氯吡胺盐酸盐 | 6170-42-9

• 物质功能分类: 分析化学 - 标准品 - 法医和兽医标准品
• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: 氯吡胺盐酸盐
• 中文别名: 盐酸氯吡胺；N-(4-氯苄基)-N',N'-二甲基-N-2-吡啶基-1,2-乙二胺盐酸盐；N-对氯苄基-N',N'-二甲基-N-(2-吡啶基)乙二胺；N-(4-氯苄基)-N",N"-二甲基-N-2-吡啶基-1,2-乙二胺盐酸盐
• 英文名称: Chloropyramine hydrochloride
• 英文别名: N'-[(4-chlorophenyl)methyl]-N,N-dimethyl-N'-pyridin-2-ylethane-1,2-diamine;hydron;chloride
• CAS: 6170-42-9
• 化学式: C₁₆H₂₀ClN₃*ClH
• 分子量: 326.269
• InChiKey: VEYWWAGBHABATA-UHFFFAOYSA-N

物化性质

• 熔点：
  172-174°
• 溶解度：
  氯仿（微溶）、甲醇（微溶）、水（微溶）
• 碰撞截面：
  167.9 Ų [M+H]+ [CCS Type: TW, Method: calibrated with polyalanine and drug standards]

计算性质

• 辛醇/水分配系数(LogP)：
  -1.11
• 重原子数：
  21
• 可旋转键数：
  6
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.31
• 拓扑面积：
  20.6
• 氢给体数：
  1
• 氢受体数：
  3

安全信息

• WGK Germany：
  3
• 危险性防范说明：
  P280,P305+P351+P338
• 危险性描述：
  H302,H312,H315,H319,H332
• 储存条件：
  -20℃

SDS

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SECTION 1: Identification of the substance/mixture and of the company/undertaking
Product identifiers
Product name : Chloropyramine hydrochloride
REACH No. : A registration number is not available for this substance as the substance
or its uses are exempted from registration, the annual tonnage does not
require a registration or the registration is envisaged for a later
registration deadline.
CAS-No. : 6170-42-9
Relevant identified uses of the substance or mixture and uses advised against
Identified uses : Laboratory chemicals, Manufacture of substances

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SECTION 2: Hazards identification
Classification of the substance or mixture
Not a hazardous substance or mixture according to Regulation (EC) No. 1272/2008.
This substance is not classified as dangerous according to Directive 67/548/EEC.
Label elements
The product does not need to be labelled in accordance with EC directives or respective national laws.
Other hazards - none

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SECTION 3: Composition/information on ingredients
Substances
: N-p-Chlorobenzyl-N′,N′-dimethyl-N-(2-pyridyl)ethylenediamine
Synonyms
Formula : C16H20ClN3 · HCl
Molecular Weight : 326,26 g/mol
CAS-No. : 6170-42-9
EC-No. : 228-216-2
No components need to be disclosed according to the applicable regulations.

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SECTION 4: First aid measures
Description of first aid measures
If inhaled
If breathed in, move person into fresh air. If not breathing, give artificial respiration.
In case of skin contact
Wash off with soap and plenty of water.
In case of eye contact
Flush eyes with water as a precaution.
If swallowed
Never give anything by mouth to an unconscious person. Rinse mouth with water.
Most important symptoms and effects, both acute and delayed
The most important known symptoms and effects are described in the labelling (see section 2.2) and/or in
section 11
Indication of any immediate medical attention and special treatment needed
no data available

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SECTION 5: Firefighting measures
Extinguishing media
Suitable extinguishing media
Use water spray, alcohol-resistant foam, dry chemical or carbon dioxide.
Special hazards arising from the substance or mixture
Carbon oxides, nitrogen oxides (NOx), Hydrogen chloride gas
Advice for firefighters
Wear self contained breathing apparatus for fire fighting if necessary.
Further information
no data available

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SECTION 6: Accidental release measures
Personal precautions, protective equipment and emergency procedures
Avoid dust formation. Avoid breathing vapours, mist or gas.
For personal protection see section 8.
Environmental precautions
Do not let product enter drains.
Methods and materials for containment and cleaning up
Sweep up and shovel. Keep in suitable, closed containers for disposal.
Reference to other sections
For disposal see section 13.

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SECTION 7: Handling and storage
Precautions for safe handling
Provide appropriate exhaust ventilation at places where dust is formed.Normal measures for preventive fire
protection.
For precautions see section 2.2.
Conditions for safe storage, including any incompatibilities
Store in cool place. Keep container tightly closed in a dry and well-ventilated place.
Specific end use(s)
Apart from the uses mentioned in section 1.2 no other specific uses are stipulated

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SECTION 8: Exposure controls/personal protection
Control parameters
Components with workplace control parameters
Exposure controls
Appropriate engineering controls
General industrial hygiene practice.
Personal protective equipment
Eye/face protection
Use equipment for eye protection tested and approved under appropriate government standards
such as NIOSH (US) or EN 166(EU).
Skin protection
Handle with gloves. Gloves must be inspected prior to use. Use proper glove removal technique
(without touching glove's outer surface) to avoid skin contact with this product. Dispose of
contaminated gloves after use in accordance with applicable laws and good laboratory practices.
Wash and dry hands.
The selected protective gloves have to satisfy the specifications of EU Directive 89/686/EEC and
the standard EN 374 derived from it.
Body Protection
Choose body protection in relation to its type, to the concentration and amount of dangerous
substances, and to the specific work-place., The type of protective equipment must be selected
according to the concentration and amount of the dangerous substance at the specific workplace.
Respiratory protection
Respiratory protection is not required. Where protection from nuisance levels of dusts are desired,
use type N95 (US) or type P1 (EN 143) dust masks. Use respirators and components tested and
approved under appropriate government standards such as NIOSH (US) or CEN (EU).
Control of environmental exposure
Do not let product enter drains.

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SECTION 9: Physical and chemical properties
Information on basic physical and chemical properties
a) Appearance Form: solid
b) Odour no data available
c) Odour Threshold no data available
d) pH no data available
e) Melting point/freezing no data available
point
f) Initial boiling point and no data available
boiling range
g) Flash point no data available
h) Evapouration rate no data available
i) Flammability (solid, gas) no data available
j) Upper/lower no data available
flammability or
explosive limits
k) Vapour pressure no data available
l) Vapour density no data available
m) Relative density no data available
n) Water solubility no data available
o) Partition coefficient: n- no data available
octanol/water
p) Auto-ignition no data available
temperature
q) Decomposition no data available
temperature
r) Viscosity no data available
s) Explosive properties no data available
t) Oxidizing properties no data available
Other safety information
no data available

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SECTION 10: Stability and reactivity
Reactivity
no data available
Chemical stability
Stable under recommended storage conditions.
Possibility of hazardous reactions
no data available
Conditions to avoid
no data available
Incompatible materials
no data available
Hazardous decomposition products
Other decomposition products - no data available
In the event of fire: see section 5

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SECTION 11: Toxicological information
Information on toxicological effects
Acute toxicity
no data available
Skin corrosion/irritation
no data available
Serious eye damage/eye irritation
no data available
Respiratory or skin sensitisation
no data available
Germ cell mutagenicity
no data available
Carcinogenicity
IARC: No component of this product present at levels greater than or equal to 0.1% is identified as
probable, possible or confirmed human carcinogen by IARC.
Reproductive toxicity
no data available
Specific target organ toxicity - single exposure
no data available
Specific target organ toxicity - repeated exposure
no data available
Aspiration hazard
no data available
Additional Information
RTECS: Not available
To the best of our knowledge, the chemical, physical, and toxicological properties have not been
thoroughly investigated.

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SECTION 12: Ecological information
Toxicity
no data available
Persistence and degradability
no data available
Bioaccumulative potential
no data available
Mobility in soil
no data available
Results of PBT and vPvB assessment
PBT/vPvB assessment not available as chemical safety assessment not required/not conducted
Other adverse effects
no data available

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SECTION 13: Disposal considerations
Waste treatment methods
Product
Offer surplus and non-recyclable solutions to a licensed disposal company.
Contaminated packaging
Dispose of as unused product.

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SECTION 14: Transport information
UN number
ADR/RID: - IMDG: - IATA: -
UN proper shipping name
ADR/RID: Not dangerous goods
IMDG: Not dangerous goods
IATA: Not dangerous goods
Transport hazard class(es)
ADR/RID: - IMDG: - IATA: -
Packaging group
ADR/RID: - IMDG: - IATA: -
Environmental hazards
ADR/RID: no IMDG Marine pollutant: no IATA: no
Special precautions for user
no data available

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SECTION 15: Regulatory information
This safety datasheet complies with the requirements of Regulation (EC) No. 1907/2006.
Safety, health and environmental regulations/legislation specific for the substance or mixture
no data available
Chemical Safety Assessment
For this product a chemical safety assessment was not carried out

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SECTION 16: Other information
Further information
Copyright 2014 Co. LLC. License granted to make unlimited paper copies for internal use
only.
The above information is believed to be correct but does not purport to be all inclusive and shall be
used only as a guide. The information in this document is based on the present state of our knowledge
and is applicable to the product with regard to appropriate safety precautions. It does not represent any
guarantee of the properties of the product. Corporation and its Affiliates shall not be held
liable for any damage resulting from handling or from contact with the above product. See
and/or the reverse side of invoice or packing slip for additional terms and conditions of sale.

制备方法与用途

生物活性

氯吡拉明盐酸盐是一种组胺受体 H1 (histamine receptor H1) 拮抗剂，还能抑制 VEGFR-3 和 FAK 的生化功能。

靶点

| VEGFR-3 |

体外研究

BT474 细胞对氯吡拉明盐酸盐（化合物1）非常敏感，在1 µM 浓度下处理48小时后，细胞活力减少了40%。与对照 MCF7-pcDNA3 细胞相比，表达 VEGFR-3 的 MCF7-VEGFR-3 细胞在1 µM 浓度下的存活率显著较高（P<0.01）。而在 10 µM 浓度下，这种差异增大至两倍（P<0.001）。继续用氯吡拉明盐酸盐处理 BT474 细胞会导致细胞增殖浓度依赖性降低。在48小时的持续治疗后，高表达 VEGFR-3 的乳腺癌细胞会发生凋亡。该效应剂量依赖，在 10 µM 浓度下氯吡拉明盐酸盐可诱导超过60%的 BT474 细胞凋亡。在我们的模型细胞系 MCF7-pcDNA3 和 MCF7-VEGFR-3 中，用10 µM 氯吡拉明盐酸盐处理48小时会导致过表达 VEGFR-3 的细胞线中凋亡细胞死亡增加四倍（分别为 18% 对 76%）。

体内研究

氯吡拉明盐酸盐在两种模型系统中都显著减少了肿瘤生长，治疗组的肿瘤大小约为对照组的20%。多柔比星以3 mg/kg剂量给药可减少约60%的肿瘤生长，但在0和3 mg/kg剂量下没有效果。相比之下，氯吡拉明盐酸盐单用可降低约50%的肿瘤生长。低剂量氯吡拉明盐酸盐与多柔比星联合使用具有持久的抗肿瘤作用（85%的肿瘤生长抑制），且效果优于两种药物单独使用。

化学性质

类白色至白色结晶性粉末，熔点168-172℃。

用途

抗过敏药。

用途

抗过敏原料药。

反应信息

• 作为反应物：
  描述：

  氯吡胺盐酸盐 在 盐酸 作用下， 反应 0.17h， 生成 chloropyramine tetrachlorocuprate(II)
  参考文献：
  名称：

  Chloropyramine Tetrachlorocuprate(II)

  摘要：

  The crystal structure of N-(4-chlorobenzyl)-N',N'-dimethyl-N-(2-pyridinio)-1, 2-ethanediammonium tetrachlorocopper(II), (C16H22ClN3)[CuCl4], contains the dication of chloropyramine, a potent anti-allergic agent effective on H-1-type receptors. The CuCl42- anion exhibits a flattened-tetrahedral geometry. The ammonium H atom is weakly bonded to two Cl atoms of the anion and the pyridyl N atom is involved in a short hydrogen bond to a Cl atom of the anion.

  DOI：

  10.1107/s0108270197002060

文献信息

• METHODS AND COMPOSITIONS FOR TREATING INFECTION
  申请人：UNIVERSITY OF ROCHESTER

  公开号：US20150238473A1

  公开（公告）日：2015-08-27

  Provided herein are compositions and methods for treating or preventing infection.

  本文提供了用于治疗或预防感染的组合物和方法。
• Small molecule toll-like receptor (TLR) antagonists
  申请人：Lipford B. Grayson

  公开号：US20070232622A1

  公开（公告）日：2007-10-04

  The invention provides methods and compositions useful for modulating signaling through Toll-like receptors. The methods involve contacting a TLR-expressing cell with a small molecule having a core structure including at least two rings. Certain of the compounds are 4-primary amino quinolines. Many of the compounds and methods are useful specifically for inhibiting immune stimulation involving at least one of TLR9, TLR8, TLR7, and TLR3. The methods may have use in the treatment of autoimmunity, inflammation, allergy, asthma, graft rejection, graft versus host disease, infection, sepsis, cancer, and immunodeficiency.

  本发明提供了用于调节通过Toll样受体信号传导的方法和组合物。该方法涉及使用一个包含至少两个环的核心结构的小分子接触TLR表达的细胞。其中某些化合物是4-主氨基喹啉。许多化合物和方法特别适用于抑制至少一个TLR9、TLR8、TLR7和TLR3的免疫刺激。该方法可能在治疗自身免疫、炎症、过敏、哮喘、移植排斥、移植物抗宿主病、感染、败血症、癌症和免疫缺陷方面有用。
• An otorhinological drug delivery device
  申请人：Schering Oy

  公开号：EP1438942A1

  公开（公告）日：2004-07-21

  The invention relates to an otorhinological delivery device comprising at least one pharmaceutically active agent. According to the invention the device comprises a core comprising said at least one pharmaceutically active agent wherein said core is made of an elastomer composition selected from the group consisting of poly(dimethylsiloxane), a siloxane-based elastomer comprising 3,3,3-trifluoropropyl groups attached to the Si-atoms of the siloxane units, a siloxane-based elastomer comprising poly(alkylene oxide) groups and mixtures thereof.

  本发明涉及一种包含至少一种药用活性剂的耳鼻喉给药装置。根据本发明，该装置包括一个包含所述至少一种药物活性剂的芯体，其中所述芯体由弹性体组合物制成，该弹性体组合物选自聚（二甲基硅氧烷）、硅氧烷基弹性体（包含连接到硅氧烷单元S原子上的3,3,3-三氟丙基）、硅氧烷基弹性体（包含聚（环氧烷）基团）及其混合物组成的组。
• Pharmaceutical composition for use in medical and veterinary ophthalmology
  申请人：Mitotech SA

  公开号：EP2823814A1

  公开（公告）日：2015-01-14

  The invention relates to pharmaceutics, medicine, in particular to manufacturing and use of pharmaceutical compositions of medicines (ophthalmic preparations) comprising mitochondria-addressed antioxidant and a set of auxiliary substances providing effective treatment for ophtalmological diseases in humans and animals.

  本发明涉及制药学、医学，特别是包含线粒体抗氧化剂和一系列辅助物质的药物组合物（眼科制剂）的制造和使用，可有效治疗人类和动物的眼科疾病。
• THE 5HT AGONIST CLEMIZOLE FOR USE IN TREATING DISORDERS
  申请人：The Regents of the University of California

  公开号：EP3632434A1

  公开（公告）日：2020-04-08

  Provided, inter alia, is the 5HT receptor agonist clemizole, or a pharmaceutically acceptable salt thereof for use in a method for treating an epilepsy disorder.

  本发明特别提供了用于治疗癫痫疾病方法的 5HT 受体激动剂 clemizole 或其药学上可接受的盐。