Molecular Formula | C27H44N4O5 |
Molar Mass | 504.66 |
Density | 1.111±0.06 g/cm3(Predicted) |
Melting Point | >209°C (dec.) |
Boling Point | 866.2±65.0 °C(Predicted) |
Solubility | DMSO: ≥ 30 mg/mL |
Appearance | Solid |
Color | White to Off-White |
pKa | 9.83±0.15(Predicted) |
Storage Condition | Hygroscopic, Refrigerator, under inert atmosphere |
Physical and Chemical Properties | Appearance: white powder |
Use | Sequence: Hexanoyl-Tyr-Ile-Ahx-NH2 |
In vitro study | Dihexa binds with high affinity to HGF and both dihexa and its parent compound Norleucine 1-AngIV induce c-Met phosphorylation in the presence of subthreshold concentrations of HGF and augment HGF-dependent cell scattering. Further, dihexa and Nle1-AngIV induce hippocampal spinogenesis and synaptogenesis similar to HGF itself. Dihexa effectively inhibits HGF dimerization at 1 μM. While dihexa at 1 nM and 10 pM alone does not activate c-Met, it markedly augments the capacity of HGF at 1.25 and 2.5 ng/mL to activate c-Met. |
In vivo study | Dihexa has a long circulating half-life. Dihexa exhibits procognitive activity. Dihexa reverses scopolamine-dependent spatial learning deficits. It improves spatial learning in aged rats. Dihexa induces spinogenesis in cultured hippocampal neurons. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.982 ml | 9.908 ml | 19.815 ml |
5 mM | 0.396 ml | 1.982 ml | 3.963 ml |
10 mM | 0.198 ml | 0.991 ml | 1.982 ml |
5 mM | 0.04 ml | 0.198 ml | 0.396 ml |
Biological activity | Dihexa (PNB-0408), an oligopeptide reagent, is an angiotensin IV analog with oral activity and permeability of the blood-brain barrier. Dihexa binds hepatocyte growth factor (HGF) with high affinity with a Kd value of 65 pM and enhances its activity against receptor c-Met. Dihexa showed excellent antipsychotic activity and improved cognitive function in animal models. Dihexa has the potential to study Alzheimer's. |
target | Kd: 65 pM (HGF) |
in vitro study | dihexa binds with high affinity to HGF and both dihexa and its parent compound Norleucine 1-AngIV inuce c-Met phosphorylation in the presence of subthreshold concentrations of HGF and augment HGF-dependent cell scattering. Further, dihexa and Nle1-AngIV induce hippocampal spinogenesis and synaptogenesis similar to HGF itself. Dihexa effectively inhibits HGF dimerization at 1 μM. While dihexa at 1 nM and 10 pM alone does not activate c-Met, it markedly augments the capacity of HGF at 1.25 and 2.5 ng/mL to activate c-Met. |
in vivo study | Dihexa has a long circulating half-life. Dihexa exhibits procognitive activity. Dihexa reverses scopolamine-dependent spatial learning deficits. It improves spatial learning in aged rats. Dihexa induces spinogenesis in cultured hippocampal neurons. |