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Dihexa (PNB-0408)

Catalog No.GC30768

Dihexa (PNB-0408) Chemical Structure

Size Price Stock Qty
10mM*1mLinDMSO
$153.00
In stock
2mg
$92.00
In stock
5mg
$138.00
In stock
10mg
$220.00
In stock
50mg
$782.00
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100mg
$1,379.00
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Sample solution is provided at 25 µL, 10mM.

Quality Control

Quality Control & SDS

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Protocol

Animal experiment:

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].

References:

[1]. Benoist CC, et al. The procognitive and synaptogenic effects of angiotensin IV-derived peptides are dependent on activation of the hepatocyte growth factor/c-met system. J Pharmacol Exp Ther. 2014 Nov;351(2):390-402.
[2]. McCoy AT, et al. Evaluation of metabolically stabilized angiotensin IV analogs as procognitive/antidementia agents. J Pharmacol Exp Ther. 2013 Jan;344(1):141-54.

Background

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.

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].

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].

[1]. Benoist CC, et al. The procognitive and synaptogenic effects of angiotensin IV-derived peptides are dependent on activation of the hepatocyte growth factor/c-met system. J Pharmacol Exp Ther. 2014 Nov;351(2):390-402. [2]. McCoy AT, et al. Evaluation of metabolically stabilized angiotensin IV analogs as procognitive/antidementia agents. J Pharmacol Exp Ther. 2013 Jan;344(1):141-54.

Chemical Properties

Cas No. 1401708-83-5 SDF
Synonyms N/A
Chemical Name N/A
Canonical SMILES OC1=CC=C(C[C@H](NC(CCCCC)=O)C(N[C@H](C(NCCCCCC(N)=O)=O)[C@@H](C)CC)=O)C=C1
Formula C27H44N4O5 M.Wt 504.66
Solubility DMSO : ≥ 30 mg/mL (59.45 mM) Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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