Bavachin significantly inhibits melanin synthesis and TYR activity. Bavachin (10 µM) inhibits the expression of TYR and JNK proteins, and the expression of TYR, TRP-1, TRP-2, ERK1, ERK2 and JNK2 mRNA in A375 cells. ICI182780 and U0126 cAN significantly reverse the bavachin treatment on the protein expression levels and the mRNA expression of TYR, TRP-1, TRP-2, ERK1, ERK2 and JNK2. Bavachin accumulates lipid in a dose dependent manner in ORO staining experiments. Bavachin significantly increases the growth of preadipoctye at 10 µM compared with the control cells in MTT assay. Bavachin also increases BrdU incorporation into newly synthesized DNA during pre-adipocyte proliferation. BrdU incorporation is enhanced by insulin and further enhanced by co-treatment with insulin and bavachin at 2 and 10 µM. Bavachin activates adipogenic factors and increases PPARγ transcriptional activity in differentiated adipocytes. Bavachin enhances insulin-stimulated glucose uptake through GLUT4 translocation via Akt and AMPK pathway. BVN significantly increases both hMAO-A and hMAO-B activities. Bavachin shows ER ligand binding activity in competitive displacement of [3H] E2 from recombinant ER. The estrogenic activity of bavachin is characterized in a transient transfection system using ERα or ERβ and estrogen-responsive luciferase plasmids in CV-1 cells with an EC50 of 320 nM and 680 nM, respectively. Bavachin increases the mRNA levels of estrogen-responsive genes such as pS2 and PR, and decreases the protein level of ERα by proteasomal pathway.
| Cell Experiment | |
|---|---|
| Cell lines | MCF-7 BOS cells |
| Preparation method | Cells were treated with 10 nM E2, 1 μM tamoxifen and bavachin as indicated for 6 days. The cell growth was determined by using MTT based colorimetric assay. |
| Concentrations | 1 μM |
| Incubation time | 6 days |
| Animal Experiment | |
|---|---|
| Animal models | |
| Formulation | |
| Dosages | |
| Administration | |
| Molecular Weight | 324.37 |
| Formula | C20H20O4 |
| CAS Number | 19879-32-4 |
| Solubility (25°C) | 10 mM in DMSO |
| 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 Estrogen Receptor Products |
|---|
| hFSH-β-(33-53) TFA
hFSH-β-(33-53) TFA, a thiol-containing peptide which corresponds to a second FSH receptor-binding domain, is a FSHR (follicle-stimulating hormone receptor) antagonist. hFSH-β-(33-53) TFA inhibits binding of FSH to receptor and is a partial agonist of estradiol synthesis in Sertoli cells. |
| Yp537
Yp537 is an estrogen receptor (ER) inhibitor that blocks dimerization of the human estrogen receptor. |
| Palazestrant
Palazestrant is a novel, orally active, estrogen receptor antagonist and selective estrogen receptor degrader. It can be used in studies related to ER+/HER2+ breast cancer. |
| Acolbifene hydrochloride
Acolbifene hydrochloride is an active metabolite of EM800 and an orally available, selective estrogen receptor modulator (SERM) that inhibits estradiol-induced ERα (IC50 = 2 nM) and ERβ (IC50 = 0.4 nM) transcriptional activity, has significant anti-estrogenic effects on the mammary gland and uterus, and has anticancer activity. possesses anticancer activity. |
| Acolbifene
Acolbifene is an active metabolite of EM800 and an orally active pure anti-estrogen and selective estrogen receptor (ER) antagonist that inhibits estradiol-induced ERα (IC50 = 2 nM) and ERβ (IC50 = 0.4 nM) transcriptional activity and has anticancer activity. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
