Org 27569

Discontinued Product

2957 has been discontinued.

View all CB<sub>1</sub> Receptors products.
说明: Potent allosteric modulator of CB1 receptors
化学名: 5-Chloro-3-ethyl-N-[2-[4-(1-piperidinyl)phenyl]ethyl-1H-indole-2-carboxamide
纯度: ≥99% (HPLC)
说明书
引用文献 (2)
评论 (1)
文献 (2)

生物活性 for Org 27569

Org 27569 is a potent CB1 receptor allosteric modulator (pEC50 = 8.24). Significantly increases binding of the CB1 agonist [3H]CP 55.940 (pKb = 5.67) and decreases binding of the CB1 inverse agonist [3H]SR 141716A (pKb = 5.95). Inhibits CB1 receptor antagonist efficacy in vitro (pKb = 7.57).

技术数据 for Org 27569

分子量 409.95
公式 C24H28ClN3O
储存 Store at RT
纯度 ≥99% (HPLC)
CAS Number 868273-06-7
PubChem ID 44828492
InChI Key AHFZDNYNXFMRFQ-UHFFFAOYSA-N
Smiles CCC2=C(C(NCCC3=CC=C(N4CCCCC4)C=C3)=O)NC1=CC=C(Cl)C=C12

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.

参考文献 for Org 27569

参考文献是支持产品生物活性的出版物。

Price et al (2005) Allosteric modulation of the Cannabinoid CB1 receptor. Mol.Pharmacol. 68 1484 PMID: 16113085

Ross (2007) Allosterism and the cannabinoid CB1 receptors: the shape of things to come. Trends Pharmacol.Sci. 28 567 PMID: 18029031

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关键词: Org 27569, Org 27569 supplier, Potent, allosteric, CB1, modulators, cannabinoids, Receptors, Org27569, cb1r, 2957, Tocris Bioscience

2 篇 Org 27569 的引用文献

引用文献是使用了 Tocris 产品的出版物。 Org 27569 的部分引用包括:

Baillie et al (2013) CB(1) receptor allosteric modulators display both agonist and signaling pathway specificity. Mol Pharmacol 83 322 PMID: 23160940

Cawston et al (2013) Real-time characterization of cannabinoid receptor 1 (CB1 ) allosteric modulators reveals novel mechanism of action. Br J Pharmacol 170 893 PMID: 23937487


Org 27569 的评论

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Works as described, very interesting compound..
By Jonathan Fay on 05/30/2019
分析类型: In Vitro
种属: Human
细胞系/组织: COSH-1

Allosteric modulation of radioactive Agonist (CP) and Antagonist (SR) binding by various concentrations of Org 27569 and inhibition of agonist stimulated GTPgS binding.

For a constitutively inactive mutant tested, Org 27569 had enhanced potency and appeared to slow radio-labeled agonist dissociation so much that equilibrium was not achieved during the typical 1 hour incubation, at higher Org concentrations.

PMID: 26100912
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