| CAS NO: | 464213-10-3 |
| 包装 | 价格(元) |
| 1mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 487.4 |
| Cas No. | 464213-10-3 |
| Formula | C23H20Cl2N4O2S |
| Synonyms | Ibipinabant|BMS 646256|JD 5001 |
| Solubility | ≤30mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide |
| Chemical Name | 3-(4-chlorophenyl)-N-[(4-chlorophenyl)sulfonyl]-4,5-dihydro-N'-methyl-4S-phenyl-1H-pyrazole-1-carboximidamide |
| Canonical SMILES | C/N=C(\NS(=O)(=O)c1ccc(Cl)cc1)/N1N=C(c2ccc(Cl)cc2)C(C1)c1ccccc1 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
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.
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