6108-05-0

• 常用中文名：盐酸利多卡因
• 常用英文名：Lidocaine HCl
• CAS号：6108-05-0
• 分子式：C₁₄H₂₅ClN₂O₂
• 分子量：288.814
• 相关类别： 原料药 Anesthetic Agents Local anesthetics
• 发布时间：2018-09-16 17:40:26
• 更新时间：2024-01-02 23:43:56
• 水合盐酸利多卡因(盐酸利多卡因水合物)抑制涉及复杂电压和使用依赖性的钠通道。水合盐酸利多卡因通过上调miR-145表达和进一步失活MEK/ERK和NF-κB信号通路,减少胃癌细胞的生长、迁移和侵袭。盐酸利多卡因水合物是一种酰胺衍生物,具有研究室性心律失常的潜力[1][2]。

名称

• 中文名: 盐酸利多卡因
• 英文名: lidocaine hydrochloride monohydrate
• 中文别名: 利多卡因 HCL; 利多卡因 HCL; N-二乙基氨基乙酰基-2,6-二甲基苯胺盐酸盐一水合物; 盐酸利多卡因一水合物
• 英文别名: 2-(diéthylamino)-N-(2,6-diméthylphényl)acétamide chlorhydrate hydrate; Xyloneural; MFCD00150329; 2-(Diethylamino)-2',6'-acetoxylidide Hydrochloride Hydrate; Lidocaine Hydrochloride Monohydrate; Lidocaine hydrochloride anhydrous; 2-(diethylamino)-N-(2,6-dimethylphenyl)acetamide hydrochloride hydrate; 2-(Diethylamino)-N-(2,6-dimethylphenyl)acetamidhydrochloridhydrat; Acetamide, 2-(diethylamino)-N-(2,6-dimethylphenyl)-, hydrochloride, hydrate (1:1:1); EINECS 200-803-8; Xylocard; N-(2,6-Dimethylphenyl)-N,N-diethylglycinamide hydrochloride hydrate; Linocaine hydrochloride; 2-(Diethylamino)-N-(2,6-dimethylphenyl)acetamide Monohydrochloride Monohydrate; Lidocaine HCl

物化性质

• 沸点: 350.8ºC at 760 mmHg
• 熔点: 68.5ºC
• 分子式: C₁₄H₂₅ClN₂O₂
• 分子量: 288.814
• 闪点: 166ºC
• 精确质量: 288.160461
• PSA: 41.57000
• LogP: 3.39440
• 外观性状: 固体
• 储存条件: 室温，干燥
• 水溶解性: H2O: soluble

生物活性

• 描述: 水合盐酸利多卡因(盐酸利多卡因水合物)抑制涉及复杂电压和使用依赖性的钠通道。水合盐酸利多卡因通过上调miR-145表达和进一步失活MEK/ERK和NF-κB信号通路,减少胃癌细胞的生长、迁移和侵袭。盐酸利多卡因水合物是一种酰胺衍生物,具有研究室性心律失常的潜力[1][2]。
• 相关类别:
  信号通路 >> 跨膜转运 >> 钠通道
  信号通路 >> 细胞凋亡 >> 细胞凋亡
  研究领域 >> 癌症
  信号通路 >> MAPK/ERK信号通路 >> MEK
  研究领域 >> 心血管疾病
  信号通路 >> MAPK/ERK信号通路 >> ERK
  信号通路 >> 干细胞及 Wnt 通路 >> ERK
• 靶点:

  ERK

  NF-κB

  MEK

• 体外研究: 利多卡因(利多卡因)(10 nM；48小时)显著减少细胞增殖[2]。利多卡因(1-10 nM；24-72小时)抑制细胞活力,在10%浓度下达到最大抑制效果 nM和治疗时间48 小时[2]。利多卡因(10 nM；48小时)显著增加凋亡细胞率[2]。利多卡因(10 nM；48小时)显著下调细胞周期蛋白D1,上调p21表达[2]。细胞增殖试验[2]细胞系：人胃癌细胞系MKN45浓度：10 nM培养时间：48小时结果：细胞增殖明显减少。细胞活力测定[2]细胞系：人胃癌细胞系MKN45浓度：1、5和10 nM培养时间：24、48、72小时结果：抑制MKN45细胞活力。凋亡分析[2]细胞系：人胃癌细胞系MKN45浓度：10 nM孵育时间：48h结果：明显提高凋亡细胞率。Western Blot分析[2]细胞系：人胃癌细胞系MKN45浓度：10 nM孵育时间：48小时结果：细胞周期蛋白D1显著下调,p21表达显著上调。
• 体内研究: 利多卡因可导致大鼠完全可逆的尾神经阻滞。与热伤害性阻滞相比,利多卡因产生的机械伤害性阻滞起效较慢,恢复更快[3]。
• 参考文献:

  [1]. Cummins TR, et al. Setting up for the block: the mechanism underlying lidocaine's use-dependent inhibition of sodium channels. J Physiol. 2007 Jul 1;582(Pt 1):11.

  [2]. Sui H, et al. Lidocaine inhibits growth, migration and invasion of gastric carcinoma cells by up-regulation of miR-145. BMC Cancer. 2019 Mar 15;19(1):233.

  [3]. Li Z, et al. Evaluation of the antinociceptive effects of lidocaine and bupivacaine on the tail nerves of healthy rats. Basic Clin Pharmacol Toxicol. 2013 Jul;113(1):31-6.

MSDS

Section 1. Chemical Product and Company Identification Lidocaine Hydrochloride monohydrate Common Name/ Trade Name Lidocaine Hydrochloride monohydrate Section 4. First Aid Measures Eye ContactCheck for and remove any contact lenses. In case of contact, immediately flush eyes with plenty of water for at least 15 minutes. Cold water may be used. Get medical attention if irritation occurs. Skin ContactWash with soap and water. Cover the irritated skin with an emollient. Get medical attention if irritation develops. Cold water may be used. Serious Skin ContactNot available. InhalationIf inhaled, remove to fresh air. If not breathing, give artificial respiration. If breathing is difficult, give oxygen. Get medical attention. Serious InhalationNot available. IngestionDo NOT induce vomiting unless directed to do so by medical personnel. Never give anything by mouth to an unconscious person. If large quantities of this material are swallowed, call a physician immediately. Loosen tight clothing such as a collar, tie, belt or waistband. Serious IngestionNot available. Section 5. Fire and Explosion Data Flammability of the Product May be combustible at high temperature. Auto-Ignition Temperature Not available. Flash PointsNot available. Flammable LimitsNot available. Products of CombustionThese products are carbon oxides (CO, CO2), nitrogen oxides (NO, NO2...), halogenated compounds. Fire Hazards in Presence of Slightly flammable to flammable in presence of heat. Various Substances Explosion Hazards in Presence Risks of explosion of the product in presence of mechanical impact: Not available. of Various SubstancesRisks of explosion of the product in presence of static discharge: Not available. Fire Fighting MediaSMALL FIRE: Use DRY chemical powder. and InstructionsLARGE FIRE: Use water spray, fog or foam. Do not use water jet. Special Remarks onAs with most organic solids, fire is possible at elevated temperatures Fire Hazards Special Remarks on Explosion Fine dust dispersed in air in sufficient concentrations, and in the presence of an ignition source is a potential Hazardsdust explosion hazard. Section 6. Accidental Release Measures Small SpillUse appropriate tools to put the spilled solid in a convenient waste disposal container. Finish cleaning by spreading water on the contaminated surface and dispose of according to local and regional authority requirements. Large SpillUse a shovel to put the material into a convenient waste disposal container. Finish cleaning by spreading water on the contaminated surface and allow to evacuate through the sanitary system. Section 7. Handling and Storage Keep away from heat. Keep away from sources of ignition. Ground all equipment containing material. Do not Precautions ingest. Do not breathe dust. Wear suitable protective clothing. If ingested, seek medical advice immediately and show the container or the label. Keep away from incompatibles such as oxidizing agents. StorageKeep container tightly closed. Keep container in a cool, well-ventilated area. Lidocaine Hydrochloride monohydrate Section 8. Exposure Controls/Personal Protection Engineering ControlsUse process enclosures, local exhaust ventilation, or other engineering controls to keep airborne levels below recommended exposure limits. If user operations generate dust, fume or mist, use ventilation to keep exposure to airborne contaminants below the exposure limit. Personal ProtectionSafety glasses. Lab coat. Dust respirator. Be sure to use an approved/certified respirator or equivalent. Gloves. Personal Protection in Case of Splash goggles. Full suit. Dust respirator. Boots. Gloves. A self contained breathing apparatus should be a Large Spillused to avoid inhalation of the product. Suggested protective clothing might not be sufficient; consult a specialist BEFORE handling this product. Exposure LimitsNot available. Section 9. Physical and Chemical Properties Physical state and appearance Solid. (crystalline powder.)OdorOdorless. TasteNot available. Molecular Weight288.81 g/mole ColorWhite. pH (1% soln/water)Not available. Not available. Boiling Point Melting Point74°C (165.2°F) Critical TemperatureNot available. Specific GravityNot available. Vapor PressureNot applicable. Vapor DensityNot available. VolatilityNot available. Not available. Odor Threshold Water/Oil Dist. Coeff.Not available. Ionicity (in Water)Not available. Dispersion PropertiesSee solubility in water. SolubilityEasily soluble in cold water. Insoluble in diethyl ether. Soluble in benzene, ethanol, chloroform Section 10. Stability and Reactivity Data The product is stable. Stability Instability TemperatureNot available. Excess heat, incompatible materials Conditions of Instability Incompatibility with variousReactive with oxidizing agents. substances CorrosivityNon-corrosive in presence of glass. Special Remarks onNot available. Reactivity Special Remarks onNot available. Corrosivity PolymerizationWill not occur. Lidocaine Hydrochloride monohydrate Section 11. Toxicological Information Routes of EntryAbsorbed through skin. Inhalation. Ingestion. Toxicity to AnimalsAcute oral toxicity (LD50): 292 mg/kg [Mouse]. Chronic Effects on HumansCauses damage to the following organs: the nervous system. May cause damage to the following organs: cardiovascular system, central nervous system (CNS). Other Toxic Effects onHazardous in case of ingestion. HumansSlightly hazardous in case of skin contact (irritant), of inhalation. Special Remarks onNot available. Toxicity to Animals Special Remarks on May cause adverse reproductive effects and birth defects (teratogenic) based on animal test data Chronic Effects on Humans Special Remarks on otherAute Potential Health Effects: Toxic Effects on HumansSkin: May cause skin irritation and numbness (anesthetic effect). When applied to the skin, it produces an anesthetic effect by blocking the signals at the nerve endings of the skin. when compounded with an ointment and applied topically, It may be absorbed by the skin cause systemic effects similar to that of ingestion. Eyes: May cause eye irritation and numbness. Inhalation: Dust may cause respiratory tract irritation and numbness. Ingestion: Harmful of swallowed. May cause abdominal discomfort, nausea, vomiting. May affect behavior/central nervous system (convulsions/seizures, drowsiness, lightheadedness, dizziness, confusion, disorientation, muscle twitching or trembling, somnolence, unusual excitement, unusual tiredness or weakness, nervousness, restlessness), cardiovascular system (hypotension, change in heart rate with possibe cardiac arrest). May also cause shortness of breath or trouble breathing, ringing or buzzing in the ears, feeling hot, cold or numb, increased sweating, blurred or double vision. Chronic Potential Health Effects: Skin: May cause allergic skin reaction with rash, hives, swelling, or abnormal sensation at the site of application. Ingestion/Inhalation: It is rare, but it may cause allergic reaction with cough, difficulty swallowing or tongue swelling, dizziness or fainting, hives or swelling of the eyelids, face or lips; itching or skin rash, stuffy nose, chest tightness, shortness of breath, trouble breathing or wheezing. Medical Conditions Aggravated by Exposure: Hypersensitivity to material; respiratory depression; existing cardiac conditions; broken or inflammed skin, burns, or open wounds at the place of application. More can be absorbed into the body quickly, which increases the chance of side effects; Liver disease (severe). The risk of side effects may be increased because of the slower removal of lidocaine from the body. Section 12. Ecological Information EcotoxicityNot available. BOD5 and CODNot available. Possibly hazardous short term degradation products are not likely. However, long term degradation products Products of Biodegradation may arise. Toxicity of the ProductsThe products of degradation are more toxic. of Biodegradation Not available. Special Remarks on the Products of Biodegradation Section 13. Disposal Considerations Waste must be disposed of in accordance with federal, state and local environmental Waste Disposal control regulations. Lidocaine Hydrochloride monohydrate Section 14. Transport Information DOT ClassificationNot a DOT controlled material (United States). Not applicable. Identification Not applicable. Special Provisions for Transport DOT (Pictograms) Section 15. Other Regulatory Information and Pictograms No products were found. It is not listed on the TSCA inventory because it is a hydrate. Federal and State Regulations California prop. 65: This product contains the following ingredients for which the State of California has California found to cause cancer which would require a warning under the statute: No products were found. Proposition 65 Warnings California prop. 65: This product contains the following ingredients for which the State of California has found to cause birth defects which would require a warning under the statute: No products were found. Other RegulationsOSHA: Hazardous by definition of Hazard Communication Standard (29 CFR 1910.1200). EINECS: This product is not on the European Inventory of Existing Commercial Chemical Substances. Canada: Not listed on Canadian Domestic Substance List (DSL) or Canadian Non- Domestic Substance List (NDSL). China: Not listed on National Inventory. Japan: Not listed on National Inventory (ENCS). Korea: Not listed on National Inventory (KECI). Philippines: Not listed on National Inventory (PICCS). Australia: Not listed on AICS. WHMIS (Canada) Not available under WHMIS (Canada). Other Classifications DSCL (EEC)R22- Harmful if swallowed.S36- Wear suitable protective clothing. S46- If swallowed, seek medical advice immediately and show this container or label. Health Hazard HMIS (U.S.A.)2 National Fire Protection 1 Flammability 1 Association (U.S.A.) Fire Hazard 2 0 Reactivity Health Reactivity 0 Specific hazard Personal Protection E WHMIS (Canada) (Pictograms) DSCL (Europe) (Pictograms) TDG (Canada) (Pictograms) Lidocaine Hydrochloride monohydrate ADR (Europe) (Pictograms) Protective Equipment Gloves. Lab coat. Dust respirator. Be sure to use an approved/certified respirator or equivalent. SECTION 16 - ADDITIONAL INFORMATION N/A

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : AN7700000 CHEMICAL NAME : 2',6'-Acetoxylidide, 2-(diethylamino)-, hydrochloride, hydrate CAS REGISTRY NUMBER : 6108-05-0 LAST UPDATED : 199706 DATA ITEMS CITED : 1 MOLECULAR FORMULA : C14-H22-N2-O.Cl-H.H2-O MOLECULAR WEIGHT : 288.86 WISWESSER LINE NOTATION : 2N2&1VMR B1 F1 &GH &QH HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 292 mg/kg TOXIC EFFECTS : Behavioral - convulsions or effect on seizure threshold REFERENCE : JPETAB Journal of Pharmacology and Experimental Therapeutics. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1909/10- Volume(issue)/page/year: 179,580,1971

安全

• 符号: GHS06
• 信号词: Danger
• 危害声明: H301
• 警示性声明: P301 + P310
• 个人防护装备: dust mask type N95 (US);Eyeshields;Faceshields;Gloves
• 危害码 (欧洲): Xn: Harmful;
• 风险声明 (欧洲): 22
• 安全声明 (欧洲): 36
• 危险品运输编码: UN 2811 6
• WGK德国: 3
• RTECS号: AN7700000
• 海关编码: 2924299090

海关

海关编码	2924299090
中文概述	2924299090. 其他环酰胺（包括环氨基甲酸酯）（包括其衍生物以及他们的盐）. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:30.0%
申报要素	品名, 成分含量, 用途, 包装
Summary	2924299090. other cyclic amides (including cyclic carbamates) and their derivatives; salts thereof. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%