PHOME
目录号 : GC40883
An HTS substrate for sEH
Cas No.:1028430-42-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
EpETrE metabolizes arachidonic acid such as 11(12-EpETrE and 14(15)-EpETrE have been identified as endothelium derived hyperpolarizing factors with vasodilator activity. Soluble epoxide hydrolase (sEH) catalyzes the conversion of EpETrEs to the corresponding DiHETrEs thereby diminishing their activity. Inhibitors of sEH may therefore have clinical utility for treating hypertension and systemic inflammation. PHOME is a fluorogenic substrate for human sEH which displays good aqueous stability and solubility making it ideal for high throughput screening (HTS) programs. Hydrolysis of the substrate yields a highly fluorescent product that can be monitored at excitation and emission wavelengths of 330 and 465 nm, respectively. This fluorescent assay has a sensitivity that is 100 times greater than previously used spectrophotometric assays. NOTE: This substrate should only be used with the pure EH. If this substrate is used with crude enzyme preparations it is critical that all esterase activity is removed or inhibited, such as with organophosphate or a trifluoroketone inhibitor, and that glutathione is depleted and/or glutathione S-transferase is inhibited.
| Cas No. | 1028430-42-3 | SDF | |
| Canonical SMILES | COc1ccc2cc(ccc2c1)C(CN)OC(=O)CC1OC1c1ccccc1 | ||
| 分子式 | C23H19NO4 | 分子量 | 373.4 |
| 溶解度 | DMF: 10 mg/ml,DMSO: 10 mg/ml | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.6781 mL | 13.3905 mL | 26.7809 mL |
| 5 mM | 0.5356 mL | 2.6781 mL | 5.3562 mL |
| 10 mM | 0.2678 mL | 1.339 mL | 2.6781 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
trans-Dichloridobis[tris-(2-methoxy-phen-yl)phosphine]palladium(II)
Acta Crystallogr Sect E Struct Rep Online 2009 Oct 10;65(Pt 11):m1342.PMID:21578098DOI:10.1107/S1600536809040719.
The structure of the title compound, [PdCl(2)(C(21)H(21)O(3)P)(2)], shows a nearly square-planar geometry for the Pd(II) atom within the Cl(2)Pd[P(PHOME)(3)](2) ligand set. The Pd(II) atom sits on a centre of inversion and therefore the asymmetric unit contains one half-mol-ecule, i.e. half of one Pd(II) atom, one Cl atom and one tris-(2-methoxy-phen-yl)phosphine ligand.
DFT modeling of silver disorder and mobility in the semiconductor cluster [Ag28S26(P(O)PHOME)12(PPh3)12]
Chemistry 2008;14(1):319-24.PMID:17990251DOI:10.1002/chem.200701119.
Disorder of silver atoms and high cation mobility are commonly observed and closely coupled features in silver chalcogenides. The ligand-stabilized cluster [Ag28(micro6-S)2{ArP(O)S2}12(PPh3)12] (1) (Ar=4-anisyl), with a total of 666 atoms, displays in its X-ray structure highly localized disorder at two core silver atoms. To explore the nature of this disorder, we have applied density functional methods to its internal structure and flexibility. The pseudo-S6 symmetry of the cluster provides six equivalent pockets to place the pair of silver atoms, and with the exception of populating neighboring sites, all permutations relax to structures with similar cores. The barrier to concerted motion of the central silver atoms from one set of pockets to the next of the Ci-symmetric conformer is estimated to be less than about 26 kJ mol(-1). Cluster 1 can be considered a model for bulk phase cation mobility.
trans-Bis[bis-(2-methoxy-phen-yl)phenyl-phosphine-κP]dichloridopalladium(II)
Acta Crystallogr Sect E Struct Rep Online 2009 Oct 10;65(Pt 11):m1341.PMID:21578097DOI:10.1107/S1600536809040744.
The structure of the title compound, [PdCl(2)(C(20)H(19)O(2)P)(2)], shows a square-planar geometry for the Pd(II) ion within a Cl(2)Pd[PPh(PHOME)(2)](2) ligand set. The Pd(II) atom sits on an inversion centre and therefore the asymmetric unit contains the Pd(II) atom, one Cl atom and one bis-(2-methoxy-phen-yl)phenyl-phosphine ligand. The trans arrangement of ligands is also imposed by symmetry.
Phenoxyl radicals: H-bonded and coordinated to Cu(II) and Zn(II)
Dalton Trans 2006 Jan 7;(1):258-67.PMID:16357984DOI:10.1039/b513221p.
Two pro-ligands ((R)LH) comprised of an o,p-di-tert-butyl-substituted phenol covalently bonded to a benzimidazole ((Bz)LH) or a 4,5-di-p-methoxyphenyl substituted imidazole ((PHOME)LH), have been structurally characterised. Each possesses an intramolecular O-H[dot dot dot]N hydrogen bond between the phenolic O-H group and an imidazole nitrogen atom and (1)H NMR studies show that this bond is retained in solution. Each (R)LH undergoes an electrochemically reversible, one-electron, oxidation to form the [(R)LH] (+) radical cation that is considered to be stabilised by an intramolecular O...H-N hydrogen bond. The (R)LH pro-ligands react with M(BF(4))(2).H(2)O (M = Cu or Zn) in the presence of Et(3)N to form the corresponding [M((R)L)(2)] compound. [Cu((Bz)L)(2)] (), [Cu((PHOME)L)(2)] (), [Zn((Bz)L)(2)] and [Zn((PHOME)L)(2)] have been isolated and the structures of .4MeCN, .2MeOH, .2MeCN and .2MeCN determined by X-ray crystallography. In each compound the metal possesses an N(2)O(2)-coordination sphere: in .4MeCN and .2MeOH the {CuN(2)O(2)} centre has a distorted square planar geometry; in .2MeCN and .2MeCN the {ZnN(2)O(2)} centre has a distorted tetrahedral geometry. The X-band EPR spectra of both and , in CH(2)Cl(2)-DMF (9 : 1) solution at 77 K, are consistent with the presence of a Cu(ii) complex having the structure identified by X-ray crystallography. Electrochemical studies have shown that each undergo two, one-electron, oxidations; the potentials of these processes and the UV/vis and EPR properties of the products indicate that each oxidation is ligand-based. The first oxidation produces [M(II)((R)L)((R)L )](+), comprising a M(ii) centre bound to a phenoxide ((R)L) and a phenoxyl radical ((R)L ) ligand; these cations have been generated electrochemically and, for R = PHOME, chemically by oxidation with Ag[BF(4)]. The second oxidation produces [M(II)((R)L )(2)](2+). The information obtained from these investigations shows that a suitable pro-ligand design allows a relatively inert phenoxyl radical to be generated, stabilised by either a hydrogen bond, as in [(R)LH] (+) (R = Bz or PHOME), or by coordination to a metal, as in [M(II)((R)L)((R)L )](+) (M = Cu or Zn; R = Bz or PHOME). Coordination to a metal is more effective than hydrogen bonding in stabilising a phenoxyl radical and Cu(ii) is slightly more effective than Zn(II) in this respect.
Incorporation of Pendant Bases into Rh(diphosphine)2 Complexes: Synthesis, Thermodynamic Studies, And Catalytic CO2 Hydrogenation Activity of [Rh(P2N2)2](+) Complexes
J Am Chem Soc 2015 Jul 1;137(25):8251-60.PMID:26042557DOI:10.1021/jacs.5b04291.
A series of five [Rh(P2N2)2](+) complexes (P2N2 = 1,5-diaza-3,7-diphosphacyclooctane) have been synthesized and characterized: [Rh(P(Ph)2N(Ph)2)2](+) (1), [Rh(P(Ph)2N(Bn)2)2](+) (2), [Rh(P(Ph)2N(PHOME)2)2](+) (3), [Rh(P(Cy)2N(Ph)2)2](+) (4), and [Rh(P(Cy)2N(PHOME)2)2](+) (5). Complexes 1-5 have been structurally characterized as square planar rhodium bis-diphosphine complexes with slight tetrahedral distortions. The corresponding hydride complexes 6-10 have also been synthesized and characterized, and X-ray diffraction studies of HRh(P(Ph)2N(Bn)2)2 (7), HRh(P(Ph)2N(PHOME)2)2 (8) and HRh(P(Cy)2N(Ph)2)2 (9) show that the hydrides have distorted trigonal bipyramidal geometries. Equilibration of complexes 2-5 with H2 in the presence of 2,8,9-triisopropyl-2,5,8,9-tetraaza-1-phosphabicyclo[3,3,3]undecane (Verkade's base) enabled the determination of the hydricities and estimated pKa's of the Rh(I) hydride complexes using the appropriate thermodynamic cycles. Complexes 1-5 were active for CO2 hydrogenation under mild conditions, and their relative rates were compared to that of [Rh(depe)2](+), a nonpendant-amine-containing complex with a similar hydricity to the [Rh(P2N2)2](+) complexes. It was determined that the added steric bulk of the amine groups on the P2N2 ligands hinders catalysis and that [Rh(depe)2](+) was the most active catalyst for hydrogenation of CO2 to formate.