Relenopride (YKP10811) hydrochloride is a specific and selective 5-HT4 receptor agonist (Ki=4.96 nM). Relenopride hydrochloride has 120-fold and 6-fold lower affinity, respectively, for 5-HT2A (Ki=600 nM) and 5-HT2B receptors (Ki=31 nM) than for 5-HT4. Relenopride hydrochloride increases gastrointestinal (GI) motility.

Product information

CAS Number: 1221416-42-7

Molecular Weight: 529.43

Formula: C24H31Cl2FN4O4

Chemical Name: (1S)-3-(4-{[(4-amino-5-chloro-2-methoxyphenyl)formamido]methyl}piperidin-1-yl)-1-(4-fluorophenyl)propyl carbamate hydrochloride

Smiles: Cl.COC1=CC(N)=C(Cl)C=C1C(=O)NCC1CCN(CC[C@H](OC(N)=O)C2C=CC(F)=CC=2)CC1

InChiKey: DMJJYQFHCCNBNI-BOXHHOBZSA-N

InChi: InChI=1S/C24H30ClFN4O4.ClH/c1-33-22-13-20(27)19(25)12-18(22)23(31)29-14-15-6-9-30(10-7-15)11-8-21(34-24(28)32)16-2-4-17(26)5-3-16;/h2-5,12-13,15,21H,6-11,14,27H2,1H3,(H2,28,32)(H,29,31);1H/t21-;/m0./s1

Technical Data

Appearance: Solid Power

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

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

Relenopride hydrochloride do not show any significant off-target binding to any other receptors, enzymes, orserotonin-receptor subtypes at 1 μM, except for binding to the 5-HT2A receptor and the 5-HT2B receptor. Relenopride hydrochloride shows antagonist activity at the 5-HT2B receptor with an IC50 of 2.1 μM and no significant activity at the 5-HT2A receptor up to 10 μM. Relenopride hydrochloride shows no activity against serotonin-receptor subtypes 5-HT1B, 5-HT1D, or 5-HT2A at 1 nM to 10 μM, or for serotonin-receptor subtype 5-HT7 at 10 nM to 30 μM.

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