普乐沙福八盐酸盐(AMD3100 8HCl)

高选择性CXCR4拮抗剂
  • ≥99%
有货

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货号 (SKU) 包装规格 是否现货 价格 数量
P129846-5mg
5mg 现货 Stock Image
P129846-10mg
10mg 现货 Stock Image
P129846-25mg
25mg 现货 Stock Image
P129846-50mg
50mg 现货 Stock Image
P129846-250mg
250mg 现货 Stock Image

基本描述

别名 普乐沙福八盐酸盐 | 1,4-双[(1,4,8,11-四氮杂环十四烷-1-基)甲基]苯八盐酸盐 | 1,1'-[1,4-亚苯基双(亚甲基)]双-1,4,8,11-四氮杂环十四烷八盐酸盐
英文别名 155148-31-5 (HCl) | Plerixafor hydrochloride | AMD3100 octahydrochloride hydrate | DTXSID20935148 | 1,1'-[1,4-Phenylenebis-(methylene)]-bis-(1,4,8,11-tetraazacyclotetradecane) octahydrochloride | Sid 791 | PLERIXAFOR OCTAHYDROCHLORIDE [WHO-DD] | AMD 3100
规格或纯度 ≥99%
英文名称 Plerixafor 8HCl (AMD3100 8HCl)
生化机理 AMD3100 octahydrochloride 是一种选择性双环酰胺衍生物,通过阻断 CXCR4 趋化因子受体发挥干细胞动员剂的作用。研究表明,AMD3100 八盐酸盐通过阻断 CXCR4 受体,使干细胞迅速从骨髓中转移出来。由于 CXCR4 受体负责调节耐化疗黑色素瘤细胞的转移,因此阻断该受体可能会减少黑色素瘤细胞的转移。此外,研究表明,AMD3100 八盐酸盐可以通过阻断病毒进入细胞来抑制人体免疫缺陷病毒在体外的复制。此外,AMD3100 八盐酸盐还能减少人类 CD4+ T 细胞的数量。Plerixafor(盐酸盐)是一种大环化合物,是 CXCR4 与其配体 SDF- 1(CXCL12)结合的不可逆拮抗剂。它能抑制 HIV 感染,IC50 值为 1-10 纳克/毫升,对 CXCR4- t 具有选择性。
储存温度 -20°C储存
运输条件 超低温冰袋运输
备注 如果有可能,您尽量在使用的当天配置溶液,并在当天使用完它。但是,如果您需要预先配制储备溶液,我们建议您将溶液等份保存在-20°C的密封小瓶中。通常,它们最多可以使用一个月。在使用前和打开样品瓶之前,我们建议您让您的产品在室温下平衡至少1小时。需要更多关于溶解度,用法和处理的建议吗?请访问我们的常见问题(FAQ)页面以获取更多详细信息。
产品介绍

Plerixafor 8HCl (AMD3100 8HCl)是Plerixafor的盐酸盐,是CXCR4趋化因子受体拮抗剂,作用于CXCR4和CXCL12调节的趋化性, IC50分别为44 nM和5.7 nM。A specific CXCR4 antagonist.

Plerixafor 8HCl (AMD3100 8HCl) is the hydrochloride of Plerixafor, a chemokine receptor antagonist for CXCR4 and CXCL12-mediated chemotaxis with IC50 of 44 nM and 5.7 nM, respectively.
A specific CXCR4 antagonist.

关联靶点(人)

KCNH2 Tclin HERG (29587 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CXCR4 Tclin C-X-C chemokine receptor type 4 (3338 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CCR3 Tchem C-C chemokine receptor type 3 (1666 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CCR5 Tclin C-C chemokine receptor type 5 (5640 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MT4 (17854 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

关联靶点(其它种属)

Mus musculus (284745 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Human immunodeficiency virus 1 (70413 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

作用机制

作用机制 Action Type target ID Target Name Target Type Target Organism Binding Site Name 参考文献

名称和识别符

分子类型 小分子
IUPAC Name 1-[[4-(1,4,8,11-tetrazacyclotetradec-1-ylmethyl)phenyl]methyl]-1,4,8,11-tetrazacyclotetradecane;octahydrochloride
INCHI InChI=1S/C28H54N8.8ClH/c1-9-29-15-17-31-13-3-21-35(23-19-33-11-1)25-27-5-7-28(8-6-27)26-36-22-4-14-32-18-16-30-10-2-12-34-20-24-36;;;;;;;;/h5-8,29-34H,1-4,9-26H2;8*1H
InChi Key UEUPDYPUTTUXLJ-UHFFFAOYSA-N
Canonical SMILES C1CNCCNCCCN(CCNC1)CC2=CC=C(C=C2)CN3CCCNCCNCCCNCC3.Cl.Cl.Cl.Cl.Cl.Cl.Cl.Cl
Isomeric SMILES C1CNCCNCCCN(CCNC1)CC2=CC=C(C=C2)CN3CCCNCCNCCCNCC3.Cl.Cl.Cl.Cl.Cl.Cl.Cl.Cl
PubChem CID 65014
分子量 794.47

化学和物理性质

溶解性 溶解度 H2O: ≥10 mg/mL, clear;DMSO:Insoluble;Ethanol:Insoluble
敏感性 对热敏感
熔点 245 °C
分子量 794.500 g/mol
XLogP3
氢键供体数Hydrogen Bond Donor Count 14
氢键受体数Hydrogen Bond Acceptor Count 8
可旋转键计数Rotatable Bond Count 4
精确质量Exact Mass 794.255 Da
单同位素质量Monoisotopic Mass 790.261 Da
拓扑极表面积Topological Polar Surface Area 78.700 Ų
重原子数Heavy Atom Count 44
形式电荷Formal Charge 0
复杂度Complexity 456.000
同位素原子数Isotope Atom Count 0
定义的原子立体中心计数Defined Atom Stereocenter Count 0
未定义的原子立体中心计数Undefined Atom Stereocenter Count 0
定义的键立体中心计数Defined Bond Stereocenter Count 0
未定义的键立体中心计数Undefined Bond Stereocenter Count 0
所有立体化学键的总数The total count of all stereochemical bonds 0
共价键合单元计数Covalently-Bonded Unit Count 9

安全和危险性(GHS)

技术规格说明书

Carbon by Elemental Analysis 41.4-42.8(%)
Purity(HPLC) 99-100(%)
Nitrogen by Elemental Analysis 13.5-14.6(%)
Appearance(P129846) White to off-white solid
NMR spectrum Conforms to Structure

质检证书(CoA,COO,BSE/TSE 和分析图谱)

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找到4个结果

批号(Lot Number) 证书类型 日期 货号
L2117239 分析证书 25-07-10 P129846
L2117240 分析证书 25-07-10 P129846
L2117241 分析证书 25-07-10 P129846
F1510057 分析证书 23-01-26 P129846

此产品的引用文献

1. Yuqian Chen, Jin Liu, Qianqian Zhang, Limin Chai, Huan Chen, Danyang Li, Yan Wang, Yuanjie Qiu, Nirui Shen, Jia Zhang, Qingting Wang, Jian Wang, Xinming Xie, Shaojun Li, Manxiang Li.  (2024)  Activation of CaMKII/HDAC4 by SDF1 contributes to pulmonary arterial hypertension via stabilization Runx2.  EUROPEAN JOURNAL OF PHARMACOLOGY,  970  (176483).  [PMID:38479721] [10.1016/j.ejphar.2024.176483]

参考文献

1. Lu W et al..  (2019)  AMD3100 Attenuates Post-Traumatic Osteoarthritis by Maintaining Transforming Growth Factor-ß1-Induced Expression of Tissue Inhibitor of Metalloproteinase-3 via the Phosphatidylinositol 3-Kinase/Akt Pathway..  Front Pharmacol,  10  (1554).  [PMID:32038242]
2. Li B et al..  (2018)  AMD3100 Augments the Efficacy of Mesothelin-Targeted, Immune-Activating VIC-008 in Mesothelioma by Modulating Intratumoral Immunosuppression..  Cancer Immunol Res,  (5): (539-551).  [PMID:29511032]
3. Negro S et al..  (2019)  An Agonist of the CXCR4 Receptor Strongly Promotes Regeneration of Degenerated Motor Axon Terminals..  Cells,  (10): [PMID:31575088]
4. Ito N et al..  (2020)  Biphasic MIF and SDF1 expression during podocyte injury promote CD44-mediated glomerular parietal cell migration in focal segmental glomerulosclerosis..  Am J Physiol Renal Physiol,  318  (3): (F741-F753).  [PMID:32068458]
5. Lu W et al..  (2016)  CXCL12/CXCR4 Axis Regulates Aggrecanase Activation and Cartilage Degradation in a Post-Traumatic Osteoarthritis Rat Model..  Int J Mol Sci,  17  (10): [PMID:27690009]
6. Du LL & Liu P.  (2016)  CXCL12/CXCR4 axis regulates neovascularization and lymphangiogenesis in sutured corneas in mice..  Mol Med Rep,  13  (6): (4987-94).  [PMID:27121088]
7. Zeng Y et al..  (2019)  Dual blockade of CXCL12-CXCR4 and PD-1-PD-L1 pathways prolongs survival of ovarian tumor-bearing mice by prevention of immunosuppression in the tumor microenvironment..  FASEB J,  33  (5): (6596-6608).  [PMID:30802149]
8. Zhou H et al..  (2015)  Effects of Exendin-4 on bone marrow mesenchymal stem cell proliferation, migration and apoptosis in vitro..  Sci Rep,  (12898).  [PMID:26250571]
9. Li B et al..  (2018)  Epigenetic Regulation of CXCL12 Plays a Critical Role in Mediating Tumor Progression and the Immune Response In Osteosarcoma..  Cancer Res,  78  (14): (3938-3953).  [PMID:29735547]
10. Zhou H et al..  (2015)  Exendin-4 enhances the migration of adipose-derived stem cells to neonatal rat ventricular cardiomyocyte-derived conditioned medium via the phosphoinositide\xa03-kinase/Akt-stromal cell-derived factor-1a/CXC chemokine receptor 4 pathway..  Mol Med Rep,  11  (6): (4063-72).  [PMID:25625935]
11. Hirata K et al..  (2019)  Exocrine tissue-driven TFF2 prevents apoptotic cell death of endocrine lineage during pancreas organogenesis..  Sci Rep,  (1636).  [PMID:30733468]
12. Lin YN et al..  (2022)  Impaired CXCL12 signaling contributes to resistance of pancreatic cancer subpopulations to T cell-mediated cytotoxicity..  Oncoimmunology,  11  (2027136).  [PMID:35127250]
13. Qin H et al..  (2021)  Inhibition of SDF-1/CXCR4 Axis to Alleviate Abnormal Bone Formation and Angiogenesis Could Improve the Subchondral Bone Microenvironment in Osteoarthritis..  Biomed Res Int,  2021  (8852574).  [PMID:34136574]
14. Iseki M et al..  (2017)  Muse Cells, Nontumorigenic Pluripotent-Like Stem Cells, Have Liver Regeneration Capacity Through Specific Homing and Cell Replacement in a Mouse Model of Liver Fibrosis..  Cell Transplant,  26  (5): (821-840).  [PMID:27938474]
15. Qin HJ et al..  (2019)  SDF-1/CXCR4 axis coordinates crosstalk between subchondral bone and articular cartilage in osteoarthritis pathogenesis..  Bone,  125  (140-150).  [PMID:31108241]
16. Yang F et al..  (2017)  SDF1-CXCR4 Signaling Maintains Central Post-Stroke Pain through Mediation of Glial-Neuronal Interactions..  Front Mol Neurosci,  10  (226).  [PMID:28785202]
17. Cugurra A et al..  (2021)  Skull and vertebral bone marrow are myeloid cell reservoirs for the meninges and CNS parenchyma..  Science,  373  (6553): [PMID:34083447]
18. Morioka N et al..  (2019)  Spinal high-mobility group box-1 induces long-lasting mechanical hypersensitivity through the toll-like receptor 4 and upregulation of interleukin-1ß in activated astrocytes..  J Neurochem,  150  (6): (738-758).  [PMID:31273787]
19. Ding Q et al..  (2019)  Stemona alkaloids suppress the positive feedback loop between M2 polarization and fibroblast differentiation by inhibiting JAK2/STAT3 pathway in fibroblasts and CXCR4/PI3K/AKT1 pathway in macrophages..  Int Immunopharmacol,  72  (385-394).  [PMID:31030094]
20. Umezu K et al..  (2020)  Stromal cell-derived factor 1 regulates in vitro sperm migration towards the cumulus-oocyte complex in cattle..  PLoS One,  15  (4): (e0232536).  [PMID:32353075]
21. Miao G et al..  (2020)  TLR2/CXCR4 coassociation facilitates Chlamydia pneumoniae infection-induced atherosclerosis..  Am J Physiol Heart Circ Physiol,  318  (6): (H1420-H1435).  [PMID:32330088]
22. Lee IP et al..  (2014)  Toxoplasma gondii is dependent on glutamine and alters migratory profile of infected host bone marrow derived immune cells through SNAT2 and CXCR4 pathways..  PLoS One,  (10): (e109803).  [PMID:25299045]
23. Jung O et al..  (2019)  VLA-4 phosphorylation during tumor and immune cell migration relies on its coupling to VEGFR2 and CXCR4 by syndecan-1..  J Cell Sci,  132  (20): [PMID:31562188]
24. Yuqian Chen, Jin Liu, Qianqian Zhang, Limin Chai, Huan Chen, Danyang Li, Yan Wang, Yuanjie Qiu, Nirui Shen, Jia Zhang, Qingting Wang, Jian Wang, Xinming Xie, Shaojun Li, Manxiang Li.  (2024)  Activation of CaMKII/HDAC4 by SDF1 contributes to pulmonary arterial hypertension via stabilization Runx2.  EUROPEAN JOURNAL OF PHARMACOLOGY,  970  (176483).  [PMID:38479721] [10.1016/j.ejphar.2024.176483]

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