MK 571钠盐(L 660711钠盐), CysLT 1 受体拮抗剂

强效,选择性和竞争性CysLT 1受体拮抗剂
有货

库存信息

关闭
货号 (SKU) 包装规格 是否现货 价格 数量
M420726-1ml
1ml 现货 Stock Image

基本描述

别名 3-[[[3-[(E)-2-(7-氯喹啉-2-基)乙烯基]苯基]-[3-(二甲氨基)-3-氧丙基]硫烷基甲基]硫烷基丙酸钠盐
英文别名 3-[{3-[(E)-2-(7-Chloro-quinolin-2-yl)-vinyl]-phenyl}-(2-diethylcarbamoyl-ethylsulfanyl)-methylsulfanyl]-propionic acid | Propanoic acid, 3-(((3-(2-(7-chloro-2-quinolinyl)ethenyl)phenyl)((3-(dimethylamino)-3-oxopropyl)thio)methyl)thio)-, (E)- | 5-(3-(2-(7-
规格或纯度 Moligand™, 10mM in DMSO
英文名称 MK 571 sodium salt (L 660711 sodium salt)
生化机理 高效,选择性和竞争性CysLT 1受体拮抗剂(IC 50 = 1.5 nM,LTD 4)。强大的MRP1抑制剂。在体内显示出抗缺血,抗炎和镇痛作用。口服有效。
储存温度 避光,-80℃储存
运输条件 超低温冰袋运输
作用类型 拮抗剂
作用机制 CysLT 1 受体拮抗剂
产品介绍

MK571 (L660711) 是一种具有口服活性的、选择性半胱氨酰白三烯受体CysLT1的拮抗剂。



 

关联靶点(人)

CYSLTR1 Tclin 半胱氨酰白三烯受体 1(Cysteinyl leukotriene receptor 1) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
ABCC1 Tchem 多药耐药相关蛋白1(Multidrug resistance-associated protein 1) (4 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
VDR Tclin Vitamin D receptor (26531 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CYSLTR1 Tclin Cysteinyl leukotriene receptor 1 (2118 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Homo sapiens (32628 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HL-60 (67320 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HEK293 (82097 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ABCG2 Tchem ATP-binding cassette sub-family G member 2 (4927 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ABCC2 Tchem Canalicular multispecific organic anion transporter 1 (1191 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ABCB11 Tchem Bile salt export pump (2311 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ABCC3 Tbio Canalicular multispecific organic anion transporter 2 (718 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
GMNN Tbio Geminin (128009 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PMP22 Tbio Peripheral myelin protein 22 (699 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
SLCO1B1 Tchem Solute carrier organic anion transporter family member 1B1 (2672 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
SLCO1B3 Tchem Solute carrier organic anion transporter family member 1B3 (2517 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
SLCO2B1 Tchem Solute carrier organic anion transporter family member 2B1 (580 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ABCC4 Tchem Multidrug resistance-associated protein 4 (785 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
USP1 Tchem Ubiquitin carboxyl-terminal hydrolase 1 (22556 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ABCC5 Tchem Multidrug resistance-associated protein 5 (50 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ABCC6 Tbio Multidrug resistance-associated protein 6 (18 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MRP3 Multidrug resistance associated protein (78 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ABCC11 Tbio ATP-binding cassette sub-family C member 11 (24 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MEN1 Tchem Menin/Histone-lysine N-methyltransferase MLL (48157 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)

Abcc1 Multidrug resistance-associated protein 1 (42 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Abcb1b P-glycoprotein 1 (174 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Hdac6 Histone deacetylase 6 (222 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Plasmodium falciparum (966862 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Cavia porcellus (23802 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Mus musculus (284745 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Rattus norvegicus (775804 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Monkey (844 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
L929 (3802 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
GCN5 Histone acetyltransferase GCN5 (89 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Luciferin 4-monooxygenase (66902 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
rep Replicase polyprotein 1ab (378 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Rorc Nuclear receptor ROR-gamma (89407 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ffp 4'-phosphopantetheinyl transferase ffp (24982 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
SARS-CoV-2 (38078 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 3-[[3-[(E)-2-(7-chloroquinolin-2-yl)ethenyl]phenyl]-[3-(dimethylamino)-3-oxopropyl]sulfanylmethyl]sulfanylpropanoic acid
INCHI InChI=1S/C26H27ClN2O3S2/c1-29(2)24(30)12-14-33-26(34-15-13-25(31)32)20-5-3-4-18(16-20)6-10-22-11-8-19-7-9-21(27)17-23(19)28-22/h3-11,16-17,26H,12-15H2,1-2H3,(H,31,32)/b10-6+
InChi Key AXUZQJFHDNNPFG-UXBLZVDNSA-N
Canonical SMILES CN(C)C(=O)CCSC(C1=CC=CC(=C1)C=CC2=NC3=C(C=CC(=C3)Cl)C=C2)SCCC(=O)O
Isomeric SMILES CN(C)C(=O)CCSC(C1=CC=CC(=C1)/C=C/C2=NC3=C(C=CC(=C3)Cl)C=C2)SCCC(=O)O
关联CAS 115104-28-4
MeSH Entry Terms (3-(3-(2-(7-chloro-2-quinolinyl)ethenyl)phenyl)((3-dimethylamino-3-oxopropyl)thio)methyl)thiopropanoic acid;L 660,711;L 660711;L-660711;MK 0571;MK 0679;MK 571;MK-0571;MK-0679;MK-571;MK-679;MK571 cpd;verlukast;verlukast, (R-(E))-isomer
分子量 515.09
Reaxy-Rn 24674053
Reaxys-RN link address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=24674053&ln=

化学和物理性质

敏感性 对光敏感
分子量 515.100 g/mol
XLogP3 5.300
氢键供体数Hydrogen Bond Donor Count 1
氢键受体数Hydrogen Bond Acceptor Count 6
可旋转键计数Rotatable Bond Count 11
精确质量Exact Mass 514.115 Da
单同位素质量Monoisotopic Mass 514.115 Da
拓扑极表面积Topological Polar Surface Area 121.000 Ų
重原子数Heavy Atom Count 34
形式电荷Formal Charge 0
复杂度Complexity 693.000
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 1
定义的键立体中心计数Defined Bond Stereocenter Count 1
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 1
共价键合单元计数Covalently-Bonded Unit Count 1

安全和危险性(GHS)

Reaxy-Rn 24674053
Reaxys-RN link address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=24674053&ln=

技术规格说明书

Concentration 9-11(mmol/L)
Proton NMR spectrum Conforms to Structure

质检证书(CoA,COO,BSE/TSE 和分析图谱)

C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:

此产品的引用文献

1. Renjie Xu, Hongdan Zhu, Lingmin Hu, Beimeng Yu, Xiaohua Zhan, Yichu Yuan, Ping Zhou.  (2020)  Characterization of the intestinal absorption of morroniside from Cornus officinalis Sieb. et Zucc via a Caco-2 cell monolayer model.  PLoS One,  15  (5): (e0227844).  [PMID:32470043] [10.1371/journal.pone.0227844]
2. Renjie Xu, Yichu Yuan, Jia Qi, Jia Zhou, Xiaowen Guo, Jian Zhang, Ruanjuan Zhan.  (2018)  Elucidation of the Intestinal Absorption Mechanism of Loganin in the Human Intestinal Caco-2 Cell Model.  Evidence-based Complementary and Alternative Medicine,  2018  (8340563).  [PMID:30671130] [10.1155/2018/8340563]
3. Min Zhang, Ying Peng, Mengyue Wang, Beibei Gao, Lijuan Zhao, Xiaobo Li.  (2019)  The influence of compatibility of Si-Ni decoction with metabolism in intestinal bacteria on transports of toxic diterpenoid alkaloids from processed aconite root across Caco-2 monolayers.  JOURNAL OF ETHNOPHARMACOLOGY,  228  (164).  [PMID:30223050] [10.1016/j.jep.2018.09.022]
4. Xu Renjie, Peng Ying, Wang Mengyue, Li Xiaobo.  (2019)  Intestinal Absorption of Isoalantolactone and Alantolactone, Two Sesquiterpene Lactones from Radix Inulae, Using Caco-2 Cells.  EUROPEAN JOURNAL OF DRUG METABOLISM AND PHARMACOKINETICS,  44  (2): (295-303).  [PMID:30209793] [10.1007/s13318-018-0510-x]
5. Yanghui Chen, Yuan Li, Junliang Luo, Zixin Li, Yu Huang, Jia Cai, Dongneng Jiang, Defeng Zhang, Jichang Jian, Jun Qiang, Bei Wang.  (2024)  A novel study of brain microvascular endothelial cells induced by astrocyte conditioned medium for constructing blood brain barrier model in vitro: A promising tool for meningitis of teleost.  FISH & SHELLFISH IMMUNOLOGY,  146  (109401).  [PMID:38266792] [10.1016/j.fsi.2024.109401]
6. Wang Aiping, Ning Jie, Zhao Lu, Xu Renjie.  (2024)  Lipid-lowering effect and oral transport characteristics study of curculigoside.  Frontiers in Cardiovascular Medicine,  11  [PMID:39015683] [10.3389/fcvm.2024.1426379]

参考文献

1. Renjie Xu, Hongdan Zhu, Lingmin Hu, Beimeng Yu, Xiaohua Zhan, Yichu Yuan, Ping Zhou.  (2020)  Characterization of the intestinal absorption of morroniside from Cornus officinalis Sieb. et Zucc via a Caco-2 cell monolayer model.  PLoS One,  15  (5): (e0227844).  [PMID:32470043] [10.1371/journal.pone.0227844]
2. Renjie Xu, Yichu Yuan, Jia Qi, Jia Zhou, Xiaowen Guo, Jian Zhang, Ruanjuan Zhan.  (2018)  Elucidation of the Intestinal Absorption Mechanism of Loganin in the Human Intestinal Caco-2 Cell Model.  Evidence-based Complementary and Alternative Medicine,  2018  (8340563).  [PMID:30671130] [10.1155/2018/8340563]
3. Min Zhang, Ying Peng, Mengyue Wang, Beibei Gao, Lijuan Zhao, Xiaobo Li.  (2019)  The influence of compatibility of Si-Ni decoction with metabolism in intestinal bacteria on transports of toxic diterpenoid alkaloids from processed aconite root across Caco-2 monolayers.  JOURNAL OF ETHNOPHARMACOLOGY,  228  (164).  [PMID:30223050] [10.1016/j.jep.2018.09.022]
4. Xu Renjie, Peng Ying, Wang Mengyue, Li Xiaobo.  (2019)  Intestinal Absorption of Isoalantolactone and Alantolactone, Two Sesquiterpene Lactones from Radix Inulae, Using Caco-2 Cells.  EUROPEAN JOURNAL OF DRUG METABOLISM AND PHARMACOKINETICS,  44  (2): (295-303).  [PMID:30209793] [10.1007/s13318-018-0510-x]
5. Yanghui Chen, Yuan Li, Junliang Luo, Zixin Li, Yu Huang, Jia Cai, Dongneng Jiang, Defeng Zhang, Jichang Jian, Jun Qiang, Bei Wang.  (2024)  A novel study of brain microvascular endothelial cells induced by astrocyte conditioned medium for constructing blood brain barrier model in vitro: A promising tool for meningitis of teleost.  FISH & SHELLFISH IMMUNOLOGY,  146  (109401).  [PMID:38266792] [10.1016/j.fsi.2024.109401]
6. Wang Aiping, Ning Jie, Zhao Lu, Xu Renjie.  (2024)  Lipid-lowering effect and oral transport characteristics study of curculigoside.  Frontiers in Cardiovascular Medicine,  11  [PMID:39015683] [10.3389/fcvm.2024.1426379]

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