SB 366791

Pricing Availability   Qty
说明: Potent and selective TRPV1 competitive antagonist
化学名: 4'-Chloro-3-methoxycinnamanilide
纯度: ≥99% (HPLC)
说明书
引用文献 (14)
评论

生物活性 for SB 366791

SB 366791 is a potent, selective and competitive vanilloid TRPV1 receptor antagonist (pA2 = 7.71 at hVR1); antagonizes hTRPV1 receptors activated by agonists, noxious heat, but not protons. Displays selectivity over a wide range of receptors and systems including CB1 and CB2 receptors, voltage-gated Ca2+ channels and the hyperpolarization-activated current (Ih).

许可信息

Sold for research purposes under agreement from GlaxoSmithKline

化合物库 for SB 366791

SB 366791 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。

技术数据 for SB 366791

分子量 287.75
公式 C16H14ClNO2
储存 Store at RT
纯度 ≥99% (HPLC)
CAS Number 472981-92-3
PubChem ID 667594
InChI Key RYAMDQKWNKKFHD-JXMROGBWSA-N
Smiles COC1=CC=CC(NC(=O)\C=C\C2=CC=C(Cl)C=C2)=C1

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for SB 366791

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
ethanol 2.88 10
DMSO 28.77 100

制备储备液 for SB 366791

以下数据基于产品分子量 287.75。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 1 mg 5 mg 10 mg
1 mM 3.48 mL 17.38 mL 34.75 mL
5 mM 0.7 mL 3.48 mL 6.95 mL
10 mM 0.35 mL 1.74 mL 3.48 mL
50 mM 0.07 mL 0.35 mL 0.7 mL

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参考文献 for SB 366791

参考文献是支持产品生物活性的出版物。

Fowler et al (2003) Inhibition of C6 glioma cell proliferation by anandamide, 1-arachidonylglycerol, and by a water soluble phosphate ester of anandamide: variability in response and involvement of arachidonic acid. Biochem.Pharmacol. 66 757 PMID: 12948856

Gavva et al (2005) Proton activation does not alter antagonist interaction with the capsaicin-binding pocket of TRPV1. Mol.Pharmacol. 68 1524 PMID: 16135784

Gunthorpe et al (2004) Identification and characterisation of SB-366791, a potent and selective vanilloid receptor (VR1/TRPV1) antagonist. Neuropharmacology 46 133 PMID: 14654105


If you know of a relevant reference for SB 366791, please let us know.

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关键词: SB 366791, SB 366791 supplier, Potent, selective, competitive, TRPV1, VR1, antagonists, Vanillioids, Receptors, TRPV, Channels, Transient, Receptor, Potential, SB366791, GlaxoSmithKline, GSK, 1615, Tocris Bioscience

14 篇 SB 366791 的引用文献

引用文献是使用了 Tocris 产品的出版物。 SB 366791 的部分引用包括:

Wang et al (2014) Innervation of enteric mast cells by primary spinal afferents in guinea pig and human small intestine. Am J Physiol Gastrointest Liver Physiol 307 G719 PMID: 25147231

Nguyen et al (2014) Transient receptor potential vanilloid type 1 channel may modulate opioid reward. Neuropsychopharmacology 39 2414 PMID: 24732880

Hazari et al (2011) TRPA1 and sympathetic activation contribute to increased risk of triggered cardiac arrhythmias in hypertensive rats exposed to diesel exhaust. Environ Health Perspect 119 951 PMID: 21377951

Price et al (2004) Cannabinoid receptor-independent actions of the aminoalkylindole WIN 55,212-2 on trigeminal sensory neurons. Br J Pharmacol 142 257 PMID: 15155534

Schuelert et al (2010) Paradoxical effects of the cannabinoid CB2 receptor agonist GW405833 on rat osteoarthritic knee joint pain. Osteoarthritis Cartilage 18 1536 PMID: 20863899

Gavva et al (2005) AMG 9810 [(E)-3-(4-t-butylphenyl)-N-(2,3-dihydrobenzo[b][1,4] dioxin-6-yl)acrylamide], a novel vanilloid receptor 1 (TRPV1) antagonist with antihyperalgesic properties. J Pharmacol Exp Ther 313 474 PMID: 15615864

Li et al (2015) The Cancer Chemotherapeutic PacT. Increases Human and Rodent Sensory Neuron Responses to TRPV1 by Activation of TLR4. J Neurosci 35 13487 PMID: 26424893

Yuan and Burrell (2010) Endocannabinoid-dependent LTD in a nociceptive synapse requires activation of a presynaptic TRPV-like receptor. J Neurophysiol 104 2766 PMID: 20884761

Westlund et al (2010) Impact of central and peripheral TRPV1 and ROS levels on proinflammatory mediators and nociceptive behavior. J Biol Chem 6 46 PMID: 20691059

Graham et al (2013) Epidermal keratinocyte polarity and motility require Ca2+ influx through TRPV1. J Cell Sci 126 4602 PMID: 23943873

Casarotto et al (2012) Opposing roles for cannabinoid receptor type-1 (CB1) and transient receptor potential vanilloid type-1 channel (TRPV1) on the modulation of panic-like responses in rats. Am J Physiol Renal Physiol 37 478 PMID: 21937980

Shabir et al (2013) Functional expression of purinergic P2 receptors and transient receptor potential channels by the human urothelium. Mol Pain 305 F396 PMID: 23720349

Alvarez-Berdugo et al (2014) Pharmacodynamics of TRPV1 agonists in a bioassay using human PC-3 cells. ScientificWorldJournal 2014 184526 PMID: 24688365

Ambrosino et al (2013) Activation and desensitization of TRPV1 channels in sensory neurons by the PPARα agonist palmitoylethanolamide. Br J Pharmacol 168 1430 PMID: 23083124


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