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(S)-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。
(S)-SLV 319图片
CAS NO:464213-10-3
包装与价格：
包装价格(元)
1mg电议
5mg电议
10mg电议

产品介绍
(S)-SLV 319 (SLV319) 是一种有效的、选择性的、口服活性的大麻素 CB1 受体拮抗剂，Ki 为 7.8 nM。
Cas No.464213-10-3
别名伊必那班,Ibipinabant|BMS 646256|JD 5001
化学名3-(4-chlorophenyl)-N-[(4-chlorophenyl)sulfonyl]-4,5-dihydro-N'-methyl-4S-phenyl-1H-pyrazole-1-carboximidamide
Canonical SMILESC/N=C(\NS(=O)(=O)c1ccc(Cl)cc1)/N1N=C(c2ccc(Cl)cc2)C(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 7,9 nM for CB1 and peripheral cannabinoid (CB2), respectively

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

It has been reported that central cannabinoid (CB1) receptor antagonists may have potential in the treatment of a variety of diseases including cognitive disorders, neuro-inflammatory disorders, obesity, septic shock, psychosis, addiction, as well as gastrointestinal disorders.

In vitro: Previous study found that (S)-SLV 319 was a potent and selective CB1 receptor antagonist with Ki values of 7.8 and 7,9 nM for CB1 and CB2, respectively. In addition, (S)-SLV 319 was found to be less lipophilic and thus more water soluble than other previously identified ligands of CB1 receptor [1].

In vivo: Previous animal study showed that in rats exposed to an ambient temperature of 22°c, a moderate dose of LPS at 25 - 100 μg/kg could induce a fall in body temperature. Such response was not affected by desensitization of intra-abdominal TRPV1 receptors with resiniferatoxin at 20 μg/kg, by systemic TRPV1 antagonism with capsazepine at 40 mg/kg, or by systemic CB2 receptor antagonism with SR144528 at 1.4 mg/kg. In contrast, CB1 receptor antagonism by SLV319 at 15 mg/kg or rimonabant at 4.6 mg/kg was able to block LPS caused hypothermia [2].

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

References:
[1] J.  H. M. Lange, H. H. van Stuivenberg, W. Veerman, et al. Novel 3,4-diarylpyrazolines as potent cannabinoid CB1 receptor antagonists with lower lipophilicity. Bioorganic & Medicinal Chemistry Letters 15, 4794-4798 (2005).
[2] Steiner AA et al.  The hypothermic response to bacterial lipopolysaccharide critically depends on brain CB1, but not CB2 or TRPV1, receptors. J Physiol. 2011 May 1;589(Pt 9):2415-31.