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Clobenpropit dihydrobromide is a potent antagonist and inverse agonist of histamine H3R (histamine H3LR,pEC50 of 8.07)

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $38 | In Stock | In Stock | |
| 5 mg | $89 | In Stock | In Stock | |
| 10 mg | $155 | In Stock | In Stock | |
| 25 mg | $347 | In Stock | In Stock | |
| 50 mg | $587 | - | In Stock | |
| 100 mg | $839 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $93 | In Stock | In Stock |
| Description | Clobenpropit dihydrobromide is a potent antagonist and inverse agonist of histamine H3R (histamine H3LR,pEC50 of 8.07) |
| Targets&IC50 | H4 receptor:13 nM (Ki), H2 receptor:5.6 (pKi), H3LR (human):9.44 (pKi), H3LR (rat):9.75 (pKi) |
| In vitro | Clobenpropit inhibited cell migration and increased apoptosis of pancreatic cancer cells in combination with gemcitabine.?Clobenpropit up-regulated E-cadherin, but down-regulated vimentin and matrix metalloproteinase 9 in real-time polymerase chain reaction[1]. |
| In vivo | Clobenpropit inhibited tumor growth (gemcitabine 294 46 mg vs combination 154 54 mg, P = 0.02) and enhanced apoptosis in combination with gemcitabine (control 2.5%, gemcitabine 25.8%, clobenpropit 9.7% and combination 40.9%, P = 0.001) by up-regulation of E-cadherin and down-regulation of Zeb1 in Panc-1 xenograft mouse. |
| Cell Research | Pancreatic cancer cells (Panc-1, MiaPaCa-2 and AsPC-1).Concentration: 50 Μm |
| Molecular Weight | 470.7 |
| Formula | C14H19Br2ClN4S |
| Cas No. | 145231-35-2 |
| Smiles | Br.Br.Clc1ccc(CNC(=N)SCCCc2cnc[nH]2)cc1 |
| Relative Density. | no data available |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||
| Solubility Information | DMSO: 4.71 mg/mL (10.01 mM), Sonication is recommended. | ||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (2.12 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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