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168079-32-1

中文名稱 利伐普坦
英文名稱 LIXIVAPTAN
CAS 168079-32-1
分子式 C27H21ClFN3O2
分子量 473.933
MOL 文件 168079-32-1.mol
更新日期 2023/03/20 15:41:29
168079-32-1 結(jié)構(gòu)式 168079-32-1 結(jié)構(gòu)式

基本信息

中文別名
利賽伐坦
利希普坦
利昔伐坦
利伐普坦
利昔普坦
利昔普坦/利伐普坦
LIXIVAPTAN游離
英文別名
CS-780
VPA 985
LIXIVAPTAN
Lixivaptan (VPA-985)
VPA985
LIXIVAPTAN (VPA 985)
N-[3-Chloro-4-(5H-pyrrolo[2,1-c][1,4]benzodiazepin-10(11H)-ylcarbonyl)phenyl]-5-fluoro-2-methylbenzamide
N-[3-Chloro-4-(5H-pyrrolo[2,1-c][1,4]benzodiazepine-10(11H)-ylcarbonyl)phenyl]-5-fluoro-2-methylbenzamide
BenzaMide,N-[3-chloro-4-(5H-pyrrolo[2,1-c][1,4]benzodiazepin-10(11H)-ylcarbonyl)phenyl]-5-fluoro-2-Methyl-
N-[3-chloro-4-(6,11-dihydropyrrolo[2,1-c][1,4]benzodiazepine-5-carbonyl)phenyl]-5-fluoro-2-methyl-benzamide
N-(3-Chloro-4-(10,11-dihydro-5H-benzo[e]pyrrolo[1,2-a][1,4]diazepine-10-carbonyl)phenyl)-5-fluoro-2-methylbenzamide
所屬類別
原料藥:泌尿系統(tǒng)用藥

物理化學(xué)性質(zhì)

熔點(diǎn)>114°C (dec.)
沸點(diǎn)626.5±55.0 °C(Predicted)
密度1.32
儲存條件room temp
溶解度在DMSO中的溶解度為20mg/mL,澄清
酸度系數(shù)(pKa)11.86±0.70(Predicted)
形態(tài)粉末
顏色白色至米色
InChIKeyPPHTXRNHTVLQED-UHFFFAOYSA-N

安全數(shù)據(jù)

危險(xiǎn)性符號(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險(xiǎn)性描述H302
WGK Germany3

常見問題列表

概述
利希普坦(Lixivaptan,1)是由美國惠氏(wyeth)公司研發(fā)的一種非肽類口服選擇性精氨酸加壓素V2受體拮抗劑,化學(xué)名為N-[3-氯-4-(10,11-二氫-5H- 吡咯并[2,1-c][1,4]苯并二氮雜卓-10-基羰基)苯基]-5-氟-2-甲基苯甲酰胺。
用途
利希普坦在用于治療充血性心力衰竭(CHF)、肝硬化并發(fā)低鈉血癥和抗利尿激素分泌失調(diào)綜合征(SIADH)病人時(shí),其在提高自由水清除率的同時(shí)并不影響腎鈉的排出,也不會激活神經(jīng)內(nèi)分泌系統(tǒng),并具有較高的安全性和耐受性。
生物活性
Lixivaptan (VPA-985, WAY-VPA 985) 是具有口服活性,選擇性的 vasopressin receptor V2 拮抗劑,對人和大鼠的 IC50 值分別為1.2 和 2.3 nM。
靶點(diǎn)

IC50: 1.2 nM (human V2), 2.3 nM (rat V2)

體外研究

Lixivaptan displays competitive antagonist activity at V2 receptors.

體內(nèi)研究

In conscious dogs, water-loaded with 30 mL/kg (po) and arginine vasopressin (AVP)-treated (0.4 μg/kg in oil, sc), lixivaptan (1, 3, and 10 mg/kg po) increases U vol over the AVP-treated vehicle group by 438, 1018, and 1133%, respectively, while U osm decreases from 1222 mOsm/kg (water-loaded and AVP treated vehicle) to 307, 221, and 175 mOsm/kg, respectively. In homozygous Brattleboro rats lacking AVP, lixivaptan at 10 mg/kg po (i.e., 10 times the dose producing V2 antagonist activity) b.i.d. for 5 days, shows a sustained antagonist action without evidence of agonist effects. In a randomized double-blind placebo-controlled ascending single dose study, patients (deprived of fluids overnight before dosing) are dosed orally with 30, 75, or 150 mg of lixivaptan. All three doses increase urine flow and serum sodium concentrations and produced significant dose-related decreases in urinary osmolality. Phase II clinical trials in patients with congestive heart failure, liver cirrhosis with ascites or syndrome of inappropriate antidiuretic hormone have demonstrated that lixivaptan increases water clearance without affecting renal sodium excretion or activating the neurohormonal system.

利伐普坦價(jià)格(試劑級)
報(bào)價(jià)日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價(jià)格
2024/11/08HY-14185利伐普坦
Lixivaptan
168079-32-12mg474元
2024/11/08HY-14185利伐普坦
Lixivaptan
168079-32-15mg748元
2024/11/08HY-14185利伐普坦
Lixivaptan
168079-32-110mM * 1mLin DMSO803元
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