>>Signaling Pathways>> GPCR/G protein>> Cannabinoid Receptor>>(S)-SLV 319

(S)-SLV 319 (Synonyms: Ibipinabant|BMS 646256|JD 5001)

Catalog No.GC10753

(S)-SLV 319(SLV319)는 7.8 nM의 Ki를 갖는 칸나비노이드 CB1 수용체의 강력하고 선택적이며 경구 활성 길항제입니다.

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(S)-SLV 319 Chemical Structure

Cas No.: 464213-10-3

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US$114.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

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.

Chemical Properties

Cas No. 464213-10-3 SDF
Synonyms Ibipinabant|BMS 646256|JD 5001
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
Formula C23H20Cl2N4O2S M.Wt 487.4
Solubility ≤30mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.0517 mL 10.2585 mL 20.517 mL
5 mM 0.4103 mL 2.0517 mL 4.1034 mL
10 mM 0.2052 mL 1.0259 mL 2.0517 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 33 reference(s) in Google Scholar.)

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