145231-35-2

中文名稱(chēng) 丙酸倍氯松二溴酸鹽溶液,1000PPM

英文名稱(chēng) 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

基本信息物理化學(xué)性質(zhì) 安全數(shù)據(jù) 圖譜信息丙酸倍氯松二溴酸鹽價(jià)格(試劑級(jí)) 常見(jiàn)問(wèn)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(lèi)別

生物化工：激動(dòng)劑抑制劑

物理化學(xué)性質(zhì)

熔點(diǎn)205°C(lit.)

儲(chǔ)存條件-20°C儲(chǔ)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

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(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
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(jiàn)問(wèn)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(dòng)劑，對(duì)組胺 H3LR 的 pEC 50 為 8.07。Clobenpropit dihydrobromide 對(duì)組胺 H4 受體起部分激動(dòng)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(jìn)凋亡 (apoptosis)。

靶點(diǎn)

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).