Chlorobutanol
(Synonyms: 三氯叔丁醇) 目录号 : GC39358
Chlorobutanol (Chlorbutol, Chloreton, Chloretone, Chlortran|, trichloro-2-methyl-2-propanol) is a preservative, sedative, hypnotic and weak local anesthetic with antibacterial and antifungal properties.
Cas No.:57-15-8
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
Chlorobutanol (Chlorbutol, Chloreton, Chloretone, Chlortran|, trichloro-2-methyl-2-propanol) is a preservative, sedative, hypnotic and weak local anesthetic with antibacterial and antifungal properties.
| Cas No. | 57-15-8 | SDF | |
| 别名 | 三氯叔丁醇 | ||
| Canonical SMILES | CC(O)(C)C(Cl)(Cl)Cl | ||
| 分子式 | C4H7Cl3O | 分子量 | 177.46 |
| 溶解度 | DMSO: ≥ 100 mg/mL (563.51 mM) | 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 | 5.6351 mL | 28.1754 mL | 56.3507 mL |
| 5 mM | 1.127 mL | 5.6351 mL | 11.2701 mL |
| 10 mM | 0.5635 mL | 2.8175 mL | 5.6351 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。
Chlorobutanol toxicity
Ann Pharmacother 1996 Oct;30(10):1179-80.PMID:8893127doi
Although Chlorobutanol is available in a large number of preparations, the incidence of toxicity appears to be low. However, with continued exposure to high-dose Chlorobutanol, significant toxicity may occur. It seems prudent to use caution in the continued administration of products containing Chlorobutanol. The lack of pharmacokinetic data warrant that extra care be used when administering chlorobutanol-containing products to patients with hepatic or renal dysfunction. Patients should be monitored for possible increased somnolence, alterations in speech pattern, dysarthria, and hemodynamic changes. Chlorobutanol toxicity should be ruled out by serum analysis if the patient exhibits any of the above reactions.
In Vivo Evaluation of the Oral Toxicity of the Chlorobutanol
Toxics 2022 Jan 7;10(1):24.PMID:35051066DOI:10.3390/toxics10010024.
Chlorobutanol (CB) is used as a preservative in cosmetics and has antibacterial activity. This study investigated the single- and repeated-dose 28-day oral toxicity of a CB solvent in Sprague Dawley (SD) rats. For the single-dose oral toxicity study, a dose of 62.5, 125, or 250 mg per kg of body weight (mg/kg b.w.) of CB was given once orally via gavage. For the repeated-dose 28-day toxicity study, the high dose was set as 100 mg/kg b.w./day, and the middle, middle-low, and low doses were set to 50, 25, and 12.5 mg/kg b.w./day, respectively. Body weight was not significantly changed in the repeated-dose toxicity study. Relative liver and kidney weights were significantly increased in both sexes of the 100 mg/kg b.w./day treatment group. However, there were histopathological changes in liver and kidney for females and males, respectively. These data suggested that the approximate lethal dose (ALD) of CB was over 250 mg/kg b.w./day in the single-dose study, and the no adverse effect level (NOAEL) for CB was over 50 and 12.5 mg/kg b.w./day for female and male rats in the repeated-dose toxicity study.
Chlorobutanol, a preservative of desmopressin, inhibits human platelet aggregation and release in vitro
Thromb Haemost 1990 Nov 30;64(3):473-7.PMID:2096493doi
Therapeutic preparations of desmopressin for parenteral use contain the preservative Chlorobutanol (5 mg/ml). We show here that Chlorobutanol is a potent inhibitor of platelet aggregation and release. It exhibited a significant inhibitory activity toward several aggregation inducers in a concentration- and time-dependent manner. Thromboxane B2 formation, ATP release, and elevation of cytosolic free calcium caused by collagen, ADP, epinephrine, arachidonic acid and thrombin respectively were markedly inhibited by Chlorobutanol. Chlorobutanol had no effect on elastase-treated platelets and its antiplatelet effect could be reversed. It is concluded that the antiplatelet effect of Chlorobutanol is mainly due to its inhibition on the arachidonic acid pathway but it is unlikely to have a nonspecific toxic effect. This antiplatelet effect of Chlorobutanol suggests that desmopressin, when administered for improving hemostasis, should not contain Chlorobutanol as a preservative.
Effects of Chlorobutanol on primary and secondary endings of isolated cat muscle spindles
Brain Res 2000 Jan 31;854(1-2):106-21.PMID:10784112DOI:10.1016/s0006-8993(99)02325-2.
The effects of the preservative Chlorobutanol on primary and secondary endings of muscle spindles isolated from the tenuissimus muscle of the cat were investigated in this study. Chlorobutanol was applied to the bathing solution in final concentrations of between 10 and 100 microg/ml. It induced a reversible and dose dependent decrease in the discharge frequency of both types of ending without any visible length change in the sensory region of the receptor. The initial activity, the peak dynamic discharge, the maximum static discharge value and the final static discharge value were evaluated from an ending's discharge pattern obtained during ramp-and-hold stretches. These four basic discharge frequencies decreased in parallel with increasing concentrations of Chlorobutanol. Their sensitivities to Chlorobutanol were similar (mean values: -0.11 to -0.29 imp/s per microg/ml Chlorobutanol) and were independent of the amplitude of stretch. The dynamic response and the static response of both primary and secondary endings remained unchanged, indicating that the sensitivity of the spindle to stretch was not influenced by Chlorobutanol. Chlorobutanol also reduced the discharge activity of the muscle spindle afferents during sinusoidal stretches. The amplitude of the receptor potential (AC component) remained unchanged under Chlorobutanol. With the available recording technique it was not possible to measure slow shifts of the membrane potential. However, a hyperpolarization of the ending's membrane might explain why the afferent discharge frequency is reduced by Chlorobutanol. The calcium dynamics of the spindle do not appear to be altered by CB, as the effect exerted on the afferent discharge by a change in the extracellular calcium concentration and a blockage of calcium channels was different from the CB effect. As the inhibitory effect of CB was reduced by ouabain, it is possible that CB activates the electrogenic Na/K pump or affects a mechanism that is closely related to the activity of the pump. The properties of the axonal membrane appear not to be altered, as Chlorobutanol did not change the shape of action potentials.
Effects of Chlorobutanol and bradykinin on myocardial excitation
Am J Physiol 1976 Feb;230(2):306-10.PMID:1083146DOI:10.1152/ajplegacy.1976.230.2.306.
The negative inotropic effect of a commonly used formulation of bradykinin (Sandoz BRS-640) was found to be due to Chlorobutanol, a constituent of the preparation. Solutions containing up to 100 mug of crystalline bradykinin/ml had no effect on tension or action-potential shape. Chlorobutanol (500 mug/ml) caused a 30% decrease in contraction amplitude and a 20% increase in action-potential duration. Chlorobutanol lowered conduction velocity and induced conduction failure and automaticity within isolated ventricular muscle strips. Chlorobutanol affected neither positive nor negative treppe. We conclude that bradykinin has no direct action on toad, frog, or rat myocardium. However, Chlorobutanol does have direct effects on myocardial cells, acting on the cell membrane and decreasing isometric tension produced by the heart.