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Iodophenpropit dihydrobromide

Potent, selective H3 antagonist CAS# 145196-87-8

Iodophenpropit dihydrobromide

Catalog No. BCC6793----Order now to get a substantial discount!

Product Name & Size Price Stock
Iodophenpropit dihydrobromide: 5mg $104 In Stock
Iodophenpropit dihydrobromide: 10mg Please Inquire In Stock
Iodophenpropit dihydrobromide: 20mg Please Inquire Please Inquire
Iodophenpropit dihydrobromide: 50mg Please Inquire Please Inquire
Iodophenpropit dihydrobromide: 100mg Please Inquire Please Inquire
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Quality Control of Iodophenpropit dihydrobromide

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Chemical structure

Iodophenpropit dihydrobromide

3D structure

Chemical Properties of Iodophenpropit dihydrobromide

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.
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.
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.

Biological Activity of Iodophenpropit dihydrobromide

DescriptionSelective H3 antagonist with high affinity (KD = 0.3 nM). Also available as part of the Histamine H3 Receptor.

Iodophenpropit dihydrobromide Dilution Calculator

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Preparing Stock Solutions of Iodophenpropit dihydrobromide

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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References on Iodophenpropit dihydrobromide

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.

Description

Iodophenpropit dihydrobromide is a potent and selective histamine H3 receptor antagonist. The binding of [125I]Iodophenpropit is selective, saturable, readily reversible, and of high affinity (KD 0.32 nM).

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