers for an observed muscle toxicity associated with the treatment of ibipinabant in dogs. With pooled control samples as backgrounds, potential marker candidates were revealed in the background-subtracted profiles of the pooled ibipinabant-treated samples.
2.Diaryl dihydropyrazole-3-carboxamides with significant in vivo antiobesity activity related to CB1 receptor antagonism: synthesis, biological evaluation, and molecular modeling in the homology model.
Srivastava BK1, Joharapurkar A, Raval S, Patel JZ, Soni R, Raval P, Gite A, Goswami A, Sadhwani N, Gandhi N, Patel H, Mishra B, Solanki M, Pandey B, Jain MR, Patel PR. J Med Chem. 2007 Nov 29;50(24):5951-66. Epub 2007 Nov 3.
A number of analogues of diaryl dihydropyrazole-3-carboxamides have been synthesized. Their activities were evaluated for appetite suppression and body weight reduction in animal models. Depending on the chemical modification of the selected dihydropyrazole scaffold, the lead compounds--the bisulfate salt of (+/-)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4,5-dihydro-1H-pyrazole-3-carboxylic acid morpholin-4-ylamide 26 and the bisulfate salt of (-)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4,5-dihydro-1H-pyrazole-3-carboxylic acid morpholin-4-ylamide 30--showed significant body weight reduction in vivo, which is attributed to their CB1 antagonistic activity and exhibited a favorable pharmacokinetic profile. The molecular modeling studies also showed interactions of two isomers of (+/-)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4,5-dihydro-1H-pyrazole-3-carboxylic acid morpholin-4-ylamide 9 with CB1 receptor in the homology model similar to those of N-piperidino-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-3-pyrazole-carboxamide (rimonabant) 1 and 4S-(-)-3-(4-chlorophenyl)-N-methyl-N'-[(4-chlorophenyl)-sulfonyl]-4-phenyl-4,5-dihydro-1H-pyrazole-1-carboxamidine (SLV-319) 2.
3.Bioisosteric replacement of dihydropyrazole of 4S-(-)-3-(4-chlorophenyl)-N-methyl-N'-[(4-chlorophenyl)-sulfonyl]-4-phenyl-4,5-dihydro-1H-pyrazole-1-caboxamidine (SLV-319) a potent CB1 receptor antagonist by imidazole and oxazole.
Srivastava BK1, Soni R, Joharapurkar A, Sairam KV, Patel JZ, Goswami A, Shedage SA, Kar SS, Salunke RP, Gugale SB, Dhawas A, Kadam P, Mishra B, Sadhwani N, Unadkat VB, Mitra P, Jain MR, Patel PR. Bioorg Med Chem Lett. 2008 Feb 1;18(3):963-8. doi: 10.1016/j.bmcl.2007.12.036. Epub 2007 Dec 23.
Design, synthesis and conformational analysis of few imidazole and oxazole as bioisosters of 4S-(-)-3-(4-chlorophenyl)-N-methyl-N'-[(4-chlorophenyl)-sulfonyl]-4-phenyl-4,5-dihydro-1H-pyrazole-1-caboxamidine (SLV-319) 2 is reported. Computer assisted conformational analysis gave a direct clue for the loss of CB1 antagonistic activity of the ligands without a fine docking simulation for the homology model.
4.The relationship of in vivo central CB1 receptor occupancy to changes in cortical monoamine release and feeding elicited by CB1 receptor antagonists in rats.
Need AB1, Davis RJ, Alexander-Chacko JT, Eastwood B, Chernet E, Phebus LA, Sindelar DK, Nomikos GG. Psychopharmacology (Berl). 2006 Jan;184(1):26-35. Epub 2005 Nov 18.
RATIONALE: Cannabinoid type 1 (CB(1)) receptor antagonists are reportedly effective in reducing food intake both preclinically and clinically. This may be due in part to their effects on monoamine release in the brain. The level of central CB(1) receptor occupancy underlying these neurobiological effects is unclear.
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CAS 362519-49-1 Slv319

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