Iodophenpropit dihydrobromidePotent, selective H3 antagonist CAS# 145196-87-8 |
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Quality Control & MSDS
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Chemical structure
3D structure
Cas No. | 145196-87-8 | SDF | Download SDF |
PubChem ID | 24978528 | Appearance | Powder |
Formula | C15H21Br2IN4S | M.Wt | 576.13 |
Type of Compound | N/A | Storage | Desiccate at -20°C |
Solubility | Soluble to 25 mM in water | ||
Chemical Name | 3-(1H-imidazol-5-yl)propyl N'-[2-(4-iodophenyl)ethyl]carbamimidothioate;dihydrobromide | ||
SMILES | C1=CC(=CC=C1CCN=C(N)SCCCC2=CN=CN2)I.Br.Br | ||
Standard InChIKey | BOSOGNBLIWPCMS-UHFFFAOYSA-N | ||
Standard InChI | InChI=1S/C15H19IN4S.2BrH/c16-13-5-3-12(4-6-13)7-8-19-15(17)21-9-1-2-14-10-18-11-20-14;;/h3-6,10-11H,1-2,7-9H2,(H2,17,19)(H,18,20);2*1H | ||
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. |
Description | Selective H3 antagonist with high affinity (KD = 0.3 nM). Also available as part of the Histamine H3 Receptor. |
Iodophenpropit dihydrobromide Dilution Calculator
Iodophenpropit dihydrobromide Molarity Calculator
1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
1 mM | 1.7357 mL | 8.6786 mL | 17.3572 mL | 34.7144 mL | 43.393 mL |
5 mM | 0.3471 mL | 1.7357 mL | 3.4714 mL | 6.9429 mL | 8.6786 mL |
10 mM | 0.1736 mL | 0.8679 mL | 1.7357 mL | 3.4714 mL | 4.3393 mL |
50 mM | 0.0347 mL | 0.1736 mL | 0.3471 mL | 0.6943 mL | 0.8679 mL |
100 mM | 0.0174 mL | 0.0868 mL | 0.1736 mL | 0.3471 mL | 0.4339 mL |
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. |
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Characterization of the binding of the first selective radiolabelled histamine H3-receptor antagonist, [125I]-iodophenpropit, to rat brain.[Pubmed:7834183]
Br J Pharmacol. 1994 Oct;113(2):355-62.
1. The binding of the first selective radiolabelled histamine H3-receptor antagonist [125I]-iodophenpropit to rat cerebral cortex membranes was characterized. 2. [125I]-iodophenpropit, radiolabelled to a high specific activity of 1900 Ci mmol-1, saturably bound to a single class of sites with a KD of 0.57 +/- 0.16 nM (n = 4) and Bmax of 268 +/- 119 fmol mg-1 protein. 3. Specific binding at a concentration below 1 nM represented 50 to 60% of total binding. 4. Binding of [125I]-iodophenpropit to rat cerebral cortex membranes was readily displaced by histamine H3-agonists and antagonists. In contrast, the inhibitory potencies of selective histamine H1- and H2-receptor ligands were very low. 5. [125I]-iodophenpropit was biphasically displaced by the histamine H3-receptor antagonists, burimamide and dimaprit, which may indicate the existence of histamine H3-receptor subtypes. Other histamine H3-receptor antagonists showed a monophasic displacement. 6. Competition binding curves of H3-agonists were biphasic and showed a rightward shift upon the addition of the nonhydrolysable GTP analogue, guanosine 5'-o-(3-thio) triphosphate (GTP gamma S; 100 microM) which implicates the interaction of histamine H3-receptors with G-proteins. The affinities of the H3-receptor antagonists iodophenpropit, thioperamide and burimamide were not altered by GTP gamma S. 7. Histamine competition binding curves were shifted to the right by different nucleotides (100 microM) with a rank order of potency GTP gamma S > Gpp(NH)p, GTP. 8 In vitro autoradiographic studies revealed a heterogeneous distribution of [125I]-iodophenpropitbinding sites in rat brain, with highest densities observed in specific cerebral cortical areas and layers,the caudate-putamen complex, the olfactory tubercles, the hippocampal formation, the amygdala complex, the hypothalamic area and the mammillary bodies.9 It is concluded that the histamine H3-receptor antagonist, [125I]-iodophenpropit, meets the criteria fo ra suitable radioligand for histamine H3-receptor binding studies in rat brain.
The first radiolabeled histamine H3 receptor antagonist, [125I]iodophenpropit: saturable and reversible binding to rat cortex membranes.[Pubmed:1330590]
Eur J Pharmacol. 1992 Jul 7;217(2-3):203-5.
We describe the binding to rat cortex membranes of [125I]iodophenpropit, the first radiolabeled histamine H3 antagonist. The binding of [125I]iodophenpropit is selective, saturable, readily reversible, and of high affinity (KD 0.32 nM; Bmax 209 fmol/mg of protein). Specific binding at a concentration of 0.3 nM accounted for 45-55% of the total binding. [125I]Iodophenpropit seems to fulfill the criteria for a suitable ligand for histamine H3 receptor binding studies.