N-propyl Hexylone (hydrochloride)
目录号 : GC44460An Analytical Reference Standard
Cas No.:27912-42-1
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
N-propyl Hexylone (hydrochloride) is an analytical reference standard categorized as a cathinone. This product is intended for research and forensic applications.
| Cas No. | 27912-42-1 | SDF | |
| Canonical SMILES | O=C(C(CCCC)NCCC)C1=CC(OCO2)=C2C=C1.Cl | ||
| 分子式 | C16H23NO3•HCl | 分子量 | 313.8 |
| 溶解度 | DMF: 2.5 mg/ml,DMSO: 14 mg/ml,Ethanol: 0.25 mg/ml,PBS (pH 7.2): 3 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 | 3.1867 mL | 15.9337 mL | 31.8674 mL |
| 5 mM | 0.6373 mL | 3.1867 mL | 6.3735 mL |
| 10 mM | 0.3187 mL | 1.5934 mL | 3.1867 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。
Differential block of N-propyl derivatives of amitriptyline and doxepin for sciatic nerve block in rats
Reg Anesth Pain Med 2005 Jul-Aug;30(4):344-50.PMID:16032586DOI:10.1016/j.rapm.2005.04.008.
Background and objectives: The propyl group of ropivacaine ( N -propyl-2',6'-pipecoloxylidide hydrochloride) could be responsible for conferring some sensory selectivity to this drug. Thus, adding a propyl group to experimental local anesthetics (LAs) (e.g., the tricyclic antidepressants amitriptyline and doxepin) to increase sensory selectivity may be useful. We, therefore, synthesized N -propyl amitriptyline and N -propyl doxepin and investigated a potential predominance of sensory/nociceptive block over motor block (differential block) in a rat sciatic nerve block model. In addition, tetrodotoxin (TTX), a naturally occuring Na + channel blocker, was coinjected to investigate whether it increased block duration. Methods: A 0.2-mL test dose of N -propyl amitriptyline and N -propyl doxepin, at a concentration of 1, 2.5, 5, and 10 mM, (alone or in combination with TTX at a concentration of 20 microM) was injected by the subfascial sciatic nerve approach. Motor function and sensory function (nociception) were evaluated by the force a rat's hind limb produced when pushing against a balance and the reaction to pinch, respectively. Results: N -propyl amitriptyline and N -propyl doxepin demonstrated prolonged block duration, with N -propyl amitriptyline displaying significant differential block at higher concentrations (5 and 10 mM). The combination of either of these drugs with TTX increased the potency as well as the efficacy. Neurotoxicity commenced at concentrations of 5 to 10 mM. Conclusions: Detailed histopathologic nerve toxicity evaluations are justified to determine whether N -propyl amitriptyline has potential as a more sensory-selective local anesthetic at lower concentrations or as a predominantly sensory-selective neurolytic agent at higher concentrations.
Adsorptive voltammetry of 2-(5-bromo-2-pyridyl)azo-5-[N-n-propyl-N-(3-sulfopropyl)amino]phenol on a carbon paste electrode in the presence of organic cations and polycation
Anal Sci 2006 Dec;22(12):1577-80.PMID:17159318DOI:10.2116/analsci.22.1577.
The adsorption of ion-association complexes on a carbon paste electrode (CPE) was investigated by cyclic voltammetry using an electroactive hydrophobic anion probe. The redox reactions of 2-(5-bromo-2-pyridyl)azo-5-[N-n-propyl-N-(3-sulfopropyl)amino]phenol (5-Br-PAPS), the analytical probe, were irreversible. The reduction of the azo group and the oxidation of the phenol were observed at -0.1 V and 0.9 V vs. SCE, respectively, in a 0.1 mol L(-1) H(2)SO(4) solution. The peak currents for the redox reaction increased with the concentration of the cationic surfactant and the accumulation time. The increase in the ratio of the peak current to the concentration of cationic surfactants was proportional to the hydrophobicity. The peak current for 5-Br-PAPS also increased when a polycation, polyhexamethylene biguanide hydrochloride, was added and was strongly dependent on the ionic strength and pH, in contrast to cationic surfactants.
Properties, stability, assay, and preliminary pharmacokinetics of the immunomodulatory 1,2-O-isopropylidene-3-O-3'(N',N'-dimethylamino-n-propyl)-D-glucofuranose hydrochloride
J Pharm Sci 1982 Apr;71(4):387-95.PMID:7086643DOI:10.1002/jps.2600710404.
1,2-O-Isopropylidene-3-O-3'(N',N'-dimethylamino-n-propyl)-D -glucofuranose hydrochloride (I) is a new agent with claimed immunomodulatory action and antiviral activity. Thin-layer chromatographic procedures and identifying tests were developed to separate the drug, its synthetic precursors, and solvolytic products, and were applied to stability studies. It is stable in 0.1 N NaOH at 60 degrees where its acid solvolysis product, 3-O-3'-(N',N'-dimethylamino-n-propyl)-D-glucose is readily degraded. The partition coefficient of I (pK'a = 9.28) between chloroform and plasma was 6.4 +/- 0.2 SEM between pH 10.5 and 11.0. Plasma and urine (0.5 ml) adjusted to pH 11.0 were extracted with 10 ml of chloroform and the extract evaporated. The reconstituted residue in 50 microliters of benzene, with the disopropylaminoethyl analog of I as an internal standard, was derivatized with 50 microliters of heptafluorobutyric anhydride at 60 degrees for 45 min and was evaporated and reconstituted in 100 microliters of benzene to be assayed for I by GLC with electron capture detection with a sensitivity of 5 ng/0.5 ml of biological fluid. The procedure was applied to pharmacokinetics in the dog and a two-compartment body model was observed with a terminal half-life of 103-130 min. At the 40-mg dose, 60-64% was excreted renally unchanged and 20-34% as unidentified metabolites. At the 200-mg dose 82-85% was excreted unchanged and 15-17% as unidentified metabolites. The respective renal clearances of I were 135 and 163 ml/min. The respective total clearances of I were 204 and 191 ml/min. These metabolites were apparently unextracted with chloroform from biological fluids at pH 11 and the liquid scintillation counting (LSC) assay of extracted radiolabeled I appeared synonomous with the GLC assay of I in such fluids.
Pharmacokinetics of intravenous and oral 1,2-O-isopropylidene-3-O-3'-(N',N'-dimethylamino-n-propyl)-D-glucofuranose hydrochloride in the dog as a function of dose and characterization of metabolites
J Pharm Sci 1983 Sep;72(9):1045-57.PMID:6631692DOI:10.1002/jps.2600720921.
The pharmacokinetics of 1,2-O-isopropylidene-3-O-3'-(N',N'-dimethylamino-n-propyl)-D-glucofuranose hydrochloride (1) was studied in dogs at intravenous and oral doses of 1-50 mg/kg. There was no significant difference between the electron-capture GLC of the heptafluorobutyric derivative of I and the radiochemical assay of chloroform extracts of plasma and urine for 1- to 20-mg/kg doses. Urinary amounts of I measured by GLC were 20% lower than radioassays of chloroform extracts at the 50-mg/kg dose. The pharmacokinetics of intravenous I was described by a two-compartment body model with sequential plasma half-lives of 7.5 +/- 0.7 and 136 +/- 6 min. No apparent dose-dependent pharmacokinetics for I was observed on intravenous or oral administration. The apparent volume of distribution of the central compartment, 13.1 +/- 0.7 liters, is approximately the volume of the total body water in a 20-kg dog. The apparent overall volume of distribution of 40.0 +/- 1.5 liters exceeds the total body water, indicative of sequestration of I in tissues. Total and renal clearances were 205 +/- 5 and 155 +/- 5 ml/min, respectively. The high renal clearance of I indicated an excess of tubular secretion. Renal clearance of I was not dependent on urine flow nor urine pH. Recovery of radioactivity in the feces after I was intravenously administered was less than 1%. Plasma protein binding of I was less than 5%, and the erythrocyte-plasma water partition coefficient was approximately unity. Compounds excreted in urine were separated into chloroform-extractable (pH 12), ethyl acetate-extractable (pH 2), and unextractable fractions which were further characterized by TLC. A multiple-extraction system was developed to estimate relative amounts and intrinsic partition coefficients of these extractable compounds from radioactivity counts of scraped plates and was applied tof the assay of these compounds in the urine after intravenous administration of I. There was a readily chloroform-extractable metabolite with an apparent partition coefficient of 3.3 and Rf 0.43 on TLC in the systems used. This apparent major metabolite could account for 8% of the administered radioactivity. Minor chloroform-extractable metabolites (0.8-3.3%) had lower apparent partition coefficients (0.26) but Rf values of 0.28 and 0.44 . Ethyl acetate-extractable compounds (1.3-2.7%) had an apparent partition coefficient of 0.81 with Rf values of 0.52 and 0.68. Three unextractable compounds had Rf values of 0.20, 0.50, and 0.62 and accounted for 0.16, 2.8, and 0.9% of the administered radioactivity.
Pharmacokinetics of the immunomodulatory 1,2-O-isopropylidene-3-O-3'-(N',N'-dimethyl-amino-n-propyl)-D-glucofuranose hydrochloride in normal human volunteers
J Pharmacokinet Biopharm 1982 Jun;10(3):247-64.PMID:7175698DOI:10.1007/BF01059260.
1,2-O-Isopropylidene-3-O-3'(N',N'-dimethyl-amino-n-propyl)-D-glucofuranose hydrochloride, I, is a substituted sugar with claimed immunomodulatory action. Pharmacokinetic studies in 10 volunteers (bolus i.v., 100 mg) showed respective half-lives for each exponential in the sum of two exponentials that characterized plasma level decay with time of 4.6 +/- 0.4 (SEM) min, t1/2(lambda 1), and 244 +/- 20 min, t1/2(lambda 2)), The total and renal clearances were 277 +/- 20 and 254 +/- 18 (SEM) ml/min, indicative of tubular secretion. Urinary recovery was 93 +/- 2%. The estimated volumes of distribution of the central compartment and overall equilibrated tissues were 14.7 +/- 1.9 and 96 +/- 8 liters, respectively. Sequential daily oral administration of large amounts in capsules (1.2, 2.1, 2.9, 4.1, and 5.0 g) permitted an estimate of 63 +/- 4 (SEM)% bioavailability from urinary recovery of drug, with estimated terminal half-lives of 454 +/- 25 min from minimal data. Orally administered 2.03 g showed a rapid absorption (t1/2 = 10 min) after a lag time of 23 min, and a terminal plasma half-life of 344 min. Plasma protein binding of I was negligible. The erythrocyte/plasma water partition coefficient was close to unity.