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CP-100356 hydrochloride

Catalog No. T22680 CAS 142715-48-8

Synonyms: CP-100356 HCl, CP 100356 hydrochloride

CP-100356 hydrochloride is an orally active and low micromolar dual inhibitor of MDR1 (P-gp) and BCRP, a nucleotide-derived substrate analogue with inhibitory effects on MDR1-mediated Calcein-AM transporter and BCRP-mediated Prazosin transporter.CP-100356 Inhibits OATP1B1, induces stomatal opening in the dark.

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CP-100356 hydrochloride Chemical Structure

CP-100356 hydrochloride, CAS 142715-48-8

Pack Size	Availability	Price/USD	Quantity
50 mg	6-8 weeks	$ 747.00
100 mg	6-8 weeks	$ 1,120.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

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Purity: 99.19%

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Description	CP-100356 hydrochloride is an orally active and low micromolar dual inhibitor of MDR1 (P-gp) and BCRP, a nucleotide-derived substrate analogue with inhibitory effects on MDR1-mediated Calcein-AM transporter and BCRP-mediated Prazosin transporter.CP-100356 Inhibits OATP1B1, induces stomatal opening in the dark.
Targets&IC50	MDR1:0.5 µM, BCRP:1.5 µM (in MDCKII cells)
In vitro	In human MDR1-transfected MDCKII cells, CP-100356 hydrochloride inhibited acetoxymethyl calcein (calcein-AM) uptake (IC50 approximately 0.5 +/- 0.07 microM) and digoxin transport (IC50 approximately 1.2 +/- 0.1 microM). Inhibition of prazosin transport (IC50 approximately 1.5 +/- 0.3 microM) in human BCRP-transfected MDCKII cells by CP-100356 hydrochloride confirmed the dual MDR1/BCRP inhibitory properties[1].
In vivo	In vivo inhibitory effects of CP-100356 hydrochloride in rats were examined after coadministration with MDR1 substrate fexofenadine and dual MDR1/BCRP substrate prazosin. Coadministration with increasing doses of CP-100356 hydrochloride resulted in dramatic increases in systemic exposure of fexofenadine (36- and 80-fold increase in C(max) and AUC at a CP-100356 hydrochloride dose of 24 mg/kg). Significant differences in prazosin pharmacokinetics were also discernible in CP-100356 hydrochloride-pretreated rats as reflected from a 2.6-fold increase in AUC.[1].

Synonyms	CP-100356 HCl, CP 100356 hydrochloride
Molecular Weight	597.1
Formula	C31H37ClN4O6
CAS No.	142715-48-8

Storage

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 5 mg/mL (8.37 mM), Sonication is recommended.

References and Literature

1. Kalgutkar AS,et al. N-(3,4-dimethoxyphenethyl)-4-(6,7-dimethoxy-3,4-dihydroisoquinolin-2[1H]-yl)-6,7-dimethoxyquinazolin-2-amine (CP-100,356) as a "chemical knock-out equivalent" to assess the impact of efflux transporters on oral drug absorption in the rat. J Pharm Sci. 2009 Dec;98(12):4914-27.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

CP-100356 hydrochloride 142715-48-8 Membrane transporter/Ion channel BCRP CP-100356 HCl CP-100356 Hydrochloride CP 100356 hydrochloride inhibitor inhibit

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