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Submit ReviewBX 513 hydrochloride is a selective CCR1 receptor antagonist (Ki values are 0.04, > 10, > 10 and > 10 nM for CCR1, CCR5, CXCR2 and CXCR4 receptors respectively). Inhibits MIP-1α-induced intracellular calcium mobilization (IC50 = 2.5 μM). Also a full inverse agonist at US28, a HCMV-encoded chemokine receptor.
BX 513 hydrochloride is also offered as part of the Tocriscreen Antiviral Library. 了解 Tocris 化合物库的更多信息。
分子量 | 481.46 |
公式 | C28H29ClN2O.HCl |
储存 | Desiccate at +4°C |
纯度 | ≥99% (HPLC) |
CAS Number | 1216540-18-9 |
PubChem ID | 56972186 |
InChI Key | SSZWNUGWOGONQJ-UHFFFAOYSA-N |
Smiles | ClC1=CC=C(C2(O)CCN(CCCC(C4=CC=CC=C4)(C#N)C3=CC=CC=C3)CC2)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 | 48.15 | 100 | |
ethanol | 24.07 | 50 |
以下数据基于产品分子量 481.46。 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 | 2.08 mL | 10.39 mL | 20.77 mL |
5 mM | 0.42 mL | 2.08 mL | 4.15 mL |
10 mM | 0.21 mL | 1.04 mL | 2.08 mL |
50 mM | 0.04 mL | 0.21 mL | 0.42 mL |
参考文献是支持产品生物活性的出版物。
Hesselgesser et al (1998) Identification and characterisation of small molecule functional antagonists of the CCR1 chemokine receptor. J.Biol.Chem. 273 15687 PMID: 9624164
Ng et al (1999) Discovery of a novel non-peptide CCR1 receptor antagonists. J.Med.Chem. 42 4680 PMID: 10579830
Casarosa et al (2003) Identification of the first nonpeptidergic inverse agonist for a constitutively active viral-encoded G-protein-coupled receptor. J.Biol.Chem. 278 5172 PMID: 12456673
If you know of a relevant reference for BX 513 hydrochloride, please let us know.
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Rheumatoid arthritis (RA) is a chronic destructive inflammatory autoimmune disease that results from a breakdown in immune tolerance, for reasons that are as yet unknown. This poster summarizes the pathology of RA and the inflammatory processes involved, as well as describing some of the epigenetic modifications associated with the disease and the potential for targeting these changes in the discovery of new treatments.