RGX-104 hydrochloride is a small-molecule LXR (liver X receptor) agonist that modulates innate immunity via transcriptional activation of the ApoE gene. Oral administration of RGX-104 hydrochloride to animals bearing palpable tumors significantly suppresses the growth of multiple cancer types. Responses are seen across a wide spectrum of malignancies, including lung cancer, melanoma, glioblastoma, and ovarian, renal cell, triple-negative breast, and colon cancer.
| Molecular Weight | 632.54 |
| Formula | C34H34Cl2F3NO3 |
| CAS Number | 610318-03-1 |
| Solubility (25°C) | DMSO ≥ 70 mg/mL (May need warming) |
| 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.
| Related Liver X Receptor Products |
|---|
| 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. |
| GSK3987
GSK3987 is a pan LXRα/β agonist with EC50s of 50 nM, 40 nM for LXRα-SRC1 and LXRβ-SRC1, respectively. GSK3987 increases the expression of ABCA1 and SREBP-1c. GSK3987 induces cellular cholesterol efflux and triglyceride accumulation. |
| BMS-779788
BMS-779788 is a LXR partial agonist with IC50 values of 68 nM for LXRα and 14 nM for LXRβ. |
| Iristectorigenin B
Iristectorigenin B is a liver X receptor (LXR) modulator, which stimulates the transcriptional activity of both LXR-α and LXR-β. |
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