L-685,458 is a potent, selective, structurally novel γ-secretase inhibitor; equipotent inhibitor of both Aβ1-42 and Aβ1-40 production.
| Molecular Weight | 672.85 |
| Formula | C39H52O6N4 |
| CAS Number | 292632-98-5 |
| Solubility (25°C) | DMSO ≥ 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[2] Manuel Hitzenberger, et al. Uncovering the Binding Mode of γ -Secretase Inhibitors
| Related Gamma-secretase/Beta-secretase Products |
|---|
| RE(EDANS)EVNLDAEFK(DABCYL)R
RE (EDANS) EVNLDAEFK (DABCYL) R is an EDANS and DABCYL double-labeled peptide，serves as a fluorescent substrate for BACE1(Em=360nm，Ex=528nm). |
| β-Secretase inhibitor
β-Secretase inhibitor ([Asn670, Sta671, Val672]-Amyloid β Peptide (662-675)) is a β-secretase and BACE1 inhibitor (IC50: 25 nM for β-secretase). |
| Mca-SEVNLDAEFK(Dnp)
Mca-SEVNLDAEFK(Dnp) is a Beta-secretase 1 (BACE-1) peptide FRET substrate, containing the 'Swedish' Lys-Met/Asn-Leu mutation of the amyloid precursor protein (APP) β-secretase cleavage site. |
| BACE1-IN-10
BACE1-IN-10 is a potent BACE1 Inhibitor. |
| OM99-2 TFA
OM99-2 TFA, an eight residue peptidomimetic, tight-binding inhibitor of human brain memapsin 2 with a Ki value of 9.58 nM. |
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