2227651-65-0
Chemical Structure
DA5-CH
Synonym(s): KP405
- CAS No.: 2227651-65-0
- Formula:C253H390N74O72
- Molecular Weight:5620.26
SMILES: O=C(NC(C)(C)C(N[C@@H](CCC(O)=O)C(NCC(N[C@@H]([C@H](O)C)C(N[C@@H](CC1=CC=CC=C1)C(N[C@@H]([C@H](O)C)C(N[C@@H](CO)C(N[C@@H](CC(O)=O)C(N[C@@H](CC2=CC=C(C=C2)O)C(N[C@@H](CO)C(N[C@@H]([C@@H](C)CC)C(N[C@@H](CC3=CC=C(C=C3)O)C(N[C@@H](CC(C)C)C(N[C@@H](CC(O)=O)C(N[C@@H](CCCCN)C(N[C@@H](CCC(N)=O)C(N[C@@H](C)C(N[C@@H](C)C(NC(C)(C)C(N[C@@H](CCC(O)=O)C(N[C@@H](CC4=CC=CC=C4)C(N[C@@H](C(C)C)C(N[C@@H](CC(N)=O)C(N[C@@H](CC5=CNC6=CC=CC=C56)C(N[C@@H](CC(C)C)C(N[C@@H](CC(C)C)C(N[C@@H](C)C(NCC(NCC(N7[C@@H](CCC7)C(N[C@@H](CO)C(N[C@@H](CO)C(NCC(N[C@@H](C)C(N8[C@@H](CCC8)C(N9[C@@H](CCC9)C(N%10[C@@H](CCC%10)C(N[C@@H](CO)C(N[C@@H](CCCCN)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCC(N)=O)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCCCN)C(N[C@@H](CCCCN)C(N[C@@H](CCCNC(N)=N)C(NCC(N[C@@H](CC%11=CC=C(C=C%11)O)C(N)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)[C@H](CC%12=CC=C(C=C%12)O)N
Biological Activity: DA5-CH (KP405) is a blood-brain barrier-permeable GLP-1/GIP receptor agonist. DA5-CH activates GLP-1 and GIP receptors, inhibits the NF-κB inflammatory pathway, reduces α-synuclein (α-synuclein) levels, restores the expression of tyrosine hydroxylase and neurotrophic factors, improves motor function, decreases amyloid plaques and phosphorylated tau protein levels in the hippocampus, restores synaptic plasticity, regulates the PI3K/AKT/GSK3β and CREB signaling pathways, and alleviates mitochondrial stress. DA5-CH can be used for research on Parkinson's disease and Alzheimer's disease[1][2][3][4][5][6][7].
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DA5-CH | DA5-CH (KP405) is a blood-brain barrier-permeable GLP-1/GIP receptor agonist. DA5-CH activates GLP-1 and GIP receptors, inhibits the NF-κB inflammatory pathway, reduces α-synuclein (α-synuclein) levels, restores the expression of tyrosine hydroxylase and neurotrophic factors, improves motor function, decreases amyloid plaques and phosphorylated tau protein levels in the hippocampus, restores synaptic plasticity, regulates the PI3K/AKT/GSK3β and CREB signaling pathways, and alleviates mitochondrial stress. DA5-CH can be used for research on Parkinson's disease and Alzheimer's disease. | |||||||||||||||||||||
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References
- [1]. Lv M, et al. The GLP-1/GIP dual-receptor agonist DA5-CH inhibits the NF-κB inflammatory pathway in the MPTP mouse model of Parkinson's disease more effectively than the GLP-1 single-receptor agonist NLY01. Brain and behavior. 2021 Aug;11(8):e2231.
- [2]. Cao Y, et al. DA5-CH, a novel GLP-1/GIP dual agonist, effectively ameliorates the cognitive impairments and pathology in the APP/PS1 mouse model of Alzheimer's disease. Eur J Pharmacol. 2018 May 15;827:215-226.
- [3]. Li C, et al. The novel GLP-1/GIP analogue DA5-CH reduces tau phosphorylation and normalizes theta rhythm in the icv. STZ rat model of AD. Brain and behavior. 2020 Mar;10(3):e01505.
- [4]. Zhang L, et al. DA5-CH and Semaglutide Protect against Neurodegeneration and Reduce -Synuclein Levels in the 6-OHDA Parkinson's Disease Rat Model. Parkinson's disease. 2022;2022:1428817. [Content Brief]
- [5]. Zhang L, et al. The Novel Dual GLP-1/GIP Receptor Agonist DA-CH5 Is Superior to Single GLP-1 Receptor Agonists in the MPTP Model of Parkinson's Disease. Journal of Parkinson's disease. 2020;10(2):523-542. [Content Brief]
- [6]. Hölscher C, et al. Glucagon-like peptide 1 and glucose-dependent insulinotropic peptide hormones and novel receptor agonists protect synapses in Alzheimer's and Parkinson's diseases. Frontiers in synaptic neuroscience. 2022;14:955258.
- [7]. Rhea EM, et al. Brain uptake pharmacokinetics of albiglutide, dulaglutide, tirzepatide, and DA5-CH in the search for new treatments of Alzheimer's and Parkinson's diseases. Tissue barriers. 2024 Oct;12(4):2292461.
