N-Phenylnaphthalen-1-amine   中文名称: 防老剂甲

Absorption, Distribution and Excretion
In male Sprague-Dawley rats administered a single oral dose of 160 mg [14C] N-phenyl-1-naphthylamine/kg bw, the chemical was well absorbed, metabolized almost completely, and excreted primarily in the feces. Radioactivity was detected in plasma within 60 min, with the maximum concentration measured after 4 hr. After 24 hr, 20% of the radioactivity was found in the GI tract (including contents), 2.4% in fatty tissue, 0.4% in the liver, and 0.1% in the kidneys. 90% of the administered radioactivity was excreted within 48 hr; 95% was excreted within 72 hr (60% in the feces and 35% in the urine).
High performance liquid chromatographic and gas chromatographic methods for the determination of N-phenyl-1-naphthylamine (I) in biological fluid and tissues were developed, and the biological fate of I was studied in male rats following single and multiple oral administration. It was assumed that the intestinal absorption of I was excellent, because the fecal excretion of unchanged I was extremely low (0.4% of dose), and there was little unchanged I excreted in the urine (0.01% of dose). A large amount of glucuronide and sulfate metabolites was excreted in the urine. After single or multiple (6 days) oral administration, a small amount of unchanged I was distributed in fat, but the distribution of unchanged I in liver, kidney, spleen, heart and lung was extremely low.

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Metabolism / Metabolites
Mono- and dihydroxy-derivatives of N-phenyl-1-naphthylamine have been identified in in vitro metabolic studies conducted with rat liver microsomes. /It was/ suggested that the hydroxyl group in the mono-hydroxy derivative is in the naphthalene moiety at a para-position to the amino group, whereas at least one hydroxyl group in the dihydroxy-derivative is at the available para-position in the naphthyl ring. Pretreatment of male rats with phenobarbital or 3-methylcholanthrene increased the rate of microsomal metabolism, indicating that more than one P-450 enzyme is involved in the metabolism of N-phenyl-1-naphthylamine.
...In the ether extract of the urine /of male Sprague-Dawley rats administered a single oral dose of 160 mg [14C] N-phenyl-1-naphthylamine/kg bw/, at least five radioactive metabolites were detected but not identified.
In studies conducted with human volunteers or laboratory animals, the isomer N-phenyl-2-naphthylamine was partially metabolized to the known human carcinogen 2-naphthylamine following ingestion or inhalation. Although data concerning the formation of this metabolite are not available for N-phenyl-1-naphthylamine, it should be noted that, based on its chemical structure, it is unlikely that N-phenyl-1-naphthylamine is metabolized to 2-naphthylamine. /N-phenyl-2-naphthylamine/

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Biological Half-Life
In male Sprague-Dawley rats administered a single oral dose of 160 mg [14C] N-phenyl-1-naphthylamine/kg bw, ...the elimination half-lives were reported as 1.68 hr for the fast elimination and 33 hr for the slow elimination.

Non-Human Toxicity Values
LD50 Rat oral 1625 mg/kg
LD50 Mouse oral 1231 mg/kg

[1]. Biochemical characterization and bacterial expression of an odorant-binding protein from Locusta migratoria. Cell Mol Life Sci. 2003 Feb;60(2):390-400.

N-phenyl-1-naphthylamine appears as white to slightly yellowish prisms or reddish brown crystalline powder. (NTP, 1992)
N-Phenyl-1-naphthylamine is a member of naphthalenes.
N-Phenyl-1-naphthylamine has been reported in Streptomyces, Arundo donax, and Triadica sebifera with data available.

C16H13N

219.28

219.104

90-30-2

7013

Prisms or needles from alcohol; leaflets from ligroin.
Tan to purple crushed solid or crystals.
White to yellowish crystals
In its pure form crystallizes into lemon yellow prisms or needles ... marketed in the form of brown to dark violet crystals or light brown to light violet granules

1.2±0.1 g/cm3

370.7±0.0 °C at 760 mmHg

60-62 °C(lit.)

190.2±14.7 °C

0.0±0.8 mmHg at 25°C

1.702

4.2

12.03

1

1

2

17

232

0

C1C=CC(NC2C3C(=CC=CC=3)C=CC=2)=CC=1

XQVWYOYUZDUNRW-UHFFFAOYSA-N

InChI=1S/C16H13N/c1-2-9-14(10-3-1)17-16-12-6-8-13-7-4-5-11-15(13)16/h1-12,17H

N-phenylnaphthalen-1-amine

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

注意： 本产品在运输和储存过程中需避光。

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

注意: 如下所列的是一些常用的体内动物实验溶解配方，主要用于溶解难溶或不溶于水的产品（水溶度<1 mg/mL）。 建议您先取少量样品进行尝试，如该配方可行，再根据实验需求增加样品量。

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注射用配方1: DMSO : Tween 80： Saline = 10 : 5 : 85 (如： 100 μL DMSO → 50 μL Tween 80 → 850 μL Saline)
*生理盐水/Saline的制备：将0.9g氯化钠/NaCl溶解在100 mL ddH ₂ O中，得到澄清溶液。
注射用配方 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL DMSO → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)
注射用配方 3: DMSO : Corn oil = 10 : 90 (如： 100 μL DMSO → 900 μL Corn oil)
示例: 以注射用配方 3 (DMSO : Corn oil = 10 : 90) 为例说明, 如果要配制 1 mL 2.5 mg/mL的工作液, 您可以取 100 μL 25 mg/mL 澄清的 DMSO 储备液，加到 900 μL Corn oil/玉米油中, 混合均匀。

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注射用配方 4: DMSO : 20% SBE-β-CD in Saline = 10 : 90 [如：100 μL DMSO → 900 μL (20% SBE-β-CD in Saline)]
*20% SBE-β-CD in Saline的制备（4°C，储存1周）：将2g SBE-β-CD (磺丁基-β-环糊精) 溶解于10mL生理盐水中，得到澄清溶液。
注射用配方 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (如： 500 μL 2-Hydroxypropyl-β-cyclodextrin (羟丙基环胡精)→ 500 μL Saline)
注射用配方 6: DMSO : PEG300 : Castor oil : Saline = 5 : 10 : 20 : 65 (如： 50 μL DMSO → 100 μL PEG300 → 200 μL Castor oil → 650 μL Saline)
注射用配方 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (如： 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
注射用配方 8: 溶解于Cremophor/Ethanol (50 : 50), 然后用生理盐水稀释。
注射用配方 9: EtOH : Corn oil = 10 : 90 (如： 100 μL EtOH → 900 μL Corn oil)
注射用配方 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL EtOH → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)

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口服配方 1: 悬浮于0.5% CMC Na (羧甲基纤维素钠)
口服配方 2: 悬浮于0.5% Carboxymethyl cellulose (羧甲基纤维素)
示例: 以口服配方 1 (悬浮于 0.5% CMC Na)为例说明, 如果要配制 100 mL 2.5 mg/mL 的工作液, 您可以先取0.5g CMC Na并将其溶解于100mL ddH2O中，得到0.5%CMC-Na澄清溶液；然后将250 mg待测化合物加到100 mL前述 0.5%CMC Na溶液中，得到悬浮液。

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口服配方 3: 溶解于 PEG400 (聚乙二醇400)
口服配方 4: 悬浮于0.2% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 5: 溶解于0.25% Tween 80 and 0.5% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 6: 做成粉末与食物混合

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注意: 以上为较为常见方法，仅供参考， InvivoChem并未独立验证这些配方的准确性。具体溶剂的选择首先应参照文献已报道溶解方法、配方或剂型，对于某些尚未有文献报道溶解方法的化合物，需通过前期实验来确定（建议先取少量样品进行尝试），包括产品的溶解情况、梯度设置、动物的耐受性等。

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。