1. Protein Tyrosine Kinase/RTK
  2. c-Met/HGFR

Dihexa (Synonyms: PNB-0408; N-hexanoic-Try-Ile-(6)-amino hexanoic amide; Hexanoyl-Tyr-Ile-Ahx-NH2)

Cat. No.: HY-16969 Purity: >98.0%
Handling Instructions

Dihexa is an orally active, blood-brain barrier-permeable angiotensin IV analog; exhibits high affinity binding hepatocyte growth factor (HGF) with a Kd of 65 pM.

For research use only. We do not sell to patients.
Dihexa Chemical Structure

Dihexa Chemical Structure

CAS No. : 1401708-83-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 200 In-stock
2 mg USD 120 In-stock
5 mg USD 180 In-stock
10 mg USD 288 In-stock
50 mg USD 1020 In-stock
100 mg USD 1800 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Dihexa is an orally active, blood-brain barrier-permeable angiotensin IV analog; exhibits high affinity binding hepatocyte growth factor (HGF) with a Kd of 65 pM.

IC50 & Target

Kd: 65 pM (HGF)[1]

In Vitro

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[1].

In Vivo

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[2].

References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 1.9815 mL 9.9077 mL 19.8153 mL
5 mM 0.3963 mL 1.9815 mL 3.9631 mL
10 mM 0.1982 mL 0.9908 mL 1.9815 mL
Please refer to the solubility information to select the appropriate solvent.
Animal Administration
[2]

Dihexa is dissolved in 75% DMSO.

Rats: Serial dilutions of dihexa in 50% DMSO or water (for dilutions of 50 µg/mL or less) are prepared from the stock used to dose the animals to be used for preparation of a standard curve. 10 µL of each serial dilution is then added to 90 µL of blank plasma for final concentrations of 0.01, 0.02, 0.05, 0.1, 0.2, 1, 10, 20, 50, and 100 µg/mL. 80 µL of each plasma sample is transferred to previously prepared tubes containing 240 µL of ice-cold acetonitrile and vortexed vigorously. 10 µL of isotonic saline containing 100 µg/mL Nle-YI-(6) aminohexanoic amide as an internal standard is added to each sample on ice. The standard-curve plasma samples are then stored at −20°C and further processed alongside the pharmacokinetic study samples[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

504.66

Formula

C₂₇H₄₄N₄O₅

CAS No.

1401708-83-5

SMILES

OC1=CC=C(C[[email protected]](NC(CCCCC)=O)C(N[[email protected]](C(NCCCCCC(N)=O)=O)[[email protected]@H](C)CC)=O)C=C1

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 30 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Dihexa
Cat. No.:
HY-16969
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