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奥美沙坦 | 144689-24-7

奥美沙坦
Olmesartan
144689-24-7
C24H26N6O3
446.5016
如需查看该化合物的详细结构式,mol文件,smile,InChi 请点击:奥美沙坦结构式
158781
奥美沙坦价格
简介
Olmesartan (RNH-6270) 是血管紧张素II受体 (AT1R) 拮抗剂,常用于高血压的相关研究。
名称和标识符
MDL MFCD00914967
InChIKey VTRAEEWXHOVJFV-UHFFFAOYSA-N
Inchi 1S/C24H26N6O3/c1-4-7-19-25-21(24(2,3)33)20(23(31)32)30(19)14-15-10-12-16(13-11-15)17-8-5-6-9-18(17)22-26-28-29-27-22/h5-6,8-13,33H,4,7,14H2,1-3H3,(H,31,32)(H,26,27,28,29)
SMILES O([H])C(C([H])([H])[H])(C([H])([H])[H])C1=C(C(=O)O[H])N(C([H])([H])C2C([H])=C([H])C(C3=C([H])C([H])=C([H])C([H])=C3C3N=NN([H])N=3)=C([H])C=2[H])C(C([H])([H])C([H])([H])C([H])([H])[H])=N1
别名信息
- 中文别名 -
  • 奥美沙坦
  • 4-(1-羟基-1-甲基乙基)-2-丙基-1-[2'-(四唑-5-基)苯基]苯基]甲基咪唑-5-羧酸
  • 奥美沙坦EP杂质A
  • 奥美沙坦酯A
  • 奥美沙坦酯EP杂质A
  • 奥美沙坦酸
  • 美沙坦酯杂质A
  • 奥美沙坦标准品
  • 奥美沙坦杂质A
  • 奥美沙坦酯
  • 奥米沙坦
  • 反式双(苄腈)二氯钯(II)
  • 夫西地酸
  • 依替米贝
- 英文别名 -
  • Olmesartan Medoxomil
  • 4-(1-Hydroxy-1-methylethyl)-2-propyl-1-[[2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-1H-imidazole-5-carboxylic acid
  • Olmesartan
  • OIMESARTAN, ENTERPRISE STANDARD
  • Olmesartan Acid
  • 5-(2-hydroxypropan-2-yl)-2-propyl-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]imidazole-4-carboxylic acid
  • CS 088
  • RNH 6270
  • 1-((2'-(1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-4-(2-hydroxypropan-2-yl)-2-propyl-1H-imidazole-5-carboxylic acid
  • 4-(1-Hydroxy-1-methylethyl)-2-propyl-1-[[2′-(2H-tetrazol-5-yl)[1,1′-biphenyl]-4-yl]methyl]-1H-imidazole-5-carboxylic acid
  • Olmesartan Medoxomi I
  • Votum
  • Olme sartan
  • 8W1IQP3U10
  • 4-(2-hydroxypropan-2-yl)-2-propyl-1-({4-[2-(1H-1,2,3,4-tetrazol-5-yl)phenyl]phenyl}methyl)-1H-imidazole-5-carboxylic acid
  • 4-(1-hydroxy-1-methylethyl)-2-propyl-1-{[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl}-1H-imidazole-5-carboxylic acid
  • 4-(1-
  • Olmesartan Medoxomil EP Impurity A
  • RNH-6270
  • Olmesartan acid
  • SMR004703526
  • OLMESARTAN [VANDF]
  • VTRAEEWXHOVJFV-UHFFFAOYSA-N
  • OLMESARTAN MEDOXOMIL IMPURITY A [EP IMPURITY]
  • OLMESARTAN MEDOXOMIL IMPURITY A [EP IMPURITY]
  • HMS3393K12
  • HMS3393K12
  • AC-9385
  • AC-9385
  • DTXSID2040571
  • DTXSID2040571
  • 1-((2'-(2H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-4-(2-hydroxypropan-2-yl)-2-propyl-1H-imidazole-5-carboxylic acid
  • 1-((2'-(2H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-4-(2-hydroxypropan-2-yl)-2-propyl-1H-imidazole-5-carboxylic acid
  • 4-(2-hydroxypropan-2-yl)-2-propyl-1-{[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl}-1H-imidazole-5-carboxylic acid
  • 4-(2-hydroxypropan-2-yl)-2-propyl-1-{[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl}-1H-imidazole-5-carboxylic acid
  • SCHEMBL94037
  • SCHEMBL94037
  • 4-(2-hydroxypropan-2-yl)-2-propyl-1-{[2'-(1H-1,2,3,4-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl]methyl}-1H-imidazole-5-carboxylic acid
  • 4-(1-hydroxy-1-methylethyl)-2-propyl-1-((2'-(1H-tetrazol-5-yl)(1,1'-biphenyl)-4-yl)methyl)-1H-imidazole-5-carboxylic acid
  • 4-(2-hydroxypropan-2-yl)-2-propyl-1-{[2'-(1H-1,2,3,4-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl]methyl}-1H-imidazole-5-carboxylic acid
  • 4-(1-hydroxy-1-methylethyl)-2-propyl-1-((2'-(1H-tetrazol-5-yl)(1,1'-biphenyl)-4-yl)methyl)-1H-imidazole-5-carboxylic acid
  • 4-(1-hydroxy-1-methylethyl)-2-propyl-1-{[2''-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl}-1H-imidazole-5-carboxylic acid
  • 4-(1-hydroxy-1-methylethyl)-2-propyl-1-{[2''-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl}-1H-imidazole-5-carboxylic acid
  • SMR000466337
  • SMR000466337
  • 4-(1-hydroxy-1-methylethyl)-2-propyl-1-{[2''-(1H-tetrazol-5-yl)[1,1''-biphenyl]-4-yl]methyl}-1H-imidazole-5-carboxylic acid
  • 4-(1-hydroxy-1-methylethyl)-2-propyl-1-{[2''-(1H-tetrazol-5-yl)[1,1''-biphenyl]-4-yl]methyl}-1H-imidazole-5-carboxylic acid
  • DB00275
  • DB00275
  • 1ST10402
  • 1ST10402
  • omesartan
  • omesartan
  • 4-(hydroxy-1-methylethyl)-2-propyl-1-{[2'-(1H-tetrazol-5-yl)-1,1'-biphenyl-4-yl]methyl}-1H-imidazole-5-carboxylic acid
  • 4-(hydroxy-1-methylethyl)-2-propyl-1-{[2'-(1H-tetrazol-5-yl)-1,1'-biphenyl-4-yl]methyl}-1H-imidazole-5-carboxylic acid
  • 4-(1-hydroxy-1-methylethyl) -2-propyl-1-{4-[2-(tetrazole -5-yl)phenyl]phenyl}methylimidazole-5-carboxylic acid
  • 4-(1-hydroxy-1-methylethyl) -2-propyl-1-{4-[2-(tetrazole -5-yl)phenyl]phenyl}methylimidazole-5-carboxylic acid
  • Benicar
  • Olmetec
  • Benicar
  • Olmetec
  • Olmesartan [USAN:INN:BAN]
  • Olmesartan [USAN:INN:BAN]
  • 4-(1-hydroxy-1-methylethyl)-2-propyl-1-{[2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl}-1H-imidazole-5-carboxylic acid
  • CS-0576
  • 4-(1-hydroxy-1-methylethyl)-2-propyl-1-{[2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl}-1H-imidazole-5-carboxylic acid
  • MLS000759446
  • CS-0576
  • MLS000759446
  • OLMESARTAN MEDOXOMIL IMPURITY, OLMESARTAN- [USP IMPURITY]
  • OLMESARTAN MEDOXOMIL IMPURITY, OLMESARTAN- [USP IMPURITY]
  • CCG-100868
  • OLMESARTAN [MI]
  • CCG-100868
  • AKOS015900241
  • OLMESARTAN [MI]
  • CCG-269198
  • AKOS015900241
  • NSC 759810
  • CCG-269198
  • NSC 759810
  • Pharmakon1600-01505206
  • Pharmakon1600-01505206
  • DTXCID0020571
  • DTXCID0020571
  • CHEBI:48416
  • CHEBI:48416
  • W-201270
  • W-201270
  • A853148
  • A853148
  • EN300-122328
  • EN300-122328
  • NCGC00246968-01
  • NCGC00246968-01
  • Z1541758605
  • Z1541758605
  • OLMESARTAN [INN]
  • OLMESARTAN [INN]
  • AS-10242
  • AS-10242
  • NC00118
  • NC00118
  • Olmesartan [USAN]
  • Olmesartan [USAN]
  • 1H-Imidazole-5-carboxylic acid, 4-(1-hydroxy-1-methylethyl)-2-propyl-1-[[2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-
  • 1H-Imidazole-5-carboxylic acid, 4-(1-hydroxy-1-methylethyl)-2-propyl-1-[[2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-
  • NCGC00246968-02
  • NCGC00246968-02
  • D05246
  • D05246
  • C21543
  • C21543
  • EC 646-413-5
  • EC 646-413-5
  • s5581
  • s5581
  • NSC-759810
  • NSC-759810
  • MLS001424016
  • MLS001424016
  • HSDB 8214
  • HSDB 8214
  • (5-Methyl-2-oxo-1,3-dioxol-4-yl)methyl 4-(2-hydroxypropan-2-yl)-2-propyl-1-((2'-(2H-tetrazol-5-yl)biphenyl-4-yl)methyl)-1H-imidazole-5-carboxylate
  • (5-Methyl-2-oxo-1,3-dioxol-4-yl)methyl 4-(2-hydroxypropan-2-yl)-2-propyl-1-((2'-(2H-tetrazol-5-yl)biphenyl-4-yl)methyl)-1H-imidazole-5-carboxylate
  • Olmesartan 100 microg/mL in Acetonitrile:Methanol
  • Olmesartan 100 microg/mL in Acetonitrile:Methanol
  • 4-(1-Hydroxy-1-methylethyl)-2-propyl-1-[[2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-1H-imidazole-5-carboxylic acid
  • 4-(1-Hydroxy-1-methylethyl)-2-propyl-1-[[2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-1H-imidazole-5-carboxylic acid
  • L001097
  • L001097
  • O0507
  • O0507
  • 4-(hydroxy-1-methylethyl)-2-propyl-1-((2'-(1H-tetrazol-5-yl)-1,1'-biphenyl-4-yl)methyl)-1H-imidazole-5-carboxylic acid
  • 4-(hydroxy-1-methylethyl)-2-propyl-1-((2'-(1H-tetrazol-5-yl)-1,1'-biphenyl-4-yl)methyl)-1H-imidazole-5-carboxylic acid
  • HMS2051K12
  • HMS2051K12
  • HMS2235O24
  • HMS2235O24
  • MFCD00914967
  • MFCD00914967
  • MLS006011945
  • MLS006011945
  • Diclofenacdiethylamine
  • Diclofenacdiethylamine
  • Olmesartan medoxomil impurity, olmesartan-
  • Olmesartan medoxomil impurity, olmesartan-
  • Olmesartan, >=98% (HPLC)
  • Olmesartan, >=98% (HPLC)
  • 4-(1-hydroxy-1-methylethyl)-2-propyl-1-((2'-(1H-tetrazol-5-yl)biphenyl-4-yl)methyl)-1H-imidazole-5-carboxylic acid
  • 4-(1-hydroxy-1-methylethyl)-2-propyl-1-((2'-(1H-tetrazol-5-yl)biphenyl-4-yl)methyl)-1H-imidazole-5-carboxylic acid
  • OLM
  • OLM
  • 4-(1-hydroxy-1-methylethyl) -2-propyl-1-{4-[2-(tetrazole-5-yl)phenyl]phenyl}methylimidazole-5-carboxylic acid
  • 4-(1-hydroxy-1-methylethyl) -2-propyl-1-{4-[2-(tetrazole-5-yl)phenyl]phenyl}methylimidazole-5-carboxylic acid
  • CHEMBL1516
  • CHEMBL1516
  • 4-(1-Hydroxy-1-methylethyl)-2-propyl-1-[[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl]-1H-imidazole-5-carboxylic Acid (Olmesartan)
  • 4-(1-Hydroxy-1-methylethyl)-2-propyl-1-[[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl]-1H-imidazole-5-carboxylic Acid (Olmesartan)
  • 4-(1-Hydroxy-1-methylethyl)-2-propyl-1-{4-[2-(tetrazol-5-yl)phenyl]phenyl}methylimidazole-5-carboxylic acid
  • 4-(1-Hydroxy-1-methylethyl)-2-propyl-1-{4-[2-(tetrazol-5-yl)phenyl]phenyl}methylimidazole-5-carboxylic acid
  • 4-(1-hydroxy-1-methylethyl)-2-propyl-1-{4-[2-(tetrazole-5-yl)phenyl]phenyl}methylimidazole-5-carboxylic acid
  • 4-(1-hydroxy-1-methylethyl)-2-propyl-1-{4-[2-(tetrazole-5-yl)phenyl]phenyl}methylimidazole-5-carboxylic acid
  • Olmesartan (USAN/INN)
  • Olmesartan (USAN/INN)
  • NS00008999
  • OLMESARTAN [WHO-DD]
  • NS00008999
  • OLMESARTAN [WHO-DD]
  • UNII-8W1IQP3U10
  • UNII-8W1IQP3U10
  • Olmesartan Medoxomil Imp. A (EP)
  • 4-(1-Hydroxy-1-methylethyl)-2-propyl-1-[[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl]-1H-imidazole-5-carboxylic Acid
  • Olmesartan
  • Olmesartan Acid
  • Olmesartan Medoxomil Impurity A
  • Olmesartan Medoxomil Imp. A (EP)
  • 4-(1-Hydroxy-1-methylethyl)-2-propyl-1-[[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl]-1H-imidazole-5-carboxylic Acid
  • Olmesartan
  • Olmesartan Acid
  • Olmesartan Medoxomil Impurity A
  • DE-092
  • DE-092
  • 4-(hydroxy-1-methylethyl)-2-propyl-1-{[2''-(1H-tetrazol-5-yl)-1,1''-biphenyl-4-yl]methyl}-1H-imidazole-5-carboxylic acid
  • 4-(hydroxy-1-methylethyl)-2-propyl-1-{[2''-(1H-tetrazol-5-yl)-1,1''-biphenyl-4-yl]methyl}-1H-imidazole-5-carboxylic acid
  • BDBM50241364
  • BDBM50241364
  • 1H-IMidazole-5-carboxylicacid,4-(1-hydroxy-1-Methylethyl)-2-propyl-1-[[2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]Methyl]-
  • HMS3604J06
  • 1H-IMidazole-5-carboxylicacid,4-(1-hydroxy-1-Methylethyl)-2-propyl-1-[[2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]Methyl]-
  • HMS3604J06
  • 1-((2'-(1H-tetrazol-5-yl)biphenyl-4-yl)methyl)-4-(2-hydroxypropan-2-yl)-2-propyl-1H-imidazole-5-carboxylic acid
  • 1-((2'-(1H-tetrazol-5-yl)biphenyl-4-yl)methyl)-4-(2-hydroxypropan-2-yl)-2-propyl-1H-imidazole-5-carboxylic acid
  • FT-0631169
  • FT-0631169
  • Q421156
  • Q421156
  • NCGC00246968-04
  • NCGC00246968-04
  • BCP12007
  • BCP12007
  • AKOS024458255
  • 144689-24-7
  • AKOS024458255
  • 144689-24-7
  • HY-17004
  • HMS3369I09
  • HY-17004
  • HMS3369I09
  • Olmesartan medoximil
  • NSC759810
  • Olmesartan medoximil
  • NSC759810
  • 1H-Imidazole-5-carboxylic acid, 4-(1-hydroxy-1-methylethyl)-2-propyl-1-((2'-(1H-tetrazol-5-yl) (1,1'-biphenyl)-4-yl)methyl)-
  • CS-088
  • 1H-Imidazole-5-carboxylic acid, 4-(1-hydroxy-1-methylethyl)-2-propyl-1-((2'-(1H-tetrazol-5-yl) (1,1'-biphenyl)-4-yl)methyl)-
  • CS-088
物化性质
实验特性
LogP 3.65660
PSA 129.81000
折射率 1.671
沸点 738.3°C at 760 mmHg
熔点 186-188°C
闪点 400.3°C
颜色与性状 白色固体
密度 1.33
计算特性
精确分子量 446.20700
氢键供体数量 3
氢键受体数量 7
可旋转化学键数量 8
同位素质量 446.207
重原子数量 33
复杂度 656
同位素原子数量 0
确定原子立构中心数量 0
不确定原子立构中心数量 0
确定化学键立构中心数量 0
不确定化学键立构中心数量 0
共价键单元数量 1
疏水参数计算参考值(XlogP) 3.2
拓扑分子极性表面积 130
海关数据
海关编码 2921590090
海关数据

中国海关编码:

2921590090

概述:

2921590090. 其他芳香多胺及衍生物及它们的盐. 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

Summary:

2921590090. other aromatic polyamines and their derivatives; salts thereof. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%

生产方法和用途
用途 降压药物。
专业数据库参考
PubChemId 158781
参考资料
Reaxys RN 7502669
化合物详情(旧版)

物理化学性质

外观与性状:白色固体
密度:1.33
熔点:186-188ºC
沸点:738.3ºC at 760mmHg
闪点:400.3ºC
折射率:1.671
蒸汽压:6.89EmmHg at 25°C

产品用途


应用领域

注意事项

1.(1)对ACEI、阿司匹林和(或)青霉素过敏者。
(2)有发生血管性水肿的危险的患者。
(3)有因喉部喘鸣,面部、舌部或声门血管性水肿而停药的病史者。
(4)主动脉或二尖瓣狭窄、肥大性心肌病、左心室流出通道阻塞的患者。
(5)肾损害(单肾或双肾动脉狭窄)、肝损害(胆汁性肝硬化或胆道阻塞)患者。
(6)糖尿病患者。
(7)同时使用保钾利尿药或补钾药的患者。
2.药物对儿童的影响:尚无18岁以下患者用药的研究资料,不推荐使用。
3.药物对妊娠的影响:妊娠中、晚期用药,可造成胎儿(或新生儿)损伤(如血压降低、高血钾,新生儿贫血、颅骨发育不全、无尿和肾衰竭等)或死亡。美国药品和食品管理局(FDA)对奥美沙坦酯的妊娠安全性分级为C级(妊娠早期)和D级(妊娠中、晚期)。
4.药物对哺乳的影响:动物试验表明,奥美沙坦酯可少量经乳汁分泌。尚不清楚是否经人乳分泌。
5.需全身麻醉的外科手术、导致血压降低的药可能阻断继发于代偿性肾素释放的AngⅡ的形成。
6.心力衰竭、低钠血症、近期加强利尿(增加利尿药用量)、肾透析、严重血容量或钠盐摄入不足的患者,可致血压过低的危险性增加。7.如患者存在血容量或钠盐摄入不足,可降低初始用量。

不良反应

1.可见心律减慢(轻微)。未观察到严重血压下降(按一日80mg给药)。
2.中枢神经系统:可见头晕、头痛。
3.代谢/内分泌系统:可见血糖、三酰甘油升高。
4.呼吸系统:可见支气管炎、咽炎、鼻窦炎、上呼吸道感染,包括流感样症状。
5.肌肉骨骼系统:可见肌酸磷酸激酶(CPK)升高。有报道可出现肌痛、骨骼痛,尤其是背部疼痛或僵直。
6.泌尿生殖系统:可见血尿。
7.肝脏:少见氨基转移酶升高(尚不确定是否由奥美沙坦酯引起)。

用法用量

口服给药初始用量,一次20mg,一日1次,共2周。一般用量,一次20~40mg,一日1次。最大用量,一次40mg,一日1次。肾功能不全时剂量:无需调整剂量。肝功能不全时剂量:无需调整剂量。

药物的相互作用

1.与甘草合用,可降低AngⅡ受体拮抗药的疗效,可能的机制是甘草可引起高盐皮质激素效应。
2.与麻黄合用,可降低AngⅡ受体拮抗药的疗效,可能的机制是麻黄中麻黄碱和伪麻黄碱的拟交感活性可产生拮抗作用。
3.与育亨宾合用,可降低AngⅡ受体拮抗药的疗效,可能的机制是育亨宾可增加去甲肾上腺上腺上腺素的释放。
4.与抗酸药合用,奥美沙坦的生物利用度未发生显著改变。
5.与地高辛、华法林合用,尚未出现明显相互作用的报道。

药代动力学

奥美沙坦口服后1周开始起效,最大降压效应的时间为2~4周。单次或多次用药,持续时间均约24h。健康受试者一次口服奥美沙坦20mg、40mg、80mg后,血药浓度达峰时间为1.4~2.8h,峰浓度分别为450ng/ml、725ng/ml、1200ng/ml,谷浓度分别为19ng/ml、35ng/ml、62ng/ml,平均曲线下面积(AUC)分别为2613(ng·h)/ml、4229(ng·h)/ml、9330(ng·h)/ml。健康受试者静脉注射2mg、4mg、8mg、16mg后,血药浓度达峰时间为10min,峰浓度分别为543ng/ml、1092ng/ml、2078ng/ml、4829ng/ml。静脉给药4mg、8mg后,AUC分别为2906(ng·h)/ml、5370(ng·h)/ml。奥美沙坦口服生物利用度为26%,进食不影响生物利用度。动物研究资料表明,少量药物可通过血-脑脊液屏障和胎盘。分布容积为17L。总蛋白结合率为99%。药物主要通过肠壁代谢,其代谢产物为有活性的奥美沙坦。口服后,肾脏清除率为0.5~0.8L/h,排泄率为35%~50%,胆汁排泄率为50%~65%,半衰期为12~18h。静脉给药1~32mg后,肾脏清除率为0.5~0.6L/h,排泄率为35%~49%,半衰期为8~13h。

药理作用

奥美沙坦为非肽类血管紧张素Ⅱ(AngⅡ)受体(AT1型)阻滞药。与血管紧张素转换酶抑制药(ACEI)相比,奥美沙坦不引起ACEI所致的干咳、皮疹和血管神经性水肿等,不良反应小,具有强而持久的降压作用。AngⅡ为肾素-血管紧张素-醛固酮系统中重要的物质,有收缩血管、刺激醛固酮合成,激动心脏、促进肾脏对钠的再吸收等功能。奥美沙坦通过选择性阻断AugⅡ与血管平滑肌AT1受体结合,从而拮抗AngⅡ的作用,抑制肾素分泌的负反馈调节,导致血浆肾素活肾素活性升高和循环AngⅡ浓度升高,但这对奥美沙坦的降压效果无明显影响。

适应症

用于高血压。

禁忌症

1.对奥美沙坦过敏者。2.孕妇。



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