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Submit Review2-Cl-IB-MECA is a high affinity and extremely selective A3 adenosine receptor agonist (Ki = 0.33 nM). Displays 2500- and 1400-fold selectivity over A1 and A2A receptors respectively. Exhibits high selectivity over the Na+-independent adenosine transporter.
Sold with the permission of the NIH, US Patent 08/091,109
分子量 | 544.74 |
公式 | C18H18ClIN6O4 |
储存 | Desiccate at +4°C |
纯度 | ≥98% (HPLC) |
CAS Number | 163042-96-4 |
PubChem ID | 3035850 |
InChI Key | IPSYPUKKXMNCNQ-PFHKOEEOSA-N |
Smiles | O[C@@H]1[C@@H]([C@](NC)=O)O[C@@H](N(C=N4)C2=C4C(NCC3=CC(I)=CC=C3)=NC(Cl)=N2)[C@@H]1O |
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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 100 |
以下数据基于产品分子量 544.74。 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 | 1.84 mL | 9.18 mL | 18.36 mL |
5 mM | 0.37 mL | 1.84 mL | 3.67 mL |
10 mM | 0.18 mL | 0.92 mL | 1.84 mL |
50 mM | 0.04 mL | 0.18 mL | 0.37 mL |
参考文献是支持产品生物活性的出版物。
Jacobson (1998) Adenosine A3 receptors: novel ligands and paradoxical effects. TiPS 19 184 PMID: 9652191
Kim et al (1994) 2-Substitution of N6-benzyladenosine-5'-uronamides enhances selectivity for A3 adenosine receptors. J.Med.Chem. 37 3614 PMID: 7932588
Schaick et al (1996) Hemodynamic effects of histamine release elicited by the selective adenosine A3 receptor agonist 2-Cl-IB-MECA in conscious rats. Eur.J.Pharmacol. 308 311 PMID: 8858305
If you know of a relevant reference for 2-Cl-IB-MECA, please let us know.
关键词: 2-Cl-IB-MECA, 2-Cl-IB-MECA supplier, selective, A3, agonists, Receptors, adenosines, 2ClIBMECA, Adenosine, 1104, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 2-Cl-IB-MECA 的部分引用包括:
Angelantonio et al (2015) Basal adenosine modulates the functional properties of AMPA receptors in mouse hippocampal neurons through the activation of A1R A2AR and A3R. Sci Rep 9 409 PMID: 26528137
Ren et al (2015) An adenosine A3 receptor agonist inhibits DSS-induced colitis in mice through modulation of the NF-κB signaling pathway. J Neurosci 5 9047 PMID: 25762375
Kan et al (2012) Imiquimod suppresses propagation of herpes simplex virus 1 by upregulation of cystatin A via the adenosine receptor A1 pathway. J Virol 86 10338 PMID: 22787201
Montinaro et al (2012) Adoptive immunotherapy with Cl-IB-MECA-treated CD8+ T cells reduces melanoma growth in mice. PLoS One 7 e45401 PMID: 23028986
Rosito et al (2012) CXCL16 orchestrates adenosine A3 receptor and MCP-1/CCL2 activity to protect neurons from excitotoxic cell death in the CNS. Neoplasia 32 3154 PMID: 22378888
Morello et al (2011) NK1.1 cells and CD8 T cells mediate the antitumor activity of Cl-IB-MECA in a mouse melanoma model. Am J Cancer Res 13 365 PMID: 21472141
Corriden et al (2013) Adenosine-A3 receptors in neutrophil microdomains promote the formation of bacteria-tethering cytonemes. Biochim Biophys Acta 14 726 PMID: 23817552
Bhanu et al (2008) Inhibition of erythroblast growth and fetal hemoglobin production by ribofuranose-substituted adenosine derivatives. J Pharmacol Exp Ther 1782 504 PMID: 18586086
Iannone et al (2014) Adenosine limits the therapeutic effectiveness of anti-CTLA4 mAb in a mouse melanoma model. EMBO Rep 4 172 PMID: 24660106
Vincenzi et al (2013) Pulsed electromagnetic fields increased the anti-inflammatory effect of A2A and A3 adenosine receptors in human T/C-28a2 chondrocytes and hFOB 1.19 osteoblasts. PLoS One 8 e65561 PMID: 23741498
Jinka et al (2011) Season primes the brain in an arctic hibernator to facilitate entrance into torpor mediated by adenosine A(1) receptors. J Neurosci 31 10752 PMID: 21795527
Man et al (2003) Alteration of the purinergic modulation of enteric neurotransmission in the mouse ileum during chronic intestinal inflammation. Br J Pharmacol 139 172 PMID: 12746236
Germack and Dickenson (2004) Characterization of ERK1/2 signalling pathways induced by adenosine receptor subtypes in newborn rat cardiomyocytes. Br J Pharmacol 141 329 PMID: 14751870
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