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145231-35-2

中文名稱 丙酸倍氯松二溴酸鹽溶液,1000PPM
英文名稱 N-(4-CHLOROBENZYL)-S-[3-(4(5)-IMIDAZOLYL)PROPYL]ISOTHIOUREA
CAS 145231-35-2
分子式 C14H17ClN4S.2BrH
分子量 470.659
MOL 文件 145231-35-2.mol
更新日期 2023/09/15 22:54:22
145231-35-2 結(jié)構(gòu)式 145231-35-2 結(jié)構(gòu)式

基本信息

中文別名
丙酸倍氯松二溴酸鹽
氯苯丙替二氫溴酸鹽
丙酸倍氯松二溴酸鹽溶液,100PPM
丙酸倍氯松二溴酸鹽溶液,1000PPM
英文別名
Clobenpropit (hydrobromide)
Clobenpropit dihydrobromide Solution, 100ppm
Clobenpropit dihydrobromide Solution, 1000ppm
3-(1H-Imidazol-4-yl)propyl 4-Chlorobenzylcarbamimidothioate Dihydrobromide
Apoptosis,inhibit,Clobenpropit dihydrobromide,histamine H3R,antagonist,inverse,Inhibitor,pancreatic,agonist,cancer,H3LR,Histamine Receptor

物理化學(xué)性質(zhì)

熔點205°C(lit.)
儲存條件-20°C儲存
溶解度DMSO: 30 mg/ml; Ethanol: 2.5 mg/ml; Water: 20 mg/ml
形態(tài)粉末晶體
顏色白色到灰色到紅色
水溶解性溶于水至100mM

安全數(shù)據(jù)

海關(guān)編碼2933.29.4300
丙酸倍氯松二溴酸鹽價格(試劑級)
報價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2024/11/08C3446氯苯丙替二氫溴酸鹽
Clobenpropit Dihydrobromide		145231-35-225mg905元

常見問題列表

生物活性
Clobenpropit dihydrobromide 是一種有效的組胺 H3R 拮抗劑/反向激動劑，對組胺 H3LR 的 pEC 50 為 8.07。Clobenpropit dihydrobromide 對組胺 H4 受體起部分激動劑的作用，Ki 為 13 nM。Clobenpropit dihydrobromide 還與 5-HT3 受體 (Ki 為 7.4 nM) 和 α2A/α2C 腎上腺素受體 (Ki 為 17.4/7.8 nM) 結(jié)合。Clobenpropit dihydrobromide 促進凋亡 (apoptosis)。
靶點

Human H3LR

9.44 (pKi)

Rat H3LR

9.75 (pKi)

H 4 receptor

13 nM (Ki)

H 2 Receptor

5.6 (pKi)

體外研究

Clobenpropit binds to human H3LR and rat H3LR with pK i s of 9.44±0.04 and 9.75±0.01. Clobenpropit exhibits low affinity for histamine H1R or H2R (pK i s of 5.2 and 5.6, respectively).
Clobenpropit inhibits [ 3 H]-dopamine transport by SH-SY5Y cells in a concentration dependent manner with maximum inhibition 82.7±2.8 % and IC 50 490 nM (pIC 50 6.31±0.11).
Clobenpropit is a subunit-selective noncompetitive antagonist at recombinant NMDA receptors (IC 50 1 μM for the NR1/NR2B receptor).
Clobenpropit (50 μM) and Gemcitabine (5 μM) combination therapy significantly increases apoptosis of Panc-1, MiaPCa-2 and AsPC-1 compared with control.

Apoptosis Analysis

Cell Line: Pancreatic cancer cells (Panc-1, MiaPaCa-2 and AsPC-1)
Concentration: 50 μM
Incubation Time:
Result: Enhanced apoptotic cell death in combination of Gemcitabine (5 μM).
體內(nèi)研究

The combination treatment of Clobenpropit (every other day intraperitoneal injection at 20 μM per kilogram for 40 d) and Gemcitabine (twice-a-week intraperitoneal injection at 125 mg/kg for 40 d) shows significant tumor growth inhibition.

Animal Model: Five-week-old male BALB/c nude mice with Panc-1 xenograft
Dosage: 20 μM per kilogram
Administration: Intraperitoneal injection; every other day for 40 days. Gemcitabine (twice-a-week intraperitoneal injection at 125 mg/kg for 40 d)
Result: The combination treatment showed significant tumor growth inhibition compared with other treatment groups (control 501±92 mg, Gemcitabine 294±46 mg, Clobenpropit 444±167 mg, and combination 154±54 mg).
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