Iodophenpropit Dihydrobromide
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MedKoo CAT#: 525348

CAS#: 145196-87-8

Description: Iodophenpropit Dihydrobromide is a potent and selective H3 antagonist.

Chemical Structure

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Iodophenpropit Dihydrobromide
CAS# 145196-87-8
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 525348
Name: Iodophenpropit Dihydrobromide
CAS#: 145196-87-8
Chemical Formula: C15H21Br2IN4S
Exact Mass: 0.00
Molecular Weight: 576.134
Elemental Analysis: C, 31.27; H, 3.67; Br, 27.74; I, 22.03; N, 9.72; S, 5.56

Price and Availability

Size Price Availability Quantity
10mg USD 350 2 Weeks
50mg USD 1100
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Synonym: Iodophenpropit Dihydrobromide

IUPAC/Chemical Name: 3-(1H-Imidazol-5-yl)propyl N"-[2-(4-iodophenyl)ethyl]carbamimidothioate dihydrobromide

InChi Key: BOSOGNBLIWPCMS-UHFFFAOYSA-N

InChi Code: 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

SMILES Code: N=C(SCCCC1=CN=CN1)NCCC2=CC=C(I)C=C2.[H]Br.[H]Br

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Product Data:
Product Data
Instruction:
View handling instruction
Biological target: 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).
In vitro activity: IPP proved to be a potent competitive H3 receptor antagonist as measured against (R)-alpha-methylhistamine-induced inhibition of electrically-evoked contractions of the guinea-pig jejunum (pA2 = 9.12 +/- 0.06, Schild slope: 1.0 +/- 0.1, n = 8). Reference: Br J Pharmacol. 1995 Oct;116(4):2315-21. https://pubmed.ncbi.nlm.nih.gov/8564266/
In vivo activity: 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. It is concluded that the histamine H3-receptor antagonist, [125I]-iodophenpropit, meets the criteria for a suitable radioligand for histamine H3-receptor binding studies in rat brain. Reference: Br J Pharmacol. 1994 Oct;113(2):355-62. https://pubmed.ncbi.nlm.nih.gov/7834183/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 50.0 86.79
Water 32.2 55.89

Preparing Stock Solutions

The following data is based on the product molecular weight 576.13 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Hansen KB, Mullasseril P, Dawit S, Kurtkaya NL, Yuan H, Vance KM, Orr AG, Kvist T, Ogden KK, Le P, Vellano KM, Lewis I, Kurtkaya S, Du Y, Qui M, Murphy TJ, Snyder JP, Bräuner-Osborne H, Traynelis SF. Implementation of a fluorescence-based screening assay identifies histamine H3 receptor antagonists clobenpropit and iodophenpropit as subunit-selective N-methyl-D-aspartate receptor antagonists. J Pharmacol Exp Ther. 2010 Jun;333(3):650-62. doi: 10.1124/jpet.110.166256. Epub 2010 Mar 2. PMID: 20197375; PMCID: PMC2879924. 2. Leurs R, Tulp MT, Menge WM, Adolfs MJ, Zuiderveld OP, Timmerman H. Evaluation of the receptor selectivity of the H3 receptor antagonists, iodophenpropit and thioperamide: an interaction with the 5-HT3 receptor revealed. Br J Pharmacol. 1995 Oct;116(4):2315-21. doi: 10.1111/j.1476-5381.1995.tb15071.x. PMID: 8564266; PMCID: PMC1908963. 3. Rodrigues AA, Jansen FP, Leurs R, Timmerman H, Prell GD. Interaction of clozapine with the histamine H3 receptor in rat brain. Br J Pharmacol. 1995 Apr;114(8):1523-4. doi: 10.1111/j.1476-5381.1995.tb14934.x. PMID: 7541279; PMCID: PMC1510403. 4. Jansen FP, Wu TS, Voss HP, Steinbusch HW, Vollinga RC, Rademaker B, Bast A, Timmerman H. Characterization of the binding of the first selective radiolabelled histamine H3-receptor antagonist, [125I]-iodophenpropit, to rat brain. Br J Pharmacol. 1994 Oct;113(2):355-62. doi: 10.1111/j.1476-5381.1994.tb16995.x. PMID: 7834183; PMCID: PMC1510107.
In vitro protocol: 1. Hansen KB, Mullasseril P, Dawit S, Kurtkaya NL, Yuan H, Vance KM, Orr AG, Kvist T, Ogden KK, Le P, Vellano KM, Lewis I, Kurtkaya S, Du Y, Qui M, Murphy TJ, Snyder JP, Bräuner-Osborne H, Traynelis SF. Implementation of a fluorescence-based screening assay identifies histamine H3 receptor antagonists clobenpropit and iodophenpropit as subunit-selective N-methyl-D-aspartate receptor antagonists. J Pharmacol Exp Ther. 2010 Jun;333(3):650-62. doi: 10.1124/jpet.110.166256. Epub 2010 Mar 2. PMID: 20197375; PMCID: PMC2879924. 2. Leurs R, Tulp MT, Menge WM, Adolfs MJ, Zuiderveld OP, Timmerman H. Evaluation of the receptor selectivity of the H3 receptor antagonists, iodophenpropit and thioperamide: an interaction with the 5-HT3 receptor revealed. Br J Pharmacol. 1995 Oct;116(4):2315-21. doi: 10.1111/j.1476-5381.1995.tb15071.x. PMID: 8564266; PMCID: PMC1908963.
In vivo protocol: 1. Rodrigues AA, Jansen FP, Leurs R, Timmerman H, Prell GD. Interaction of clozapine with the histamine H3 receptor in rat brain. Br J Pharmacol. 1995 Apr;114(8):1523-4. doi: 10.1111/j.1476-5381.1995.tb14934.x. PMID: 7541279; PMCID: PMC1510403. 2. Jansen FP, Wu TS, Voss HP, Steinbusch HW, Vollinga RC, Rademaker B, Bast A, Timmerman H. Characterization of the binding of the first selective radiolabelled histamine H3-receptor antagonist, [125I]-iodophenpropit, to rat brain. Br J Pharmacol. 1994 Oct;113(2):355-62. doi: 10.1111/j.1476-5381.1994.tb16995.x. PMID: 7834183; PMCID: PMC1510107.

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