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Elacridar hydrochloride Data Sheet

Product Name: Elacridar hydrochloride
Elacridar hydrochloride
CAS No.: 143851-98-3
Cat. No.: HY-50880
MWt: 600.1
Formula: C34H34ClN3O5
Purity : >98%
Solubility: DMSO : 62.5 mg/mL (104.15 mM; Need ultrasonic); H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)
Mechanisms: Target: Cancer
Biological Activity:
Elacridar hydrochloride (GF120918A) is an orally active P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP) inhibitor. Elacridar hydrochloride can be used to examine the influence of efflux transporters on drug distribution to brain and it can be used for the research of cancer[1][2]. In Vitro: Elacridar hydrochloride (0.001-1 μM; 2 h) inhibits cell viability of 786-O cells[2].
Elacridar hydrochloride (5 μM; 24 h) affects P-glycoprotein and ABCG2 protein expression levels in MCF-7 and 786-O cell lines[2].
Elacridar hydrochloride (5 μM; 24 h) affects 99mTc-MIBI intracellular accumulation in MCF-7 and 786-O cells[2]. In Vivo: Elacridar hydrochloride (100 mg/kg; i.p. once) shows different distribution in brain and plasma[1].
1.19 Plasma Pharmacokinetic Parameters of Elacridar hydrochloride in mice[1].
Mice
PO 100 mg/kg
Mice
IP 100 mg/kg
Mice
IV 2.5 mg/kg
CL/F (ml/min) 2.05 33.2 0.46
Vd/F (liter) 3.5 12.3 0.17
t1/2 (h) 20 4.3 4.4
AUC0-inf (μg·min/ml) 1460 90.3 161.4
F 0.22 0.013 1

Caution: Not fully tested. For research purposes only

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