الصفحة الرئيسية>>Signaling Pathways>> GPCR/G protein>> Cannabinoid Receptor>>(R)-SLV 319

(R)-SLV 319

رقم الكتالوجGC10028

(R) -SLV 319 هو مضاد قوي وانتقائي لمستقبلات القنب 1 (CB1) بقيمة Ki تبلغ 894 نانومتر

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(R)-SLV 319 التركيب الكيميائي

Cas No.: 656827-86-0

الحجم السعر المخزون الكميّة
1mg
112٫00
متوفر
5mg
445٫00
متوفر
10mg
670٫00
متوفر

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Sample solution is provided at 25 µL, 10mM.

Description of (R)-SLV 319

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.

Chemical Properties of (R)-SLV 319

Cas No. 656827-86-0 SDF
Chemical Name 3-(4-chlorophenyl)-N-[(4-chlorophenyl)sulfonyl]-4,5-dihydro-N'-methyl-4R-phenyl-1H-pyrazole-1-carboximidamide
Canonical SMILES C/N=C(\NS(=O)(=O)c1ccc(Cl)cc1)/N1N=C(c2ccc(Cl)cc2)[C@@H](C1)c1ccccc1
Formula C23H20Cl2N4O2S M.Wt 487.4
الذوبان ≤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 of (R)-SLV 319

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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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