Clobenpropit dihydrobromide 是一种有效的组胺H3R拮抗剂/反向激动剂，对组胺 H3LR 的pEC50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)。
| 生物活性 | Clobenpropit dihydrobromide is a potenthistamine H3Rantagonist/inverse agonist with apEC50of 8.07 for histamine H3LR[1]. Clobenpropit dihydrobromide acts as partial agonist athistamine H4receptors (Ki13 nM). Clobenpropit dihydrobromide also binds to serotonin 5-HT3 receptors (Ki7.4 nM) and α2A/α2C adrenoceptors (Ki17.4/7.8 nM)[2]. Clobenpropit dihydrobromide increasesapoptosis[3]. |
| IC50& Target[1][2] | Human H3LR 9.44 (pKi) | Rat H3LR 9.75 (pKi) | H4receptor 13 nM (Ki) | H2Receptor 5.6 (pKi) |
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体外研究
(In Vitro) | Clobenpropit binds to human H3LR and rat H3LR with pKis of 9.44±0.04 and 9.75±0.01. Clobenpropit exhibits low affinity for histamine H1R or H2R (pKis of 5.2 and 5.6, respectively)[1].
Clobenpropit inhibits [3H]-dopamine transport by SH-SY5Y cells in a concentration dependent manner with maximum inhibition 82.7±2.8 % and IC50490 nM (pIC506.31±0.11)[2].
Clobenpropit is a subunit-selective noncompetitive antagonist at recombinant NMDA receptors (IC501 μM for the NR1/NR2B receptor)[2].
Clobenpropit (50 μM) and Gemcitabine (5 μM) combination therapy significantly increases apoptosis of Panc-1, MiaPCa-2 and AsPC-1 compared with control[3].
Apoptosis Analysis[3] | 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). |
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体内研究
(In Vivo) | 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[3].
| Animal Model: | Five-week-old male BALB/c nude mice with Panc-1 xenograft[3] | | 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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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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