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159138-80-4

中文名稱 卡立泊來德
英文名稱 CARIPORIDE
CAS 159138-80-4
分子式 C12H17N3O3S
分子量 283.35
MOL 文件 159138-80-4.mol
更新日期 2023/03/20 15:41:25
159138-80-4 結(jié)構(gòu)式 159138-80-4 結(jié)構(gòu)式

基本信息

中文別名
卡立泊來德
N-(氨基亞氨基甲基)-4-(1-甲基乙基)-3-(甲磺酰基)苯甲酰胺
英文別名
CS-1692
CARIPORIDE
Cariporide (HOE-642)
N-(diaminomethylene)-4-isopropyl-3-mesyl-benzamide
N-(Aminoiminomethyl)-4-(1-methylethyl)-3-(methylsulfonyl)benzamide
N-[bis(azanyl)methylidene]-3-methylsulfonyl-4-propan-2-yl-benzamide
BenzaMide,N-(aMinoiMinoMethyl)-4-(1-Methylethyl)-3-(Methylsulfonyl)-
所屬類別
生物化工:激動劑抑制劑

物理化學(xué)性質(zhì)

熔點90-94° (dec)
密度1.34
儲存條件2-8°C
溶解度insoluble in H2O; ≥12.05 mg/mL in DMSO; ≥2.675 mg/mL in EtOH with gentle warming and ultrasonic
形態(tài)粉末
顏色白色至米色

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險性描述H302-H315-H319-H335
RTECS號CV2310560

常見問題列表

生物活性
Cariporide是有效的選擇性NHE1抑制劑,在CHO-K1細胞中對hNHE1的IC50值為30 nM。
靶點
TargetValue
NHE1
(CHO-K1 cells)
30 nM
體外研究

Cariporide significantly suppresses markers of cell death, such as TUNEL positivity and caspase-3 cleavage, at 8 or 16 hours. Cariporide remarkably suppresses cytosolic Na + and Ca 2+ accumulation. Cariporide prevents mitochondrial membrane potential loss induced by H 2+ O 2+ . Cariporide (HOE-642) ameliorates myocardial ischemia/reperfusion injury, by the well-established reduction of cytosolic Ca 2+ in cardiac myocytes through inhibition of Na + /H + exchange. Cariporide (HOE-642), has inhibitory effects on the degranulation of human platelets, the formation of platelet–leukocyte-aggregates, and the activation of the GPIIb/IIIa receptor (PAC-1).

體內(nèi)研究

Intravenous administration of cariporide significantly decreases brain Na + uptake and reduces cerebral edema, brain swelling, and infarct volume.

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