| Chemical & Physical Properties | |
|---|---|
| CAS Number | 143851-98-3 |
| Catalog No. | 2A-1172295 |
| Chinese Name | 依克立达盐酸盐 |
| Synonyms | UNII-NX2BHH1A5B; Elacridar HCl; Elacridar hydrochloride; Elacridar hydrochloride (USAN); Elacridar (hydrochloride) |
| Molecular Formula | C34H34ClN3O5 |
| Molecular Weight | 600.10400 |
| Purity | 98.00 |
| Boiling Point | 701.6ºC at 760 mmHg |
| Storage Condition | 2-8℃ |
| Application | Elacridar (GF120918; GW0918) hydrochloride is a P-glycoprotein inhibitor and is often used as a tool compound in in vivo and in vitro experiments. |
| HTC | 2934999090 |
| PubChem ID | 10257276 |
| SMILES | COc1cc2c(cc1OC)CN(CCc1ccc(NC(=O)c3cccc4c(=O)c5cccc(OC)c5[nH]c34)cc1)CC2.Cl |
| InChI | InChI=1S/C34H33N3O5.ClH/c1-40-28-9-5-7-26-32(28)36-31-25(33(26)38)6-4-8-27(31)34(39)35-24-12-10-21(11-13-24)14-16-37-17-15-22-18-29(41-2)30(42-3)19-23(22)20-37;/h4-13,18-19H,14-17,20H2,1-3H3,(H,35,39)(H,36,38);1H |
| InChI Key | IQOJZZHRYSSFJM-UHFFFAOYSA-N |
| Use of | Elacridar Hcl (GF120918; GW0918) is a P-glycoprotein inhibitor, and has been used both in vitro and in vivo as a tool inhibitor of P-glycoprotein (Pgp) to investigate the role of transporters in the disposition of various test molecules.IC50 value:Target: P-glycoprotein In vitro, GF120918A demonstrated high plasma protein binding across species, although a definitive protein binding evaluation was precluded by poor recovery, particularly in buffer and in mouse, rat, and dog plasma. GF120918A did not demonstrate potent inhibition of several human cytochrome P450 enzymes evaluated in vitro, with IC(50) values well above concentrations anticipated to be achieved in vivo. Together, these data confirm the utility of GF120918A as a tool P-glycoprotein inhibitor in preclinical species and offer additional guidance on preclinical dose regimens likely to produce P-glycoprotein-mediated effects. Properties Name N-[4-[2-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)ethyl]phenyl]-5-methoxy-9-oxo-10H-acridine-4-carboxamide,hydrochloride Synonym More Synonyms Elacridar hydrochloride Biological Activity Description Elacridar Hcl (GF120918; GW0918) is a P-glycoprotein inhibitor, and has been used both in vitro and in vivo as a tool inhibitor of P-glycoprotein (Pgp) to investigate the role of transporters in the disposition of various test molecules.IC50 value:Target: P-glycoprotein In vitro, GF120918A demonstrated high plasma protein binding across species, although a definitive protein binding evaluation was precluded by poor recovery, particularly in buffer and in mouse, rat, and dog plasma. GF120918A did not demonstrate potent inhibition of several human cytochrome P450 enzymes evaluated in vitro, with IC(50) values well above concentrations anticipated to be achieved in vivo. Together, these data confirm the utility of GF120918A as a tool P-glycoprotein inhibitor in preclinical species and offer additional guidance on preclinical dose regimens likely to produce P-glycoprotein-mediated effects. Related Catalog Signaling Pathways >> Membrane Transporter/Ion Channel >> P-glycoprotein Research Areas >> Cancer References [1]. Sane R, Mittapalli RK, Elmquist WF. Development and evaluation of a novel microemulsion formulation of elacridar to improve its bioavailability. J Pharm Sci. 2013 Jan 18. [2]. Bankstahl JP, Bankstahl M, Romermann K, et al. Tariquidar and Elacridar Are Dose-Dependently Transported by P-Glycoprotein and Bcrp at the Blood-Brain Barrier: A Small-Animal PET and In-Vitro Study. Drug Metab Dispos. 2013 Jan 10. [3]. Sane R, Agarwal S, Elmquist WF. Brain distribution and bioavailability of elacridar after different routes of administration in the mouse. Drug Metab Dispos. 2012 Aug;40(8):1612-9. [5]. Kuppens IE, Witteveen EO, Jewell RC, et al. A phase I, randomized, open-label, parallel-cohort, dose-finding study of elacridar (GF120918) and oral topotecan in cancer patients. Clin Cancer Res. 2007 Jun 1;13(11):3276-85. [6]. Hong Xiao, et al. Polymeric nanovesicle as simultaneous delivery platform with Doxorubicin conjugation and Elacridar encapsulation for enhanced treatment of multidrug-resistant breast cancer. J. Mater. Chem. B. 2018 Oct. Chemical & Physical Properties Exact Mass 599.21900 PSA 92.89000 LogP 6.37310 InChIKey IQOJZZHRYSSFJM-UHFFFAOYSA-N Storage condition 2-8℃ Safety Information HS Code 2934999090 |
| Tax Rebate | 13.0% |
| Supervision | None. MFN tariff: 6.5%. Ordinary tariff: 20.0% |
| Transport Info | Product name: Summary 2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0% |
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