Description
SB-203186 hydrochloride is a potent, selective and competitive 5-HT4 antagonist. SB-203186 hydrochloride antagonizes the 5-HT4 receptor-mediated relaxations of the carbachol-contracted rat isolated oesophagus against 5-HT with pKB values of 10.9 (rat oesophagus), 9.5 (guinea-pig ileum), and 9.0 (human colon) respectively.
Product information
CAS Number: 207572-69-8
Molecular Weight: 308.80
Formula: C16H21ClN2O2
Chemical Name: 2-(piperidin-1-yl)ethyl 1H-indole-3-carboxylate hydrochloride
Smiles: Cl.O=C(OCCN1CCCCC1)C1=CNC2=CC=CC=C12
InChiKey: LYMBEMCUJNDSBZ-UHFFFAOYSA-N
InChi: InChI=1S/C16H20N2O2.ClH/c19-16(20-11-10-18-8-4-1-5-9-18)14-12-17-15-7-3-2-6-13(14)15;/h2-3,6-7,12,17H,1,4-5,8-11H2;1H
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 100 mg/mL (323.83 mM; Need ultrasonic).
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:
Pretreatment with SB-203186 (10 μM) enhances the 5-HT-induced contractions of the antral strips.
In Vivo:
Intraduodenally administered SB-203186 (0.3-3 mg/kg) to new-born Camborough piglets produced blockade of 5-HT-evoked tachycardia which was maximal after 20 min and lasted for more than 3 h with 0.3 mg/kg. SB-203186 (0.1-3mg/kg, i.v.) surmountably antagonised 5-HT-evoked tachycardia in anaesthetized Yucatan minipigs or new-born Camborough piglets with similar potency.
Products are for research use only. Not for human use.
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