T0901317 is a potent, high affinity liver X receptor (LXR) agonist. T0901317 binds and activates PXR with the same nanomolar potency with which it stimulates LXR activity. T0901317 induces expression not only of LXR target genes, but also of PXR target genes in cells and animals. T0901317 decreases amyloid-β production in primary neurons in vitro. T0901317 also exhibits inverse agonist activity at constitutive androstane receptors (CAR). Although T0901317 is a much more potent activator of LXR than FXR, this ligand actually activates FXR more potently than a natural bile acid FXR ligand, chenodeoxycholic acid. T0901317 treatment of 11-week-old APP23 mice for 6 days showed a significant increase in ABCA1 expression and a decrease in the ratio of soluble APP (sAPP)beta- to sAPPalpha-cleavage products. T0901317 decreases amyloidogenic processing of APP in vitro and in vivo, thus supporting the search for potent and specific LXR ligands with properties allowing therapeutic application.
 |
Source | ARYA Atheroscler (2017). Figure 1. T0901317 |
| Method | PCR | |
| Cell Lines | Mice | |
| Concentrations | 30 mg/kg | |
| Incubation Time | 48 hour | |
| Results | In fact, a combination of T0901317 and anti-miR-33 insignificantly increased ABCA1 gene expression |
| Molecular Weight | 481.33 |
| Formula | C17H12F9NO3S |
| CAS Number | 293754-55-9 |
| Solubility (25°C) | DMSO 72 mg/mL Ethanol 60 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.
[3] Houck KA, et al. Mol Genet Metab. T0901317 is a dual LXR/FXR agonist.
| Related Liver X Receptor Products |
|---|
| Rovazolac
Rovazolac is a liver x receptor (LXR) modulator, which can be used in the study of immune system disorders and atopic dermatitis. |
| GW6340
GW6340 is an intestinal-specific LXR agonist. |
| Larsucosterol
Larsucosterol is an endogenous sulfated oxysterol and a potent hepatic X receptor (LXR) and DNA methylase (DNMTS) antagonist that regulates endogenous lipogenesis as well as inhibits cholesterol biosynthesis by lowering mRNA levels and inhibiting SREBP-1 activation. May be used in studies related to psoriasis. |
| 24(S)-Hydroxycholesterol
24(S)-Hydroxycholesterol (24S-OHC), the major brain cholesterol metabolite, plays an important role to maintain homeostasis of cholesterol in the brain. 24(S)-Hydroxycholesterol (24S-OHC) is one of the most efficient endogenous LXR agonist known and is present in the brain and in the circulation at relatively high levels. 24(S)-Hydroxycholesterol (24S-OHC) is a very potent, direct, and selective positive allosteric modulator of NMDARs with a mechanism that does not overlapthat of other allosteric modulators. |
| GW3965
GW3965 is a potent, selective liver X receptor (LXR) agonist with EC50s of 190 nM and 30 nM for hLXRα and hLXRβ, respectively. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
