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Submit ReviewSR 140333 is a potent NK1 receptor antagonist (Ki = 0.74 nM. IC50 = 1.6 nM). Inhibits substance P-invoked calcium mobilization and outward current (IC50 = 1.3 nM); blocks NK1-mediated nitric oxide-dependent vasodilation in vivo.
SR 140333 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 656.12 |
公式 | C37H45Cl3N2O2 |
储存 | Store at -20°C |
纯度 | ≥97% (HPLC) |
CAS Number | 153050-21-6 |
PubChem ID | 108166 |
InChI Key | NQHFSECYQAQZBN-LSYPWIJNSA-M |
Smiles | O=C(N2C[C@@](CC[N+]3(CC5)CCC(C4=CC=CC=C4)5CC3)([C@]6=CC=C(Cl)C(Cl)=C6)CCC2)CC1=CC(OC(C)C)=CC=C1.[Cl-] |
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 | 65.61 | 100 | |
ethanol | 65.61 | 100 |
以下数据基于产品分子量 656.12。 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 | 1.52 mL | 7.62 mL | 15.24 mL |
5 mM | 0.3 mL | 1.52 mL | 3.05 mL |
10 mM | 0.15 mL | 0.76 mL | 1.52 mL |
50 mM | 0.03 mL | 0.15 mL | 0.3 mL |
参考文献是支持产品生物活性的出版物。
Hall and Brain (1994) Inhibition by SR140333 of NK1 tachykinin receptor-evoked, nitric oxide-dependent vasodilation in the hamster cheek pouch microvasculature in vivo. Br.J.Pharmacol. 113 522 PMID: 7530573
Nieuwmeyer et al (2006) Ava[L-Pro9,N-MeLeu10] substance P(7-11) (GR 73632) and Sar9, Met(O2)11 increase distention-induced peristalsis through activation of neurokinin-1 receptors on smooth muscle and interstitial cells of Caj J.Pharmacol.Exp.Ther. 317 439 PMID: 16330493
Oury-Donat et al (1994) SR 140333, a novel, selective, and potent nonpeptide antagonist of the NK1 tachykinin receptor: characterization on the U373MG cell line. J.Neurochem. 62 1399 PMID: 7510780
Emonds-Alt et al (1993) In vitro and in vivo biological activities of SR140333, a novel non-peptide tachykinin NK1 receptor antagonist. Eur.J.Pharmacol. 250 403 PMID: 7509286
If you know of a relevant reference for SR 140333, please let us know.
关键词: SR 140333, SR 140333 supplier, SR140333, neurokinin1, nk1, tachykinins, receptor, antagonists, potent, NK1, Receptor, 4012, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 SR 140333 的部分引用包括:
Xinzhong et al (2019) A Mast-Cell-Specific Receptor Mediates Neurogenic Inflammation and Pain. Neuron 101 412-420.e3 PMID: 30686732
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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.
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