(R)-SLV 319
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
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.
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 487.4 |
Cas No. | 656827-86-0 |
Formula | C23H20Cl2N4O2S |
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-4R-phenyl-1H-pyrazole-1-carboximidamide |
SDF | Download SDF |
Canonical SMILES | C/N=C(\NS(=O)(=O)c1ccc(Cl)cc1)/N1N=C(c2ccc(Cl)cc2)[C@@H](C1)c1ccccc1 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 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。 |