Clobenpropit dihydrobromide

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Clobenpropit dihydrobromide

Catalog No.: PC0173

Size: 5 mg, 10 mg, 25 mg,50 mg, 100 mg, 200 mg, 500 mg

Description

Clobenpropit dihydrobromide is a potent histamine H3R antagonist/inverse agonist and partial agonist of H4 receptors (Ki 13 nM). Clobenpropit dihydrobromide also binds to serotonin 5-HT3 receptors and α2A/α2C adrenergic receptors. Chlorprofen dihydroborb increases apoptosis.

Molecular Weight	470.65
Formula	C14H19Br2ClN4S
CAS No.	145231-35-2
Appearance	Solid
Color	White to off-white
SMILES	N=C(SCCCC1=CN=CN1)NCC2=CC=C(Cl)C=C2.[H]Br.[H]Br
Shipping	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
*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). 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). Clobenpropit is a subunit-selective noncompetitive antagonist at recombinant NMDA receptors (IC₅₀ 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.
*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.

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