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Submit ReviewBGC 20-1531 hydrochloride is a high affinity and selective EP4 antagonist (Ki = 3 nM). Exhibits >2500-fold selectivity for EP4 over EP2 and EP3. Also selective over a range of other prostanoid receptors, ion channels, transporters and enzymes. Inhibits PGE2-induced vasodilation of middle cerebral and meningeal arteries in vitro, and carotid blood flow in vivo. Orally bioavailable.
BGC 20-1531 hydrochloride 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 | 529 |
公式 | C26H24N2O6S.HCl |
储存 | Desiccate at RT |
纯度 | ≥98% (HPLC) |
CAS Number | 1962928-26-2 |
PubChem ID | 121513858 |
InChI Key | ZSHYZCXOFPPBMH-UHFFFAOYSA-N |
Smiles | CC(OC(C(NS(C4=CC=CC=C4C)(=O)=O)=O)=C3)=C3COC(C=C2)=CC=C2C1=NC=C(OC)C=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 | 49.25 | 100 |
以下数据基于产品分子量 529。 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 | 1.89 mL | 9.45 mL | 18.9 mL |
5 mM | 0.38 mL | 1.89 mL | 3.78 mL |
10 mM | 0.19 mL | 0.95 mL | 1.89 mL |
50 mM | 0.04 mL | 0.19 mL | 0.38 mL |
参考文献是支持产品生物活性的出版物。
Sutton et al (2014) From virtual to clinical: The discovery of PGN-1531, a novel antagonist of the prostanoid EP4 receptor. Bioorg.Med.Chem.Lett. 24 2212 PMID: 24703233
If you know of a relevant reference for BGC 20-1531 hydrochloride, please let us know.
关键词: BGC 20-1531 hydrochloride, BGC 20-1531 hydrochloride supplier, BGC20-1531, hydrochloride, PGN1531, high, affinity, selective, EP4, antagonists, orally, bioavailable, active, PGN, 1531, Prostanoid, Receptors, 5327, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 BGC 20-1531 hydrochloride 的部分引用包括:
David et al (2022) Tumor-Derived Lysophosphatidic Acid Blunts Protective Type I Interferon Responses in Ovarian Cancer. Cancer Discov 12 1904-1921 PMID: 35552618
Perkins et al (2018) Autocrine-paracrine prostaglandin E2 signaling restricts TLR4 internalization and TRIF signaling. Nat.Immunol. 19 1309 PMID: 30397349
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