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Submit ReviewPD 176252 is a non-peptide gastrin-releasing peptide receptor (GRP-R, BB2) and neuromedin B receptor (NMB-R, BB1) antagonist (Ki values are 0.17 and 1.0 nM for BB1 and BB2 respectively). Inhibits proliferation of rat C6 glioma cells (IC50 = 2 μM) and inhibits NCI-H1299 xenograft proliferation in nude mice (IC50 = 5 μM).
分子量 | 584.67 |
公式 | C32H36N6O5 |
储存 | Store at +4°C |
纯度 | ≥98% (HPLC) |
CAS Number | 204067-01-6 |
PubChem ID | 9829828 |
InChI Key | NNFUWNLENRUDHR-HKBQPEDESA-N |
Smiles | O=C(NC3=CC=C([N+]([O-])=O)C=C3)N[C@@](C)(CC5=CNC4=CC=CC=C45)C(NCC1(C2=CC=C(OC)C=N2)CCCCC1)=O |
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 | 58.47 | 100 |
以下数据基于产品分子量 584.67。 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 | 1.71 mL | 8.55 mL | 17.1 mL |
5 mM | 0.34 mL | 1.71 mL | 3.42 mL |
10 mM | 0.17 mL | 0.86 mL | 1.71 mL |
50 mM | 0.03 mL | 0.17 mL | 0.34 mL |
参考文献是支持产品生物活性的出版物。
Ashwood et al (1998) PD 176252 - the first high affinity non-peptide gastrin-releasing peptide (BB2) receptor antagonist Bioorg.Med.Chem.Lett. 8 2589 PMID: 9873586
Moody et al (2000) Nonpeptide neuromedin B receptor antagonists inhibit the proliferation of C6 cells Eur.J.Pharmacol. 409 133 PMID: 11104826
Moody et al (2003) Nonpeptide gastrin releasing peptide receptor antagonists inhibit the proliferation of lung cancer cells Eur.J.Pharmacol. 474 21 PMID: 12909192
Schepetkin et al (2011) Gastrin-releasing peptide/neuromedin B receptor antagonists pD176252, PD168368, and related analogs are potent agonists of human formyl-peptide receptors. Mol.Pharmacol. 79 77 PMID: 20943772
If you know of a relevant reference for PD 176252, please let us know.
关键词: PD 176252, PD 176252 supplier, GRP, BB2, NMB, BB1, receptor, antagonists, GRP-Preferring, Receptors, Gastrin-Releasing, Peptide-Preferring, NMB-Preferring, Neuromedin, B-Preferring, Bombesin, PD176252, 2602, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 PD 176252 的部分引用包括:
González et al (2009) Characterization of putative GRP- and NMB-receptor antagonist's interaction with human receptors. Peptides 30 1473 PMID: 19463875
Atkins et al (2010) Circadian integration of glutamatergic signals by little SAAS in novel suprachiasmatic circuits. PLoS One 5 e12612 PMID: 20830308
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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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Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.