SKU : MC524457
CAS Number : 145231-35-2
Molecular Formula : C14H18BrClN4S | Molecular Weight : 389.74
Quote RequestPurity | NLT 98% |
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Storage | at 20ºC 2 years |
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Chemical Name | Clobenpropit (dihydrobromide) |
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CAS Number | 145231-35-2 |
MDL Number | MFCD23160277 |
Molecular Formula | C14H18BrClN4S |
Molecular Weight | 389.74 |
Clobenpropit dihydrobromide is a potent histamine H3R antagonist/inverse agonist with a pEC50 of 8.07 for histamine H3LR[1]. Clobenpropit acts as partial agonist at histamine H4 receptors (Ki 13 nM). Clobenpropit also binds to serotonin 5-HT3 receptors (Ki 7.4 nM) and α2A/α2C adrenoceptors (Ki 17.4/7.8 nM)[2]. Clobenpropit increases apoptosis[3]. IC50 & Target: pEC50: 8.07 (histamine H3LR)[1]
Ki: 13 nM (histamine H4 receptors), 7.4 nM (serotonin 5-HT3 receptors), 17.4/7.8 nM (α2A/α2C adrenoceptors)[2]
pKi: 9.44±0.04 (human H3LR), 9.75±0.01 (Rat H3LR), 5.2 (histamine H1R), 5.6 (histamine H2R)[1]. 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 IC50 490 nM (pIC50 6.31±0.11)[2].
Clobenpropit is a subunit-selective noncompetitive antagonist at recombinant NMDA receptors (IC50 1 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]. 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].
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