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(R)-SLV 319
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
(R)-SLV 319图片
CAS NO:656827-86-0
包装与价格：
包装价格(元)
1mg电议
5mg电议
10mg电议

产品介绍
(R)-SLV 319 是一种有效的选择性大麻素受体 1 (CB1) 拮抗剂，Ki 值为 894 nM。
Cas No.656827-86-0
化学名3-(4-chlorophenyl)-N-[(4-chlorophenyl)sulfonyl]-4,5-dihydro-N'-methyl-4R-phenyl-1H-pyrazole-1-carboximidamide
Canonical SMILESC/N=C(\NS(=O)(=O)c1ccc(Cl)cc1)/N1N=C(c2ccc(Cl)cc2)[C@@H](C1)c1ccccc1
分子式C23H20Cl2N4O2S
分子量487.4
溶解度≤30mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Ki: 7.8 and 7943 nM for CB1 and CB2 receptors, respectively by SLV 319

(R)-SLV 319 is a CB1 receptor antagonist.

Central cannabinoid (CB1) receptor antagonists can be used in the treatment of various diseases including cognitive disorders, neuroinflammatory disorders, obesity, septic shock, psychosis, addiction, as well as gastrointestinal disorders.

In vitro: (R)-SLV 319 is the inactive enantiomer of SLV 319 with 100-fold less affinity for the CB1 receptor. SLV 319 was identified as a potent and selective CB1 receptor antagonist with Ki values of 7.8 and 7,943 nM for CB1 and peripheral cannabinoid (CB2) receptors, respectively. SLV 319 was found to be less lipophilic and thus more water soluble than other known CB1 receptor ligands [1,2].

In vivo: A previous animal study examined the chronic effects of SLV 319 in hyperinsulinemic Zucker rats to determine their chronic effects on insulinemia. Results showed that R SLV 319 at 10 mg·kg-1·day-1 elicited body weight-independent improvements in insulinemia and glycemia during 10 wk of chronic treatment. Moreover, SLV 319 treatment caused glucose intolerance in CB1 but not SUR1-KO mice [3].

Clinical trial: So far, no clinical study has been conducted.

References:
[1] Lange, J. H.M.,Coolen, H.K.A.C.,van Stuivenberg, H.H., et al. Synthesis, biological properties, and molecular modeling investigations of novel 3,4-diarylpyrazolines as potent and selective CB1 cannabinoid receptor antagonists. Journal of Medicinal Chemistry 47(3), 627-643 (2004).
[2] Lange, J. H.M.,van Stuivenberg, H.H.,Veerman, W., et al. Novel 3,4-diarylpyrazolines as potent cannabinoid CB1 receptor antagonists with lower lipophilicity. Bioorganic & Medicinal Chemistry Letters 15, 4794-4798 (2005).
[3] Lynch CJ, Zhou Q, Shyng SL, Heal DJ, Cheetham SC, Dickinson K, Gregory P, Firnges M, Nordheim U, Goshorn S, Reiche D, Turski L, Antel J. Some cannabinoid receptor ligands and their distomers are direct-acting openers of SUR1 K(ATP) channels. Am J Physiol Endocrinol Metab. 2012 Mar 1;302(5):E540-51.