GP 1a

Cat. No. 2764 6 篇引用文献提交评论说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）

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说明： CB₂ receptor inverse agonist

化学名： N-(Piperidin-1-yl)-1-(2,4-dichlorophenyl)-1,4-dihydro-6-methylindeno[1,2-c]pyrazole-3-carboxamide

纯度： ≥99% (HPLC)

引用文献 (6)

文献 (1)

生物活性技术数据溶解性计算器说明书参考文献

生物活性 for GP 1a

GP 1a is a CB₂ receptor inverse agonist (pEC₅₀ = 7.1), shown in cAMP, GTPγS and β-arrestin recruitment assays. Demonstrates approximately 30-fold selectivity for CB₂ receptors over CB₁ receptors. Increases P-ERK1/2 expression in HL-60 cells in vitro.

技术数据 for GP 1a

分子量	441.35
公式	C₂₃H₂₂Cl₂N₄O
储存	Store at RT
纯度	≥99% (HPLC)
CAS Number	511532-96-0
PubChem ID	10252734
InChI Key	FNOMTMVRTBHRET-UHFFFAOYSA-N
Smiles	CC1=CC2=C(C=C1)C1=C(C2)C(=NN1C1=CC=C(Cl)C=C1Cl)C(=O)NN1CCCCC1

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 GP 1a

	溶剂	最高浓度 mg/mL	最高浓度 mM
溶解性
	DMSO	44.13	100
	ethanol	44.13	100

制备储备液 for GP 1a

以下数据基于产品分子量 441.35。 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.

浓度/溶剂体积/质量	1 mg	5 mg	10 mg
1 mM	2.27 mL	11.33 mL	22.66 mL
5 mM	0.45 mL	2.27 mL	4.53 mL
10 mM	0.23 mL	1.13 mL	2.27 mL
50 mM	0.05 mL	0.23 mL	0.45 mL

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产品说明书 for GP 1a

分析证书/产品说明书

化学品安全技术说明书

参考文献 for GP 1a

参考文献是支持产品生物活性的出版物。

Murineddu et al (2006) Tricyclic pyrazoles. 4. Synthesis and biological evaluation of analogues of the robust and selective CB2 cannabinoid ligand 1-(2',4'-dichlorophenyl)-6-methyl-N-piperidin-1-yl-1,4-dihydroindeno[1,2-c]pyrazole-3-carboxam J.Med.Chem. 49 7502 PMID: 17149879

Tschop et al (2009) The cannabinoid receptor 2 is critical for the host response to sepsis. J.Immunol. 183 499 PMID: 19525393

Soethoudt et al (2017) Cannabinoid CB₂ receptor ligand profiling reveals biased signalling and off-target activity. Nat.Commun. 8 13958 PMID: 28045021

If you know of a relevant reference for GP 1a, please let us know.

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关键词: GP 1a, GP 1a supplier, selective, CB2, receptor, agonists, cannabinoid, receptors, GP1a, cb2r, Receptors, 2764, Tocris Bioscience

6 篇 GP 1a 的引用文献

引用文献是使用了 Tocris 产品的出版物。 GP 1a 的部分引用包括：

Sheng et al (2019) Antiallodynic Effects of Cannabinoid Receptor 2 (CB2R) Agonists on Retrovirus Infection-Induced Neuropathic Pain. Pain Res Manag 2019 1260353 PMID: 31354896

Soethoudt et al (2017) Cannabinoid CB₂ receptor ligand profiling reveals biased signalling and off-target activity. Nat.Commun. PMID: 28045021

Newton and Klein (2012) Cannabinoid 2 (CB2) receptor involvement in the down-regulation but not up-regulation of serum IgE levels in immunized mice. PLoS One 7 591 PMID: 22552780

Robert et al (2012) The anti-apoptotic Bcl-B protein inhibits BECN1-dependent autophagic cell death. Int J Clin Exp Pathol 8 637 PMID: 22498477

Zhang et al (2015) CB2R orchestrates fibrogenesis through regulation of inflammatory response during the repair of skeletal muscle contusion. Am J Physiol Regul Integr Comp Physiol 8 3491 PMID: 26097533

Wang et al (2013) Activation of cannabinoid receptor 2 inhibits experimental cystitis. J Neuroimmune Pharmacol 304 R846 PMID: 23515618

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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

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Cannabinoid Receptor Ligands Scientific Review

Written by Roger Pertwee, this review discusses compounds which affect the activity of the endocannabinoid system, focusing particularly on ligands that are most widely used as experimental tools and denotes compounds available from Tocris.