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雷帕霉素

mTORC1复合抑制剂
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货号 (SKU) 包装规格 是否现货 价格 数量
S115842-10mg
10mg 现货 Stock Image
S115842-25mg
25mg 现货 Stock Image
S115842-50mg
50mg 现货 Stock Image
S115842-250mg
250mg 现货 Stock Image
S115842-1g
1g 现货 Stock Image

基本描述

别名 雷帕霉素 | 西罗莫司 | (3S,6R,7E,9R,10R,12R,14S,15E,17E,19E,21S,23S,26R,27R,34aS)-9,10,12,13,14,21,22,23,24,25,26,27,32,33,34,34a-十六氢-9,27-二羟基-3-[(1R)-2-[(1S,3R,4R)-4-羟基-3-甲氧基环己基]-1-甲基乙基]-10,21-二甲氧基-6,8,12,14,20,26-六甲基-23,27-环氧-3H-吡啶并[2,1-c][1,4]氧杂氮杂环三十一烯-1,5,11,2
英文别名 AY 22989 | AY-22989 | CHEBI:9168 | EC 610-965-5 | HMS2089A21 | RAPA | (1R,9S,12S,15R,16E,18R,19R,21R,23S,24E,26E,28E,30S,32S,35R)-1,18-dihydroxy-12-{(2S)-1-[(1S,3R,4R)-4-hydroxy-3-methoxycyclohexyl]propan-2-yl}-19,30-dimethoxy-15,17,21,23,29,35-hexamethyl
规格或纯度 Moligand™, ≥98%(HPLC)
英文名称 Rapamycin
生化机理 一种大环三烯抗生素,能与雷帕霉素分子靶标(mTOR)结合并对其产生抑制作用。它与 FKBP12 形成复合物,能结合并抑制雷帕霉素分子靶标(mTOR)。雷帕霉素是一种强效免疫抑制剂,具有抗癌活性。与 FKBP-12 结合,抑制 mTOR(雷帕霉素哺乳动物靶标)C1 信号传导。在体外和体内诱导自噬。
应用 Rapamycin 是一种特异性的 mTOR 抑制剂,IC50 为 0.1 nM。
储存温度 -20°C储存,充氩
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

雷帕霉素是从 吸水链霉菌中分离得到的一种抗真菌抗生素。这种抗生素对所有的 白色念珠菌都有效。它可阻断激活T辅助细胞所需的信号转导通路。Rapamycin 是一种特异性的 mTOR 抑制剂,IC50 为 0.1 nM。

Rapamycin is an anti-fungal antibiotic isolated from Streptomyces hygroscopicus. This antibiotic is active against all strains of Candida albicans. It blocks the signal transduction pathways required for the activation of T-helper cells.

纯度 ≥98%(HPLC)

关联靶点(人)

FKBP1A Tclin 肽基脯氨酰顺反异构酶 FKBP1A(Peptidyl-prolyl cis-trans isomerase FKBP1A) (10 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)
FKBP1B Tchem 肽基脯氨酰顺反异构酶 FKBP1B(Peptidyl-prolyl cis-trans isomerase FKBP1B) (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)
FKBP5 Tchem 肽基脯氨酰顺反异构酶 FKBP5(Peptidyl-prolyl cis-trans isomerase FKBP5) (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)
EIF4E Tchem 真核翻译起始因子4E(Eukaryotic translation initiation factor 4E) (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)
PDCD4 Tchem 程序性细胞死亡蛋白 4(Programmed cell death protein 4) (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)
MTOR Tclin 丝氨酸/苏氨酸蛋白激酶 mTOR(Serine/threonine-protein kinase mTOR) (7 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)

名称和识别符

PubChem SID 488195295
分子类型 小分子
IIUPAC Name (1R,9S,12S,15R,16E,18R,19R,21R,23S,24E,26E,28E,30S,32S,35R)-1,18-dihydroxy-12-[(2R)-1-[(1S,3R,4R)-4-hydroxy-3-methoxycyclohexyl]propan-2-yl]-19,30-dimethoxy-15,17,21,23,29,35-hexamethyl-11,36-dioxa-4-azatricyclo[30.3.1.04,9]hexatriaconta-16,24,26,28-tetraene-2,3,10,14,20-pentone
INCHI 1S/C51H79NO13/c1-30-16-12-11-13-17-31(2)42(61-8)28-38-21-19-36(7)51(60,65-38)48(57)49(58)52-23-15-14-18-39(52)50(59)64-43(33(4)26-37-20-22-40(53)44(27-37)62-9)29-41(54)32(3)25-35(6)46(56)47(63-10)45(55)34(5)24-30/h11-13,16-17,25,30,32-34,36-40,42-44,46-47,53,56,60H,14-15,18-24,26-29H2,1-10H3/b13-11+,16-12+,31-17+,35-25+/t30-,32-,33-,34-,36-,37+,38+,39+,40-,42+,43+,44-,46-,47+,51-/m1/s1
InChi Key QFJCIRLUMZQUOT-HPLJOQBZSA-N
Smiles CC1CCC2CC(C(=CC=CC=CC(CC(C(=O)C(C(C(=CC(C(=O)CC(OC(=O)C3CCCCN3C(=O)C(=O)C1(O2)O)C(C)CC4CCC(C(C4)OC)O)C)C)O)OC)C)C)C)OC
Isomeric SMILES C[C@@H]1CC[C@H]2C[C@@H](/C(=C/C=C/C=C/[C@H](C[C@H](C(=O)[C@@H]([C@@H](/C(=C/[C@H](C(=O)C[C@H](OC(=O)[C@@H]3CCCCN3C(=O)C(=O)[C@@]1(O2)O)[C@H](C)C[C@@H]4CC[C@H]([C@@H](C4)OC)O)C)/C)O)OC)C)C)/C)OC
分子量 914.19
Reaxy-Rn 5848501

化学和物理性质

溶解性 不溶于水;可溶于氯仿、丙酮、二甲基甲酰胺、甲醇、乙醚
敏感性 对热敏感
比旋光度 -150° (C=0.2,MeOH)
熔点 177 °C(dec.)
分子量 914.200 g/mol
XLogP3 6.000
氢键供体数Hydrogen Bond Donor Count 3
氢键受体数Hydrogen Bond Acceptor Count 13
可旋转键计数Rotatable Bond Count 6
精确质量Exact Mass 913.555 Da
单同位素质量Monoisotopic Mass 913.555 Da
拓扑极表面积Topological Polar Surface Area 195.000 Ų
重原子数Heavy Atom Count 65
形式电荷Formal Charge 0
复杂度Complexity 1760.000
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 15
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 4
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 4
共价键合单元计数Covalently-Bonded Unit Count 1

安全和危险性(GHS)

象形图 GHS08
信号词 危险
RTECS VE6250000
Merck Index 8114

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批号(Lot Number) 证书类型 货号
G2326284 分析证书 S115842
G2326288 分析证书 S115842
G2326272 分析证书 S115842
G2326291 分析证书 S115842
C2505453 分析证书 S115842
C2505454 分析证书 S115842
C2505456 分析证书 S115842
C2505457 分析证书 S115842
C2505458 分析证书 S115842
E2305205 分析证书 S115842
E2305213 分析证书 S115842
E2305215 分析证书 S115842
E2305216 分析证书 S115842
E2305219 分析证书 S115842
K2228737 分析证书 S115842
H2428300 分析证书 S115842
H2428319 分析证书 S115842
H2428320 分析证书 S115842
H2428322 分析证书 S115842
H2428321 分析证书 S115842
E2421160 分析证书 S115842
E2421161 分析证书 S115842
E2421162 分析证书 S115842
E2421163 分析证书 S115842
E2421478 分析证书 S115842
B2518461 分析证书 S115842
B2518477 分析证书 S115842
B2518504 分析证书 S115842
G2326282 分析证书 S115842
E2305202 分析证书 S115842
E2305212 分析证书 S115842
E2305217 分析证书 S115842
E2305193 分析证书 S115842
E2305104 分析证书 S115842
K2228734 分析证书 S115842
K2228735 分析证书 S115842
K2228736 分析证书 S115842
K2228738 分析证书 S115842
H2230023 分析证书 S115842
G2227352 分析证书 S115842
G2227353 分析证书 S115842
G2227354 分析证书 S115842
G2227355 分析证书 S115842
J2215165 分析证书 S115842
K2218143 分析证书 S115842
D2009140 分析证书 S115842

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引用文献

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