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1780259-94-0

中文名稱(chēng) 1780259-94-0
英文名稱(chēng) ZK756326(dihydrochloride)
CAS 1780259-94-0
分子式 C21H29ClN2O3
分子量 392.92
MOL 文件 1780259-94-0.mol
更新日期 2023/03/20 15:41:27
1780259-94-0 結(jié)構(gòu)式 1780259-94-0 結(jié)構(gòu)式

基本信息

中文別名
非肽趨化因子受體激動(dòng)劑(ZK756326 DIHYDROCHLORIDE)
英文別名
ZK 756326 (hydrochloride)
ZK756326(dihydrochloride)

物理化學(xué)性質(zhì)

儲(chǔ)存條件-20°C儲(chǔ)存
溶解度PBS (pH 7.2): 10 mg/ml
形態(tài)結(jié)晶固體
顏色White to off-white

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險(xiǎn)性描述H302-H315-H319-H335
防范說(shuō)明P261-P305+P351+P338
1780259-94-0價(jià)格(試劑級(jí))
報(bào)價(jià)日期產(chǎn)品編號(hào)產(chǎn)品名稱(chēng)CAS號(hào)包裝價(jià)格
2024/11/08HY-101038A1780259-94-0
ZK756326 dihydrochloride
1780259-94-05mg600元
2024/11/08HY-101038A1780259-94-0
ZK756326 dihydrochloride
1780259-94-010mM * 1mLin DMSO660元
2024/11/08HY-101038A1780259-94-0
ZK756326 dihydrochloride
1780259-94-010mg900元

常見(jiàn)問(wèn)題列表

生物活性
ZK756326 dihydrochloride 是一種非肽趨化因子受體激動(dòng)劑,作用于 CC 趨化因子受體 CCR8。
靶點(diǎn)

CCR8

1.8 μM (IC 50 , in U87 cells)

5-HT 1A

5.4 μM (IC 50 )

5-HT 2B

4.4 μM (IC 50 )

5-HT 2C

34.8 μM (IC 50 )

5-HT 5A

16 μM (IC 50 )

5-HT 6

5.9 μM (IC 50 )

α 2A

<20 μM (IC 50 )

體外研究

ZK 756326 inhibits the binding of the CCR8 ligand I-309 (CCL1), with an IC 50 value of 1.8 μM. ZK 756326 is a full agonist of CCR8, dose-responsively eliciting an increase in intracellular calcium and cross-desensitizing the response of the receptor to CCL1. ZK 756326 stimulates extracellular acidification in cells expressing human CCR8. Binding competition assays are performed on a series of other G-protein-coupled receptors to determine whether the interaction of ZK 756326 is specific for CCR8. In these assays, ZK 756326 is tested at 50 μM for inhibition of radiolabeled ligand binding. At this concentration, ZK 756326 shows >28 fold specificity for CCR8 compared with 26 other GPCRs, all with IC 50 values of >50 μM. There is less selectivity when ZK 756326 is tested against the serotonergic receptors 5-HT 1A , 5-HT 2B , 5-HT 2C , 5-HT 5A , 5-HT 6 , and the adrenergic receptor α2A, in which IC 50 values of 5.4, 4,4, 34.8, 16, 5.9, and <20 μM (at 20 μM 65% inhibition), respectively, are observed. The compound is unlikely to be an agonist on these biogenic amine receptors, because when tested at concentrations up to 10 μM on a representative receptor, 5-HT 1A , it shows no agonist activity in a GTPγS binding assay.

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