| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
Purity: ≥98%
Prucalopride HCl (formerly known as R93877; R-108512; Resolor; Resotran; trade name: Motegrity), the hydrochloride salt of prucalopride which is a novel enterokinetic compound and is the first representative of the benzofuran class, is a novel selective, high affinity 5-HT (serotonin) receptor agonist for 5-HT4A and 5-HT4B receptor with anti-constipation effects. It inhibits 5-HT4A and 5-HT4B receptor with Ki values of 2.5 nM and 8 nM, respectively, and exhibits >290-fold selectivity against other 5-HT receptor subtypes. Prucalopride induces contractions in a concentration-dependent manner with pEC50 of 7.5. Prucalopride significantly amplifies the rebound contraction of the guinea-pig proximal colon after electrical field stimulation. Prucalopride was approved by FDA in December 2018 to treat chronic idiopathic constipation.
| ln Vitro |
|
||
|---|---|---|---|
| ln Vivo |
|
||
| Animal Protocol |
|
||
| References |
Eur J Pharmacol.2001 Jun 29;423(1):71-83;N Engl J Med.2008 May 29;358(22):2344-54.
|
| Molecular Formula |
C18H27CL2N3O3
|
|---|---|
| Molecular Weight |
403.33
|
| Exact Mass |
403.143
|
| CAS # |
179474-80-7
|
| Related CAS # |
Prucalopride;179474-81-8
|
| PubChem CID |
9931054
|
| Appearance |
Typically exists as solid at room temperature
|
| LogP |
3.983
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
26
|
| Complexity |
445
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
KKMOQGWTJRGLNN-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C18H26ClN3O3.ClH/c1-24-9-2-6-22-7-3-12(4-8-22)21-18(23)14-11-15(19)16(20)13-5-10-25-17(13)14;/h11-12H,2-10,20H2,1H3,(H,21,23);1H
|
| Chemical Name |
4-amino-5-chloro-N-[1-(3-methoxypropyl)piperidin-4-yl]-2,3-dihydro-1-benzofuran-7-carboxamide;hydrochloride
|
| Synonyms |
R-108512; Prucalopride Succinate; R 108512; R-93877 HCl; R 93877 hydrochloride; R-108512; R108512; Resolor; Resotran; R93877; trade name: Motegrity
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
|
|||
|---|---|---|---|---|
| Solubility (In Vivo) |
|
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4794 mL | 12.3968 mL | 24.7936 mL | |
| 5 mM | 0.4959 mL | 2.4794 mL | 4.9587 mL | |
| 10 mM | 0.2479 mL | 1.2397 mL | 2.4794 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA