Relative receptor affinities, metabolic and mitogenic potencies, and IR off-rates [% of human insulin].

<p>All assays were performed in at least three independent experiments. Data are means ± SD and presented relative to human insulin. For human insulin, IR assay IC₅₀ values were in the picomolar affinity range, IGF-IR assay IC₅₀ values were in the nanomolar affinity range, rFFC assay EC₅₀ values were in the picomolar range, and mitogenic assay EC₅₀ values were in the nanomolar range (HMECs) and low nanomolar range (L6-hIR). The dissociation rate constant for human insulin was (3.7±0.3×10⁻² min⁻¹).</p

Representative dissociation curves of [¹²⁵I]-labelled insulin or analogue from BHK-hIR cells.

<p>Dissociation was measured at different time points and the residual binding expressed as a percentage of initial binding. Dissociation of (<b>A</b>) B10D (♦) and B10E (▪); (<b>B</b>) B10W (▴), human insulin (•), and B10R (▾). Data points are means ± SEM (n = 3).</p

Representative dose-response profiles for mitogenic potency determination.

<p>Human insulin (•) or insulin analogue (B10D (♦), B10E (▪), or B10A (▾)) stimulated incorporation of [³H]-thymidine into DNA is shown in (<b>A</b>) L6-hIR cells and (<b>B</b>) HMECs. Data points are means ± SEM (n = 3).</p

Relative receptor binding affinities.

<p>Receptor binding affinities for the solubilised IR-A (light teal), IR-B (dark teal) and IGF-IR (gray) relative to human insulin. The gray dotted line represents 100% binding affinity compared to that of human insulin. Data are means ± SD (n = 3).</p