1. GPCR/G Protein
    Neuronal Signaling
    Immunology/Inflammation
  2. Histamine Receptor
  3. Clobenpropit dihydrobromide

Clobenpropit dihydrobromide 

Cat. No.: HY-101198
Handling Instructions

Clobenpropit dihydrobromide is a potent histamine H3R antagonist/inverse agonist with a pEC50 of 8.07 for histamine H3LR. Clobenpropit dihydrobromide acts as partial agonist at histamine H4 receptors (Ki 13 nM). Clobenpropit dihydrobromide also binds to serotonin 5-HT3 receptors (Ki 7.4 nM) and α2A/α2C adrenoceptors (Ki 17.4/7.8 nM). Clobenpropit dihydrobromide increases apoptosis.

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Clobenpropit dihydrobromide Chemical Structure

Clobenpropit dihydrobromide Chemical Structure

CAS No. : 145231-35-2

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Description

Clobenpropit dihydrobromide is a potent histamine H3R antagonist/inverse agonist with a pEC50 of 8.07 for histamine H3LR[1]. Clobenpropit dihydrobromide acts as partial agonist at histamine H4 receptors (Ki 13 nM). Clobenpropit dihydrobromide also binds to serotonin 5-HT3 receptors (Ki 7.4 nM) and α2A/α2C adrenoceptors (Ki 17.4/7.8 nM)[2]. Clobenpropit dihydrobromide increases apoptosis[3].

IC50 & Target[1][2]

Human H3LR

9.44 (pKi)

Rat H3LR

9.75 (pKi)

H4 receptor

13 nM (Ki)

H2 Receptor

5.6 (pKi)

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].

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).
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).
Molecular Weight

470.65

Formula

C₁₄H₁₉Br₂ClN₄S

CAS No.

145231-35-2

SMILES

N=C(SCCCC1=CN=CN1)NCC2=CC=C(Cl)C=C2.[H]Br.[H]Br

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Storage

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References
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Keywords:

Clobenpropit dihydrobromideHistamine Receptorhistamine H3RantagonistinverseagonistH3LRH4pancreaticcancerInhibitorinhibitorinhibit

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Clobenpropit dihydrobromide
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HY-101198
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