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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 | Availability | Quantity |
---|---|---|---|
1 mg | $38 | In Stock | |
5 mg | $89 | In Stock | |
10 mg | $155 | In Stock | |
25 mg | $347 | In Stock | |
50 mg | $587 | In Stock | |
100 mg | $839 | In Stock |
Description | Clobenpropit dihydrobromide is a potent antagonist and inverse agonist of histamine H3R (histamine H3LR,pEC50 of 8.07) |
Targets&IC50 | H2 receptor:5.6 (pKi), H4 receptor:13 nM (Ki), 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 Îœm |
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. | ||||||||||||||||||||
Solubility Information | DMSO: 4.71 mg/mL (10 mM), Sonication is recommended. | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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