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127191-97-3

中文名稱 1-[N,O-二(5-異喹啉磺?;?-N-甲基-L-型酪氨酸]-4-苯基哌嗪
英文名稱 KN-62
CAS 127191-97-3
分子式 C38H35N5O6S2
MDL 編號(hào) MFCD00083180
分子量 721.84
MOL 文件 127191-97-3.mol
更新日期 2024/11/08 11:09:18
127191-97-3 結(jié)構(gòu)式 127191-97-3 結(jié)構(gòu)式

基本信息

中文別名
1-[N,O-二(5-異喹啉磺酰基)-N-甲基-L-型酪氨酸]-4-苯基哌嗪
5-異喹啉磺酸 4-[(2S)-2-[(5-異喹啉磺?;?甲氨基]-3-氧代-3-(4-苯基-1-哌嗪基)丙基]苯酯
英文別名
KN-62
所屬類別
生物化工:酪氨酸類衍生物

物理化學(xué)性質(zhì)

熔點(diǎn)92-94°C
沸點(diǎn)964.7±75.0 °C(Predicted)
密度1.388
儲(chǔ)存條件−20°C
儲(chǔ)存條件-20°C
溶解度45% (w/v) aq 2-hydroxypropyl-β-cyclodextrin: 0.93 mg/mL
溶解度45% (w/v) aq 2-羥丙基-β-環(huán)糊精:0.93 mg/mL
酸度系數(shù)(pKa)4.07±0.13(Predicted)
形態(tài)solid
形態(tài)固體
顏色white
顏色白色
CAS 數(shù)據(jù)庫127191-97-3(CAS DataBase Reference)

安全數(shù)據(jù)

安全說明24/25
安全說明S24/25
WGK Germany3
WGK Germany3
海關(guān)編碼29339980

知名試劑公司產(chǎn)品信息

常見問題列表

生物活性
KN-62 是一種有效,選擇性的鈣調(diào)蛋白依賴性蛋白激酶 II (CaMK-II)抑制劑,IC50 為 0.9 μM, KN-62 也是非競(jìng)爭(zhēng)性的 P2X7 受體拮抗劑,IC50 約為 15 nM。
靶點(diǎn)

IC50: 0.9 μM (CaMK II), 15 nM (P2X 7 receptor, in HEK293 cells)

體外研究

KN-62 is a selective antagonist of Ca 2+ /calmodulin-dependent protein kinase II (CaMKII). KN-62 potently antagonizes ATP-stimulated Ba 2+ influx into fura-2 loaded human lymphocytes with an IC 50 of 12.7±1.5 nM (n=3) and complete inhibition of the flux at a concentration of 500 nM. Similarly, KN-62 inhibits ATP-stimulated ethidium + uptake, measured by time resolved flow cytometry, with an IC 50 of 13.1±2.6 nM (n=4) and complete inhibition of the flux at 500 nM. KN-62 is found to be a potent antagonist in a functional assay, inhibition of ATP-induced K + efflux in HEK293 cells expressing recombinant human P2X 7 receptors. In human leukemic B lymphocytes, KN-62 reduces the rate of permeability increase to larger permeant cations, like ethidium, induced by Bz-ATP with an IC 50 of 13.1 nM. KN-62 at a concentration of 3 μM has no effect on ATP-induced ethidium influx through the rat P2X 7 receptor, while the IC 50 at the human P2X 7 receptor is 0.1 μM. KN-62 has considerable selectivity for P2X 7 receptors within the P2 family.

體內(nèi)研究

The antidepressant-like behavior of ZnCl 2 (10 mg/kg, p.o.) (p<0.01) is prevented by CAMKII inhibitor KN-62 (1 μg/site, i.c.v.). The two-way ANOVA reveals a significantly main effect of KN-62 treatment [F(1,28)=27.47, p<0.01], no main effect of ZnCl 2 treatment [F(1,28)=0.84, p>0.05] and a significant effect of KN-62×ZnCl 2 treatment interaction [F(1,28)=22.57, p<0.01] to immobility time. As revealed by the post-hoc analysis, the anti-immobility effect of ZnCl 2 is completely prevented by treatment of animals with KN-62. No effect in locomotor activity in the open-field test is observed: (KN-62 treatment [F(1,24)=1.97, p>0.05], ZnCl 2 treatment [F(1,24)=3.99, p>0.05] and KN-62×ZnCl 2 treatment interaction [F(1,24)=0.61, p>0.05]).

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