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Prucalopride Succinat

Cat. No. M2965
Prucalopride Succinat Structure
Synonym:

R-108512

Size Price Availability Quantity
10mg USD 40  USD40 In stock
25mg USD 50  USD50 In stock
50mg USD 80  USD80 In stock
100mg USD 130  USD130 In stock
250mg USD 220  USD220 In stock
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Quality Control & Documentation
Biological Activity

Prucalopride is a selective, high affinity 5-HT4 receptor agonist, inhibiting human 5-HT(4a) and 5-HT(4b) receptor with Ki value of 2.5 nM and 8 nM, respectively.

Chemical Information
Molecular Weight 485.96
Formula C18H26ClN3O3.C4H6O4
CAS Number 179474-85-2
Solubility (25°C) DMSO 80 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Daniel A Hussar, et al. Prucalopride succinate, Fostamatinib disodium hexahydrate, Avatrombopag maleate, and Lusutrombopag

[2] Stephen Flach, et al. A Phase I Study to Investigate the Absorption, Pharmacokinetics, and Excretion of [(14)C]Prucalopride After a Single Oral Dose in Healthy Volunteers

[3] Baira Shandilya Mahamuni, et al. Selective separation and characterisation of stress degradation products and process impurities of prucalopride succinate by LC-QTOF-MS/MS

[4] Gabrio Bassotti, et al. Prucalopride succinate for the treatment of constipation: an update

[5] A Tomillero, et al. Gateways to clinical trials

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Keywords: Prucalopride Succinat, R-108512 supplier, 5-HT Receptor, inhibitors, activators


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