ChemiSCREEN Membrane Preparation Recombinant Human MC ₁ Melanocortin Receptor

The melanocortin-1 receptor (MC₁) is a member of the G-protein-coupled receptor family of proteins that is responsible for regulating skin and hair color. The MC₁ receptor is regulated by the physiological agonists alpha-melanocyte-stimulating hormone (alphaMSH) and adrenocorticotropic hormone (ACTH), and antagonist agouti signaling protein (ASP) (Rouzud et al., 2005). In 1995 a landmark study demonstrated that over 80% of humans with red hair or fair skin have a dysfunctional variant of the MC₁ gene (Valverde et al., 1995). MC₁ is, therefore, a major determinant of sun sensitivity and genetic risk factor for melanoma and non-melanoma skin cancer. Millipore′s MC₁ membrane preparations are crude membrane preparations made from our proprietary stable recombinant cell lines to ensure high-level of GPCR surface expression; thus, they are ideal HTS tools for screening of agonists and antagonists of MC₁. The membrane preparations exhibit a Kd of 1.3nM for [¹²⁵I]-[Nle⁴, D-Phe⁷]-α-MSH (NDP-αMSH). With 0.3 nM [¹²⁵I]-NDP-αMSH, 5μg/well MC₁ Membrane Prep typically yields greater than 50-fold signal-to-background ratio.

Human MC1 GPCR membrane preparation for Radioligand binding Assays & GTPγS binding.

Radioligand binding assay and GTPγS binding.

Liquid in packaging buffer: 50 mM Tris pH 7.4, 10% glycerol and 1% BSA with no preservatives. Packaging method: Membranes protein were adjusted to 1 mg/mL in packaging buffer, and dispensed at 1 mL/vial. Vials were rapidly frozen, and stored at -80°C.

Maintain frozen at -70°C for up to 2 years. Do not freeze and thaw.

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