在 RAW 264.7 鼠巨噬细胞系细胞中，愈创木酚可抑制 COX-2 基因的表达和脂多糖 (LPS) 响应的 NF-κB 激活。酚类物质，包括苯酚、丁子香酚、愈创木酚和香草醛，对羊水泡腺前列腺素环加氧酶的抑制浓度为50%。还原顺序如下：苯酚（1600 μM）>香草醛（>500 μM）>愈创木酚（72 μM）>丁子香酚（12 μM）[1]。

Absorption, Distribution and Excretion
In rats, guaiacol is rapidly absorbed, being present in the blood 5 minutes after oral administration, and reaching its peak plasma concentration in about 10 minutes. Its elimination from the blood is usually as rapid.
Excreted by rabbits in combined form with sulfate (15%) and glucuronic acid (72%).
CREOSOTE IS RAPIDLY ABSORBED FROM THE GASTROENTERIC TRACT AND THROUGH THE SKIN. IT APPEARS TO BE EXCRETED IN THE URINE MAINLY IN CONJUGATION WITH SULFURIC, HEXURONIC, & OTHER ACIDS. OXIDATION ALSO OCCURS WITH THE FORMATION OF CMPD THAT IMPART A SMOKY APPEARANCE TO THE URINE. TRACES ARE EXCRETED BY WAY OF THE LUNGS.
Medical experience indicates that toxic quantities can be absorbed through the skin quite readily.
Methoxyphenol largely absorbed from digestive tract and stored in blood, kidneys, and respiratory organs. Excreted by rabbits in combined form with sulfate (15%) and glucuronic acid (72%).
In rats, guaiacol is rapidly absorbed, being present in the blood 5 minutes after oral administration, and reaching its peak plasma concentration in about 10 minutes. Its elimination from the blood is usually as rapid.

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Metabolism / Metabolites
.../IT APPEARS TO BE CONJUGATED/ WITH SULFURIC, HEXURONIC & OTHER ACIDS. OXIDATION...OCCURS WITH FORMATION OF COMPOUNDS THAT IMPART A SMOKY APPEARANCE TO THE URINE.
Several strains of Aspergillus niger hydroxylated anisole to give o-hydroxyanisole as main product.
o-Methoxyphenol yields 3-methoxycatechol probably in rabbit; yields o-methoxyphenyl sulfate probably in rabbit. o-Methoxyphenol yields catechol in rat; yields 1,2-dimethoxybenzene in mouse, rabbit, guinea pig, and rat. /From table/

Toxicity Data
LC50 (mice) = 7,570 mg/m3

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Interactions
Methoxyphenol has been found to contribute to the carcinogenic effect of tobacco smoke in rats.
Absorption was delayed when ibuprofen and guaiacol administered simultaneously.

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Non-Human Toxicity Values
LD50 Mouse male oral 525 mg/kg
LD50 Rat female oral 870 mg/kg
LD50 Rat male oral 885 mg/kg
LD50 Mouse subcutaneous 6.25-12.5 ug
LD50 Rat oral 725 mg/kg
LD50 Mouse oral 621 mg/kg
LD50 Rat oral 520 mg/kg

[1]. Re-evaluation of cyclooxygenase-2-inhibiting activity of vanillin and Guaiacol in macrophages stimulated with lipopolysaccharide. Anticancer Res. 2007 Mar-Apr;27(2):801-7.

O-methoxyphenol appears as colorless to amber crystals or liquid. Density (of solid) 1.129 g / cm3. Solidifies at 28 °C (82.4 °F), but may remain liquid for a long time even at a much lower temperature. Slightly water soluble. Soluble in aqueous sodium hydroxide. Used medicinally as an expectorant. Used, because of its anti-oxidant properties, as an anti-skinning agent for paints.
Guaiacol is a monomethoxybenzene that consists of phenol with a methoxy substituent at the ortho position. It has a role as an expectorant, a disinfectant, a plant metabolite and an EC 1.1.1.25 (shikimate dehydrogenase) inhibitor. It is functionally related to a catechol.
Guaiacol is an agent thought to have disinfectant properties and used as an expectorant. Guaiacol is a phenolic natural product first isolated from Guaiac resin and the oxidation of lignin. Guaiacol is also present in wood smoke, as a product of pyrolysis of lignin. Guaiacol has been found in the urine of patients with neuroblastoma and pheochromocytoma.
Guaiacol has been reported in Angelica gigas, Rhodotorula mucilaginosa, and other organisms with data available.
Guaiacol is a phenolic compound with a methoxy group and is the monomethyl ether of catechol. Guaiacol is readily oxidized by the heme iron of peroxidases including the peroxidase of cyclooxygenase (COX) enzymes. It therefore serves as a reducing co-substrate for COX reactions. Guaiacol is a phenolic natural product first isolated from Guaiac resin and the oxidation of lignin. It is a yellowish aromatic oil that is now commonly derived from guaiacum or wood creosote. It is used medicinally as an expectorant, antiseptic, and local anesthetic. Guaiacol is used in traditional dental pulp sedation, and has the property of inducing cell proliferation; guaiacol is a potent scavenger of reactive oxygen radicals and its radical scavenging activity may be associated with its effect on cell proliferation. Guaiacol is also used in the preparation of synthetic vanillin. Guaiacol is also present in wood smoke, as a product of pyrolysis of lignin. Guaiacol has been found in the urine of patients with neuroblastoma and pheochromocytoma. (A3556, A3559).
2-methoxyphenol is a metabolite found in or produced by Saccharomyces cerevisiae.
An agent thought to have disinfectant properties and used as an expectorant. (From Martindale, The Extra Pharmacopoeia, 30th ed, p747)
See also: Wood Creosote (part of); Tolu balsam (USP) (part of); Creosote (annotation moved to).

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Drug Indication
It is used medicinally as an expectorant, antiseptic, and local anesthetic. Guaiacol is used in traditional dental pulp sedation, and has the property of inducing cell proliferation; guaiacol is a potent scavenger of reactive oxygen radicals and its radical scavenging activity may be associated with its effect on cell proliferation.

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Therapeutic Uses
IT IS USED EMPIRICALLY AS AN EXPECTORANT TO LESSEN AMT OF MUCOUS IN THE CHRONIC STAGES OF BRONCHITIS & BRONCHIECTASIS. IT IS FREQUENTLY PRESCRIBED FOR ITS STIMULANT EXPECTORANT ACTION AS A CONSTITUENT OF A STEAM INHALANT. THE ANTISEPTIC ACTION IS WEAK & NOT CLINICALLY USEFUL. ... IT HAS BEEN EMPLOYED AS A LOCAL ANESTHETIC IN DENTISTRY, IN A MANNER SIMILAR TO THYMOL. IT IS OCCASIONALLY EMPLOYED EXTERNALLY FOR ITS DISINFECTANT ACTION.
MEDICATION (VET): TOPICALLY (1.0-1.5%), IN UDDER AND WOUND TREATMENT OINTMENTS & IN POULTICES; WHEN ELIMINATED BY RESP MUCOUS MEMBRANES, SLIGHT ANTISEPTIC & LOCAL ANESTHETIC EFFECTS MAY OCCUR. INTERNALLY ... USED IN ANTIFERMENT & ANTIBLOAT MIXTURES.
ANTIPYRETIC; STYPTIC; ASTRINGENT
MEDICATION (VET): PARASITICIDE, DEODORANT
Disinfectants; Expectorants
Medication (Vet): ... Oral or parenteral mucolytic antiseptic antitussive in bronchopneumonias. ... Inhalant. In antiphlogistic, anodyne liquids on congested udders, in horse leg paints, and in poultices. Spray over tail biting swine to ... discourage cannibalism. Parenteral /dosage/ in camphorated oil. US mfr use 50 mg/mL concentration.
For the symptomatic relief of coughs associated with colds, bronchial catarrh, influenza and upper respiratory tract infections such as laryngitis and pharyngitis. Codeine is a well-known centrally acting cough suppressant. Guaiacol acts as an expectorant, loosening bronchial secretions in the respiratory tract. /Guaiacol, codeine combination/

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Drug Warnings
THE REPEATED ABSORPTION OF THERAPEUTIC DOSES FROM GASTROENTERIC TRACT MAY INDUCE SIGNS OF CHRONIC INTOXICATION, CHARACTERIZED BY DISTURBANCES OF VISION & DIGESTION (INCR PERISTALSIS & EXCRETION OF BODY FECES). IN ISOLATED CASES OF "SELF-MEDICATION", HYPERTENSION & ALSO GENERAL CARDIOVASCULAR COLLAPSE HAVE BEEN DESCRIBED.
WHEREVER CREOSOTE IS INDICATED FOR INTERNAL MEDICATION CREOSOTE FROM WOOD TAR SHOULD BE DISPENSED & UNDER NO CIRCUMSTANCES SHOULD CREOSOTE FROM COAL TAR BE GIVEN, UNLESS EXPLICITLY SO DIRECTED.
Do not use in Cats.

C7H8O2

124.1372

124.052

90-05-1

Guaiacol-d3;74495-69-5;Guaiacol-d7;1065473-05-3;Guaiacol-13C6;202326-52-1;Guaiacol-d4;7329-52-4;Guaiacol-d4-1;20189-11-1

460

Colorless to light yellow <26°C powder,>29°C liquid

1.2±0.1 g/cm3

207.5±29.0 °C at 760 mmHg

26-29 °C(lit.)

79.3±24.3 °C

0.2±0.4 mmHg at 25°C

1.538

2.11

29.46

1

2

1

9

83

0

OC1C(OC)=CC=CC=1

LHGVFZTZFXWLCP-UHFFFAOYSA-N

InChI=1S/C7H8O2/c1-9-7-5-3-2-4-6(7)8/h2-5,8H,1H3

2-methoxyphenol

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

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

DMSO : ≥ 100 mg/mL (~805.54 mM)
H2O : ~37.5 mg/mL (~302.08 mM)

配方 1 中的溶解度: ≥ 2.5 mg/mL (20.14 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 25.0 mg/mL澄清DMSO储备液加入到400 μL PEG300中，混匀；然后向上述溶液中加入50 μL Tween-80，混匀；加入450 μL生理盐水定容至1 mL。
*生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。

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配方 2 中的溶解度: ≥ 2.5 mg/mL (20.14 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 25.0 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中，混匀。
*20% SBE-β-CD 生理盐水溶液的制备（4°C，1 周）：将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中，得到澄清溶液。

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配方 3 中的溶解度: ≥ 2.5 mg/mL (20.14 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 25.0 mg/mL 澄清 DMSO 储备液加入到 900 μL 玉米油中并混合均匀。

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配方 4 中的溶解度: 16.67 mg/mL (134.28 mM) in PBS (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液; 超声助溶.

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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。