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Submit ReviewIT1t dihydrochloride
说明： Potent CXCR4 antagonist
化学名： N,N'-Dicyclohexylcarbamimidothioic acid (5,6-dihydro-6,6-dimethylimidazo[2,1-b]thiazol-3-yl)methyl ester dihydrochloride
纯度： ≥99% (HPLC)
生物活性 for IT1t dihydrochloride
IT1t dihydrochloride is a potent CXCR4 antagonist (IC50 = 1.1 nM in calcium mobilization assays). Orally available. Blocks interaction with the HIV envelope protein, gp120 (IC50 = 7 nM, inhibition of X4-tropic HIV-1IIIB attachment).
技术数据 for IT1t dihydrochloride
| 分子量 | 479.57 |
| 公式 | C21H34N4S2.2HCl |
| 储存 | Store at +4°C |
| 纯度 | ≥99% (HPLC) |
| CAS Number | 1092776-63-0 |
| PubChem ID | 25178351 |
| InChI Key | HFXJOXOIINQOEB-UHFFFAOYSA-N |
| Smiles | CC1(C)CN(C(CS/C(NC4CCCCC4)=N/C3CCCCC3)=CS2)C2=N1.Cl.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.
溶解性数据 for IT1t dihydrochloride
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 4.8 | 10 | |
| water | 47.96 | 100 |
制备储备液 for IT1t dihydrochloride
以下数据基于产品分子量 479.57。 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 | 2.09 mL | 10.43 mL | 20.85 mL |
| 5 mM | 0.42 mL | 2.09 mL | 4.17 mL |
| 10 mM | 0.21 mL | 1.04 mL | 2.09 mL |
| 50 mM | 0.04 mL | 0.21 mL | 0.42 mL |
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产品说明书 for IT1t dihydrochloride
参考文献 for IT1t dihydrochloride
参考文献是支持产品生物活性的出版物。
Thoma et al (2008) Orally bioavailable isothioureas block function of the chemokine receptor CXCR4 in vitro and in vivo. J.Med.Chem. 51 7915 PMID: 19053768
If you know of a relevant reference for IT1t dihydrochloride, please let us know.
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关键词: IT1t dihydrochloride, IT1t dihydrochloride supplier, CXCR4, antagonists, HIV, envelope, protein, gp120, chemokines, receptors, type, 4, Chemokine, CXC, Receptors, 4596, Tocris Bioscience
7 篇 IT1t dihydrochloride 的引用文献
引用文献是使用了 Tocris 产品的出版物。 IT1t dihydrochloride 的部分引用包括：
Mathias et al (2021) Cell surface thermal proteome profiling tracks perturbations and drug targets on the plasma membrane. Nat Methods 18 84-91 PMID: 33398190
Smith et al (2019) Control of TLR7-mediated type I IFN signaling in pDCs through CXCR4 engagement-A new target for lupus treatment. Sci Adv 5 eaav9019 PMID: 31309143
Yung-Chi et al (2019) Characterization, Dynamics, and Mechanism of CXCR4 Antagonists on a Constitutively Active Mutant. Cell Chem Biol 26 662-673.e7 PMID: 30827936
Martin J et al (2020) Kinetic Analysis of the Early Signaling Steps of the Human Chemokine Receptor CXCR4. Mol Pharmacol 98 72-87 PMID: 32474443
Ludger et al (2020) Microtiter plate-based antibody-competition assay to determine binding affinities and plasma/blood stability of CXCR4 ligands. Sci Rep 10 16036 PMID: 32994431
Martine J et al (2020) Monitoring Allosteric Interactions with CXCR4 Using NanoBiT Conjugated Nanobodies. Cell Chem Biol 27 1250-1261.e5 PMID: 32610042
White et al (2020) CRISPR-Mediated Protein Tagging with Nanoluciferase to Investigate Native Chemokine Receptor Function and Conformational Changes. Cell Chem Bio PMID: 32053779
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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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