Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C36H54N6O5 |
| Molecular Weight | 650.8512 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 5 / 5 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CN[C@H](CC(C)C)C(=O)N[C@H](C(C)C)C(=O)N[C@H](CC1=CC=CC=C1)C(=O)N[C@H](CC2=CC=CC=C2)C(=O)N[C@H](CC(C)C)C(N)=O
InChI
InChIKey=TUSUWHFYKZZRIG-JQWMYKLHSA-N
InChI=1S/C36H54N6O5/c1-22(2)18-27(32(37)43)39-34(45)29(20-25-14-10-8-11-15-25)40-35(46)30(21-26-16-12-9-13-17-26)41-36(47)31(24(5)6)42-33(44)28(38-7)19-23(3)4/h8-17,22-24,27-31,38H,18-21H2,1-7H3,(H2,37,43)(H,39,45)(H,40,46)(H,41,47)(H,42,44)/t27-,28-,29-,30-,31-/m1/s1
Apan (PPI-1019) is the lead compound of a series of β-amyloid-derived peptides designed by Praecis Pharmaceuticals in the US to interact with β-amyloid peptide, facilitating its clearance. Apan is derived from the D-enantiomeric Cholyl-LVFFA-NH2. Apan is developed by Praecis Pharmaceuticals to treat Alzheimer's Disease. Apan inhibits the aggregation of beta-amyloid and its associated nerve cell toxicity. In addition, Apan reaches the brain in quantities that are sufficient to block the aggregation of beta-amyloid molecules and alter the course of the disease. PPI-1019 completed phase I and II clinical trials and was found to be safe, well tolerated and amenable to cross bbb. After peptide administration, levels of Aβ1-40 in the CSF increased, which might be discussed as a sign for Aβ clearance out of the brain. PI-1019 had been in phase I/II clinical trials by Praecis Pharmaceuticals (acquired by GlaxoSmithKline in 2007) for the treatment of Alzheimer's disease(AD). However, this study had been discontinued.
Originator
Approval Year
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2F25P9Y22O
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290828-45-4
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9830969
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DTXSID60951685
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PPI-1019
Created by
admin on Fri Dec 15 15:28:47 GMT 2023 , Edited by admin on Fri Dec 15 15:28:47 GMT 2023
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PRIMARY | PPI-1019 (Apan) inhibits the aggregation of beta-amyloid and its associated nerve cell toxicity. In addition, Apan reaches the brain in quantities that are sufficient to block the aggregation of beta-amyloid molecules and alter the course of the disease. Accumulation of beta-amyloid in the brain is often thought of as a defect in the ability to clear beta-amyloid from the brain through the cerebral spinal fluid (CSF). Both humans and transgenic mice with Alzheimer's disease plaques show increased levels of beta-amyloid in the brain and decreased levels in the CSF. Transgenic mice treated with Apan show significant increases in beta-amyloid levels in the CSF, indicating that Apan is able to mobilize beta-amyloid in the brain and may be facilitating its clearance. | ||
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DB05832
Created by
admin on Fri Dec 15 15:28:47 GMT 2023 , Edited by admin on Fri Dec 15 15:28:47 GMT 2023
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ACTIVE MOIETY
