前往化源商城

入驻化源商城

品牌现货直购

上海化源世纪贸易有限公司
上海市上海市普陀区
产品名：Azelastine
纯度：99.35%
规格：
联系人：徐经理
联系电话：13311869306

上海阿拉丁生化科技股份有限公司
上海市上海市浦东新区
产品名：Azelastine
纯度：98.0%
规格：100mg/200mg/1g/1g
联系人：阿拉丁
联系电话：400-620-6333

上海创赛科技有限公司
上海市上海市嘉定区
产品名：[Perfemiker]Azelastine,98%
纯度：98.0%
规格：100mg/200mg/1g
联系人：夏言
联系电话：18016376636

查看所有供应商和价格请点击：

58581-89-8生产厂家

58581-89-8价格

58581-89-8

58581-89-8结构式

常用中文名：盐酸氮卓斯汀
常用英文名：Azelastine
CAS号：58581-89-8
分子式：C₂₂H₂₄ClN₃O
分子量：381.898
相关类别：原料药抗变态反应药抗组胺药
发布时间：2018-04-25 08:00:00
更新时间：2024-01-08 09:20:08
Azelastine是第二代H1受体拮抗剂。

化源商城直购

中文名	氮卓斯汀
英文名	azelastine
中文别名	4-[(4-氯苯基)甲基]-2-(六氢-1-甲基-1H-氮杂卓-4-基)-1(2H)-酞嗪酮 4-[(4-氯苯基)甲基]-2-(六氢-1-甲基-1H-氮杂卓)二氮杂萘酮氮卓司丁 4-[(4-氯苯基)甲基]-2-(六氢-1-甲基-1H-氮杂卓-4-基)二氮杂萘酮盐酸氮卓斯汀
英文别名	UNII:ZQI909440X 4-(4-Chlorobenzyl)-2-(1-methyl-4-azepanyl)-1(2H)-phthalazinone 1(2H)-Phthalazinone, 4-[(4-chlorophenyl)methyl]-2-(hexahydro-1-methyl-1H-azepin-4-yl)- Optilast 4-(p-Chlorobenzyl)-2-(N-methylperhydroazepin-4-yl)-1(2H)-phthalazinone Allergodil 4-[(4-chlorophenyl)methyl]-2-(1-methylazepan-4-yl)phthalazin-1(2H)-one Azelastine 4-[(4-Chlorophenyl)methyl]-2-(hexahydro-1-methyl-1H-azepin-4-yl)-1(2H)-phthalazinone 4-(4-Chlorobenzyl)-2-(1-methylazepan-4-yl)phthalazin-1(2H)-one Rhinolast MFCD00242781 4-(p-Chlorobenzyl)-2-(hexahydro-1-methyl-1H-azepin-4-yl)-1(2H)-phthalazinone

描述	Azelastine是第二代H1受体拮抗剂。
相关类别	信号通路 >> G 蛋白偶联受体/G 蛋白 >> 组胺受体信号通路 >> 免疫及炎症 >> 组胺受体研究领域 >> 炎症/免疫
参考文献	[1]. Kempuraj, D., et al., Azelastine is more potent than olopatadine n inhibiting interleukin-6 and tryptase release from human umbilical cord blood-derived cultured mast cells. Ann Allergy Asthma Immunol, 2002. 88(5): p. 501-6. [2]. Canonica, G.W., et al., Topical azelastine in perennial allergic conjunctivitis. Curr Med Res Opin, 2003. 19(4): p. 321-9. [3]. Lieberman, P., M.A. Kaliner, and W.J. Wheeler, Open-label evaluation of azelastine nasal spray in patients with seasonal allergic rhinitis and nonallergic vasomotor rhinitis. Curr Med Res Opin, 2005. 21(4): p. 611-8.

密度	1.3±0.1 g/cm3
沸点	533.9±60.0 °C at 760 mmHg
分子式	C₂₂H₂₄ClN₃O
分子量	381.898
闪点	276.7±32.9 °C
精确质量	381.160797
PSA	38.13000
LogP	3.71
外观性状	白色晶体粉末
蒸汽压	0.0±1.4 mmHg at 25°C
折射率	1.642
储存条件	贮藏在密闭容器内，在干燥，阴凉处保存
稳定性	单水合物：从乙醇-水结晶。可鉴定出两种不同的晶型。盐酸氮革斯汀(Azelastine Hydrochloride)：C22H24ClN3O?HCl。[79307-93-0]。白色结晶性粉末，无臭，味苦。溶于氯仿、二氯甲烷或冰醋酸，略溶于甲醇，微溶于无水乙醇或水，不溶于丙酮或乙醚。熔点225～229℃。急性毒性LD₅₀雄、雌小鼠，雄、雌大鼠，雄、雌豚鼠(mg/kg)：124，139，310，417，126，130口服；36.5，35.5，26.9，30.3，23.0，24.8静脉注射；597.0，57.2，143.0，115.0，46.2，52.2肌肉注射；63.0，54.2，66.5，59.6。41.0．37.3皮下注射。
分子结构	1、摩尔折射率：109.97 2、摩尔体积（cm³/mol）：304.5 3、等张比容（90.2K）：799.5 4、表面张力（dyne/cm）：47.4 5、极化率（10^-24cm³）：43.59
计算化学	1.疏水参数计算参考值（XlogP）:4.4 2.氢键供体数量:0 3.氢键受体数量:3 4.可旋转化学键数量:3 5.互变异构体数量:无 6.拓扑分子极性表面积35.9 7.重原子数量:27 8.表面电荷:0 9.复杂度:558 10.同位素原子数量:0 11.确定原子立构中心数量:0 12.不确定原子立构中心数量:1 13.确定化学键立构中心数量:0 14.不确定化学键立构中心数量:0 15.共价键单元数量:1
更多	1. 性状：油状物 2. 密度（g/cm³,20℃）：未确定 3. 相对蒸汽密度（g/mL,空气=1）：未确定 4. 熔点（ºC）：未确定 5. 沸点（ºC,0.01mmHg）：未确定 6. 沸点（ºC,5.2kPa）：未确定 7. 折射率（°）：未确定 8. 闪点（℉）：未确定 9. 比旋光度（º）：未确定 10. 自燃点或引燃温度（ºC）：未确定 11. 蒸气压（kPa,25ºC）：未确定 12. 饱和蒸气压（kPa,60ºC）：未确定 13. 燃烧热（KJ/mol）：未确定 14. 临界温度（ºC）：未确定 15. 临界压力（KPa）：未确定 16. 油水（辛醇/水）分配系数的对数值：未确定 17. 爆炸上限（%,V/V）：未确定 18. 爆炸下限（%,V/V）：未确定 19. 溶解性（mg/mL）：溶于二氯甲烷

生态学数据:

对水是稍微危害的，若无政府许可，勿将材料排入周围环境

CHEMICAL IDENTIFICATION

RTECS NUMBER :: TH9203800

CHEMICAL NAME :: 1(2H)-Phthalazinone, 4-((4-chlorophenyl)methyl)-2-(hexahydro-1-methyl-1H-a zepin-4-yl)-

CAS REGISTRY NUMBER :: 58581-89-8

LAST UPDATED :: 199612

DATA ITEMS CITED :: 12

MOLECULAR FORMULA :: C22-H24-Cl-N3-O

MOLECULAR WEIGHT :: 381.94

WISWESSER LINE NOTATION :: T66 BVNNJ E1R DG& C- DT7NTJ A1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 310 mg/kg

TOXIC EFFECTS :: Peripheral Nerve and Sensation - flaccid paralysis without anesthesia (usually neuromuscular blockage) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - other changes

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 31,1184,1981

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 43200 ug/kg

TOXIC EFFECTS :: Peripheral Nerve and Sensation - flaccid paralysis without anesthesia (usually neuromuscular blockage) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - other changes

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 31,1184,1981

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 59600 ug/kg

TOXIC EFFECTS :: Peripheral Nerve and Sensation - flaccid paralysis without anesthesia (usually neuromuscular blockage) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - other changes

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 31,1184,1981

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 26900 ug/kg

TOXIC EFFECTS :: Peripheral Nerve and Sensation - flaccid paralysis without anesthesia (usually neuromuscular blockage) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - other changes

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 31,1184,1981

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 115 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 17,1106,1986

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 124 mg/kg

TOXIC EFFECTS :: Peripheral Nerve and Sensation - flaccid paralysis without anesthesia (usually neuromuscular blockage) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - other changes

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 31,1184,1981

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 42800 ug/kg

TOXIC EFFECTS :: Peripheral Nerve and Sensation - flaccid paralysis without anesthesia (usually neuromuscular blockage) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - other changes

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 31,1184,1981

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 54200 ug/kg

TOXIC EFFECTS :: Peripheral Nerve and Sensation - flaccid paralysis without anesthesia (usually neuromuscular blockage) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - other changes

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 31,1184,1981

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 25400 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 17,1106,1986

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 59700 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 17,1106,1986

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 51300 ug/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Behavioral - changes in motor activity (specific assay) Gastrointestinal - nausea or vomiting

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 31,1184,1981

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 13700 ug/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Behavioral - changes in motor activity (specific assay) Gastrointestinal - nausea or vomiting

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 31,1184,1981

危害码 (欧洲)	N-T,N,T
风险声明 (欧洲)	R50/53:Very Toxic to aquatic organisms, may cause long-term adverse effects in the aquatic environment . R23/25:Toxic by inhalation and if swallowed .
安全声明 (欧洲)	S61-S60-S45-S28A-S20/21-S28
危险品运输编码	1557
RTECS号	CY5950000
包装等级	III
危险类别	6.1(b)
海关编码	2933990090

1878-66-6结构式

1878-66-6

~%

58581-89-8结构式

58581-89-8

文献：Archiv der Pharmazie, , vol. 321, # 4 p. 205 - 208

85-44-9结构式

85-44-9

~%

58581-89-8结构式

58581-89-8

文献：Archiv der Pharmazie, , vol. 321, # 4 p. 205 - 208

105279-16-1结构式

105279-16-1

~%

58581-89-8结构式

58581-89-8

文献：Archiv der Pharmazie, , vol. 321, # 4 p. 205 - 208

1859-33-2结构式

1859-33-2

~%

58581-89-8结构式

58581-89-8

文献：Archiv der Pharmazie, , vol. 321, # 4 p. 205 - 208

53242-76-5结构式

53242-76-5

~%

58581-89-8结构式

58581-89-8

文献：Archiv der Pharmazie, , vol. 321, # 4 p. 205 - 208

上游产品 4
1878-66-6 85-44-9 1859-33-2 53242-76-5
下游产品 0

30.6g的对氯苄基苯乙酮-邻-羧酸(I)及16g硫酸肼和9.4g氢氧化钠溶于250ml水的溶液一起加热。洗涤和干燥后，得27g 4-(4-氯苄基)-1-(2H)-酞嗪酮(化合物(Ⅱ))。
将20g的2-(2-氯乙基)-N-甲基四氢吡咯盐酸盐加入4.4g氢氧化钠溶于20ml水的溶液。加热到70℃后，将其滴人加热到70℃的27g的化合物(Ⅱ)的40ml50%氢氧化钠水溶液中。在该温度再加热lh。冷却后，用水稀释，过滤除去不溶物后，溶入二氯甲烷。用稀盐酸进行提取，提取液用氢氧化钾水溶液碱化。析出的油状物再溶入二氯甲烷，干燥，浓缩。粗品的收率在90%以上。转化为盐酸盐后，再重结晶提纯，得盐酸氮革斯汀，熔点225~229℃。

海关编码	2933990090
中文概述	2933990090. 其他仅含氮杂原子的杂环化合物. 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:20.0%
申报要素	品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期
Summary	2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%