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| ln Vivo |
In an intranasal davunetide (2 μg/kg) administered once daily for five days a week for sixteen weeks, a diabetic rat model demonstrated protection against problems of the central nervous system [3].
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| Animal Protocol |
Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rats (induced by intraperitoneal (ip) injection of streptozotocin (STZ)) [3]
Doses: 2 μg/kg Route of Administration: Intranasal administration starting the day after STZ injection, Daily dosing, 5 days per week, for 16 weeks Experimental Results: Impaired spatial memory in diabetic rats was observed in the water maze, manifested by an attenuated learning curve and worsened performance in the probe memory test. Davonidetide treatment Dramatically improved both measures. All experiments were performed in *Drosophila melanogaster*. Expression of htauON3R, htauON4R, and Aβ42;htauON4R was directed to motor neurons using the D42-Gal4 driver or pan-neuronally using Elav-Gal4. Davunetide (NAP) was dissolved in basic fly food at concentrations of 50 ng/mL, 500 ng/mL, 2.5 μg/mL, and 25 μg/mL. Larvae were reared on NAP-containing food from the egg stage (preventive protocol) or transferred to NAP food after 4 days for 1 day (rescue protocol). [1] Larval locomotion was assessed in wandering third instar larvae on 100 cm² plates for 2 min using Ethovision tracking software. Parameters measured included body wall contractions per minute, velocity, and meander. [1] For electron microscopy, larval peripheral nerves were dissected, fixed, and processed. Transverse sections were examined, and correctly aligned microtubule profiles were counted. [1] Axonal transport was assessed using a vGFP reporter expressed in motor neurons. Larvae were imaged, and the total area of vGFP accumulation in peripheral nerves was quantified. [1] NMJs were stained with anti-horseradish peroxidase (HRP) to visualize presynaptic boutons and anti-tubulin to visualize the cytoskeleton. NMJ area was measured. [1] Tau phosphorylation and protein levels were assessed by western blot of larval and adult head homogenates using antibodies against total tau and phospho-tau epitopes (AT8, AT180, etc.). [1] |
| References |
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| Additional Infomation |
Davinetide is an oligopeptide. Davinetide has been used in clinical trials to treat progressive non-fluent aphasia, progressive supranuclear palsy, predictive tau proteinosis (including corticobasal degeneration syndrome), and frontotemporal dementia associated with Parkinson's syndrome related to chromosome 17. Davinetide is the first drug to improve memory function by influencing the mechanisms that cause physical damage to neurofibrillary tangles in the brain. Neurofibrillary tangles are one of two known pathological markers of amnesic mild cognitive impairment (aMCI) and Alzheimer's disease (AD). Davinetide is derived from a naturally occurring neuroprotective brain protein called activity-dependent neuroprotective protein. Mechanism of Action: Davinetide interacts with microtubules to 1) prevent the formation of neurofibrillary tangles, protecting the microtubule network from "death signals"; and 2) repair the microtubule network if the brain cell death process has already begun. The repair of the microtubule network explains the improved cognitive abilities in treated animals compared to the untreated group.
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| Molecular Formula |
C36H60N10O12
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|---|---|
| Molecular Weight |
824.93
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| Exact Mass |
824.439
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| CAS # |
211439-12-2
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| Related CAS # |
211439-12-2;
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| PubChem CID |
9832404
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
1333.8±65.0 °C at 760 mmHg
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| Flash Point |
760.5±34.3 °C
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| Vapour Pressure |
0.0±0.6 mmHg at 25°C
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| Index of Refraction |
1.566
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| LogP |
-1.78
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| Hydrogen Bond Donor Count |
10
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| Hydrogen Bond Acceptor Count |
13
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| Rotatable Bond Count |
22
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| Heavy Atom Count |
58
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| Complexity |
1560
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| Defined Atom Stereocenter Count |
9
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| SMILES |
CC[C@@H]([C@H](NC([C@@H](NC([C@@H](NC([C@@H]1CCCN1C([C@@H](NC([C@@H](N)CC(N)=O)=O)C)=O)=O)C(C)C)=O)CO)=O)C(N2CCC[C@H]2C(N[C@H](C(O)=O)CCC(N)=O)=O)=O)C
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| InChi Key |
DWLTUUXCVGVRAV-XWRHUKJGSA-N
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| InChi Code |
InChI=1S/C36H60N10O12/c1-6-18(4)28(35(56)46-14-8-9-23(46)31(52)41-21(36(57)58)11-12-25(38)48)44-30(51)22(16-47)42-33(54)27(17(2)3)43-32(53)24-10-7-13-45(24)34(55)19(5)40-29(50)20(37)15-26(39)49/h17-24,27-28,47H,6-16,37H2,1-5H3,(H2,38,48)(H2,39,49)(H,40,50)(H,41,52)(H,42,54)(H,43,53)(H,44,51)(H,57,58)/t18-,19-,20-,21-,22-,23-,24-,27-,28-/m0/s1
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| Chemical Name |
(2S)-5-amino-2-[[(2S)-1-[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2,4-diamino-4-oxobutanoyl]amino]propanoyl]pyrrolidine-2-carbonyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-3-methylpentanoyl]pyrrolidine-2-carbonyl]amino]-5-oxopentanoic acid
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| Synonyms |
Davunetide AL 208 AL 108
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~151.53 mM)
H2O : ~100 mg/mL (~121.22 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (2.52 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.2122 mL | 6.0611 mL | 12.1222 mL | |
| 5 mM | 0.2424 mL | 1.2122 mL | 2.4244 mL | |
| 10 mM | 0.1212 mL | 0.6061 mL | 1.2122 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT01056965 | COMPLETED | Drug: davunetide (AL-108, NAP) Drug: Placebo nasal spray |
Corticobasal Degeneration Syndrome Frontotemporal Dementia With Parkinsonism Linked to Chromosome 17 Predicted Tauopathies, Including |
University of California, San Francisco | 2010-01 | Phase 1 |
| NCT01110720 | COMPLETED | Drug: Davunetide Drug: Placebo |
Progressive Supranuclear Palsy | Allon Therapeutics | 2010-10 | Phase 2 Phase 3 |
| NCT00505765 | COMPLETEDWITH RESULTS | Drug: AL-108 Drug: AL-108 Drug: Placebo Drug: Placebo |
Schizophrenia | University of California, Los Angeles | 2007-07 | Phase 2 |
| NCT00404014 | COMPLETED | Drug: AL-208 Drug: Placebo |
Mild Cognitive Impairment | Allon Therapeutics | 2006-08 | Phase 2 |
| NCT00422981 | COMPLETED | Drug: AL-108 Drug: AL-108 Drug: Placebo |
Mild Cognitive Impairment, So Stated | Allon Therapeutics | 2007-01 | Phase 2 |
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