丙酸倍氯松二溴酸盐溶液,1000PPM CAS#: 145231-35-2

丙酸倍氯松二溴酸盐溶液,1000PPM

生物活性靶点体外研究体内研究用途与合成方法 MSDS 丙酸倍氯松二溴酸盐溶液,1000PPM价格(试剂级) 上下游产品信息

中文名称	丙酸倍氯松二溴酸盐溶液,1000PPM
中文同义词	丙酸倍氯松二溴酸盐溶液,100PPM;氯苯丙替二氢溴酸盐;丙酸倍氯松二溴酸盐溶液,1000PPM;丙酸倍氯松二溴酸盐
英文名称	N-(4-CHLOROBENZYL)-S-[3-(4(5)-IMIDAZOLYL)PROPYL]ISOTHIOUREA
英文同义词	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
CAS号	145231-35-2
分子式	C14H17ClN4S.2BrH
分子量	470.659
EINECS号
相关类别
Mol文件	145231-35-2.mol
结构式

丙酸倍氯松二溴酸盐溶液,1000PPM 性质

熔点	205°C(lit.)
储存条件	Store at -20°C
溶解度	DMSO：30mg/mL；乙醇：2.5mg/mL；水：20mg/mL
形态	粉末晶体
颜色	白色到灰色到红色
水溶解性	Soluble to 100 mM in water

丙酸倍氯松二溴酸盐溶液,1000PPM 用途与合成方法

生物活性

Clobenpropit dihydrobromide 是一种有效的组胺 H3R 拮抗剂/反向激动剂，对组胺 H3LR 的 pEC 50 为 8.07。Clobenpropit dihydrobromide 对组胺 H4 受体起部分激动剂的作用，Ki 为 13 nM。Clobenpropit dihydrobromide 还与 5-HT3 受体 (Ki 为 7.4 nM) 和 α2A/α2C 肾上腺素受体 (Ki 为 17.4/7.8 nM) 结合。Clobenpropit dihydrobromide 促进凋亡 (apoptosis)。

靶点

Human H3LR

9.44 (pKi)

Rat H3LR

9.75 (pKi)

H ₄ receptor

13 nM (Ki)

H ₂ Receptor

5.6 (pKi)

体外研究

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).

体内研究

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).

安全信息

海关编码	2933.29.4300

MSDS信息

丙酸倍氯松二溴酸盐溶液,1000PPM 价格(试剂级)

更新日期	产品编号	产品名称	CAS号	包装	价格
2024/04/30	C3446	氯苯丙替二氢溴酸盐 Clobenpropit Dihydrobromide	145231-35-2	25mg	905元

丙酸倍氯松二溴酸盐溶液,1000PPM