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 結構式

基本信息物理化學性質(zhì) 安全數(shù)據(jù) 圖譜信息丙酸倍氯松二溴酸鹽價格(試劑級) 常見問題列表

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

所屬類別

生物化工：激動劑抑制劑

物理化學性質(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)

海關編碼2933.29.4300

圖譜信息

丙酸倍氯松二溴酸鹽溶液,1000PPM(145231-35-2)核磁圖(¹HNMR)

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
2026/06/05	HY-101198	丙酸倍氯松二溴酸鹽 Clobenpropit dihydrobromide	145231-35-2	1 mg	350元
2026/06/05	HY-101198	丙酸倍氯松二溴酸鹽 Clobenpropit dihydrobromide	145231-35-2	5 mg	950元
2026/06/05	HY-101198	丙酸倍氯松二溴酸鹽 Clobenpropit dihydrobromide	145231-35-2	10 mM * 1 mL in DMSO	984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).