[CAS NO. 497259-23-1] TPPB
PRODUCTS SPECIFICATIONS [497259-23-1]
DESCRIPTION [497259-23-1]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 501.54 |
| Molecular Formula | C27H30F3N3O3 |
| SMILES | O=C(NC1=CC=C(N(C)[C@@H](C(C)C)C(N[C@H](CO)C2)=O)C2=C1)/C=C/C=C/C3=CC=C(C(F)(F)F)C=C3 |
1 Publications Citing Use of MCE
Summary
TPPB is a cell-permeable benzolactam-derived protein kinase C ( PKC ) activator with a K i of 11.9 nM.
IC50 & Target
|
PKC 11.9 nM (Ki) |
In Vitro
By use of a cell line derived from an Alzheimer’s disease patient, significant enhancement of sAPPα secretion is achieved at 1 μM concentration for TPPB (Compound 5e) [1] . TPPB has a role against Aβ 25-35 -induced neurotoxicity in PC12 cells. TPPB at concentration of 1 μM could antagonize Aβ 25-35 induced cell damage. TPPB could increase the phosphorylation of Akt, PKC, MARCKS and MAPK, which are inhibited by Aβ 25-35 treatment. TPPB inhibits the activation of caspase-3 induced by Aβ 25-35 [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
TPPB is evaluated for induction of hyperplasia after topical application to the shaved backs of outbred Sencar mice and shows a modest response at 300 μg [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 125 mg/mL ( 249.23 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.9939 mL | 9.9693 mL | 19.9386 mL |
| 5 mM | 0.3988 mL | 1.9939 mL | 3.9877 mL |
| 10 mM | 0.1994 mL | 0.9969 mL | 1.9939 mL |
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1.
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2.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.25 mg/mL (4.49 mM); Clear solution
References
- [1] Kozikowski AP, et al. New amide-bearing benzolactam-based protein kinase C modulators induce enhanced secretion of the amyloid precursor protein metabolite sAPPalpha. J Med Chem. 2003 Jan 30;46(3):364-73.
- [2] Yang HQ, et al. Neuroprotective effects of new protein kinase C activator TPPB against Aβ25-35 induced neurotoxicity in PC12 cells. Neurochem Res. 2012 Oct;37(10):2213-21.
