There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.
Type
HazMat fee for 500 gram (Estimated)
Excepted Quantity
USD 0.00
Limited Quantity
USD 15-60
Inaccessible (Haz class 6.1), Domestic
USD 80+
Inaccessible (Haz class 6.1), International
USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic
USD 100+
Accessible (Haz class 3, 4, 5 or 8), International
ER (Estrogen Receptor) is the receptor of estrogens. The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. ER has two receptor subtypes, ERα and ERβ. ERα and ERβ have different tissue distributions and each receptor has similar or unique roles in estrogen-dependent gene expressions.
PHTPP is an selective ERβ antagonist. PHTPP showed a relative binding affinity 36-fold selective for ERβ than ERα[1]. In HEC-1-A cells transfected with estrogen-responsive reporter gene plasmids, 1 μM PHTPP inhibited estrogen stimulated ERβ activity but did not suppress estrogen stimulated ERα activity[2]. 10 μM PHTPP effectively inhibited ERβ transcriptional activity in HEK293 cells transfected with ERβ expressing vector[3]. At the concentrations of 10, 15 and 20 μM, PHTPP dose-dependently inhibited the growth of bladder cancer cells J82, 647v and T24 detected at day 6. J82 cells treated by 20 μM PHTPP had less invasive ability than control group[3].
In a mouse model of BBN-induced bladder cancer, 10 μl of 10 mM PHTPP solution i.p. injected every other day for 12 weeks resulted in smaller tumor masses and better survival rate compared to control group. Moreover, 100% of the mice in the control group developed tumors with muscle invasion while the data was only around 33% in the PHTPP treated group[3].
PHTPP 细胞实验
Cell Line
Concentration
Treated Time
Description
References
MCF7 cells
100 nM
24 hours
PHTPP inhibits ERβ-mediated glycolytic metabolism
J Natl Cancer Inst. 2017 Mar 1;109(3):1-14.
Fibroblast-like synoviocytes (FLSs)
5 nM
24 hours
PHTPP partially reversed the upregulation of GPX4, LPAR3, and ESR2 in FLSs induced by LXA4
Redox Biol. 2024 Jul;73:103143.
Patient-derived BSCs
100 nM
12 days
PHTPP significantly reduces mammosphere formation
J Natl Cancer Inst. 2017 Mar 1;109(3):1-14.
Human uterine artery endothelial cells (hUAECs)
1 μM
24 hours
To investigate the effect of PHTPP (ERβ antagonist) on estradiol-stimulated AT2R expression. Results showed that PHTPP completely attenuated estradiol-induced AT2R mRNA and protein expression.
PHTPP did not inhibit E2β-induced PGI2 production in P-UAECs, indicating that E2β-induced PGI2 production is primarily mediated via ER-α and independent of ER-β
Hypertension. 2013 Feb;61(2):509-18.
Rat thoracic aorta vascular smooth muscle cells (VSMCs)
5 μmol/L
PHTPP, as a specific ERβ antagonist, was used to block the inhibitory effect of farrerol on VSMC proliferation, showing that PHTPP significantly attenuated the inhibitory effect of farrerol
Acta Pharmacol Sin. 2011 Apr;32(4):433-40.
Neonatal rat cardiomyocytes
100 nM
PHTPP prevented the inhibition of BMP4-induced BMP4 protein expression by estrogen
Br J Pharmacol. 2015 Dec;172(23):5586-95.
PHTPP 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
SD rats
MIA-induced KOA model
Intraperitoneal injection
100 μg/kg
Injected before each exercise session for 4 weeks
PHTPP partially reversed the improvement in pain behavior and joint pathology in KOA rats induced by treadmill exercise
Redox Biol. 2024 Jul;73:103143.
NOD/SCID mice
MCF7 xenograft model
Daily injections
4 mg/kg
Daily for five weeks
PHTPP significantly reduces tumor volume
J Natl Cancer Inst. 2017 Mar 1;109(3):1-14.
C57BL/6J mice
Cyclophosphamide-induced DOR model
Intraperitoneal injection
2 mg/kg or 4 mg/kg
Every other day for 14 days
To evaluate the therapeutic effect of PHTPP on DOR model mice. Results showed that PHTPP treatment restored normal sex hormone secretion, estrus cycle duration, follicle development, oocyte quality, and litter size.
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