Elacridar

SKU: orb1305209

Description

Elacridar (GG918) is a potent, dual inhibitor of the efflux transporters P-glycoprotein and BCRP. It is widely used in pharmacological research to enhance the bioavailability and brain penetration of co-administered drugs in both in vitro and in vivo models.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 143664-11-3
• MW: 563.64
• Purity: >99.99% (May vary between batches)
• Formula: C₃₄H₃₃N₃O₅
• SMILES: COc1cc2CCN(CCc3ccc(NC(=O)c4cccc5c4[nH]c4c(OC)cccc4c5=O)cc3)Cc2cc1OC
• Target: P-gp,BCRP
• Solubility: DMSO:7.86 mg/mL (13.95 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  HEK293 cells:0.41 μM|MDCK cells:0.43 μM|MCF-7 cells:0.4 μM|MDCK cells-II:0.4 μM
• In Vivo:
  METHODS: Elacridar (GG918) was administered to FVB wild-type mice in three different ways (2.5 mg/kg, intravenous injection; 100 mg/kg, intraperitoneal injection; 100 mg/kg, oral administration) to study the pharmacokinetic parameters of Elacridar (GG918) in plasma and brain. RESULTS The pharmacokinetic parameters of Elacridar (GG918) in plasma and brain were different in the three administration METHODS: the half-life in plasma after intravenous administration was 4.4 hours, in brain was 1.5 hours, and the Kp value was 0.82; the half-life in plasma after intraperitoneal injection was 4.3 hours, in brain was 9.2 hours, and the Kp value was 0.48; the half-life in plasma after intraperitoneal injection was 20 hours, in brain was 16 hours, and the Kp value was 4.31.
• In Vitro:
  METHODS: MCF-7, Caki-1 and 786-O cell lines were treated with Elacridar (GG918) (5 μM, 24 hours). Cell lysates were prepared and loaded into each well. Protein expression was determined by immunoblotting. β-actin expression was detected to normalize the total protein load. RESULTS Elacridar (GG918) affected the expression levels of P-glycoprotein and ABCG2 proteins in MCF-7 and 786-O cell lines; and affected the intracellular accumulation of Tc-MIBI in MCF-7 and 786-O cells.
• Cell Research:
  3.0×103 cells per well are seeded in a 96-well plate. After 24 h incubation, an optimum concentration gradient of elacridar is added to each well. After culturing for 48 h, cell viability is assessed using the proliferation reagent, MTT. Control cells are treated with the vehicle only, 0.1% DMSO. After this nal incubation, the medium is aspirated and precipitated formazan crystals are dissolved in DMSO (100 μL/well). The absorbance of each well is measured at 540 nm, and a reference wavelength of 650 nm is read with a multiskan JX microplate reader. Cell viability is calculated as percentage of the control value. (Only for Reference)

Storage & Handling

• Storage: store at low temperature,keep away from direct sunlight,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Cluster of differentiation 243, CD243, Breast cancer resistance protein, 786-O, ABCB1, ABCG2, BCRP, cancer, Inhibitor, inhibit, Multidrug resistance protein 1, MCF-7, MDR1, GW120918, GW-120918, GW 120918, GW 0918, GW0918, GW-0918, Elacridar, GG 918, GF120918, GF-120918, GF 120918, GG-918, GG918, sunitinib, P-glycoprotein, P-gp (P-glycoprotein), P-gp, Pgp

Compound Identifiers

PubChem CID

119373