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HazMat fee for 500 gram (Estimated)
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USD 0.00
Limited Quantity
USD 15-60
Inaccessible (Haz class 6.1), Domestic
USD 80+
Inaccessible (Haz class 6.1), International
USD 150+
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Accessible (Haz class 3, 4, 5 or 8), International
VDR (vitamin D receptor), as a member of the nuclear receptor superfamily, mediates the biological activity of 1,25-dihydroxyvitamin D3 (calcitriol) which is generated from vitamin D by successive hydroxylations in the liver and kidney. VDR can regulate a variety of illnesses in intestine, kidney, bone, skin, heart, and various other organs[3]. Calcitriol, the most biologically active metabolite of vitamin D, is a non-selective VDR agonist with IC50 of 0.4 nM. Calcitriol is a potent inhibitor of PHA (phytohemagglutinin)-induced lymphocyte proliferation, achieving 70% inhibition of tritiated thymidine incorporation after 72 h in culture. Furthermore, calcitriol suppresses interleukin-2 (IL-2) production by PHA-stimulated peripheral blood mononuclear cells in a concentration-dependent fashion[4]. In HL-60 cells, a human myelomonocytic leukemia cell line, calcitriol arrests cells in G1; this effect is mediated through an increase in p27. Calcitriol mediated arrest in G0/G1 is also observed in human breastcancer lines. In vivo, a decrease in tumor volume induced by calcitriol correlates with a significant decrease in the intratumoral p21 expression[5].
Calcitriol/骨化三醇 细胞实验
Cell Line
Concentration
Treated Time
Description
References
FHC cells
100 nM
Calcitriol promoted the proliferation of FHC cells
Front Pharmacol. 2021 Nov 16;12:727704.
Primary cortical neurons
1 nM, 10 nM, 100 nM, 500 nM
24 h
To evaluate the effect of Calcitriol on neuronal cell viability. The results showed that 1 nM and 10 nM Calcitriol had no toxic effect, while 100 nM and 500 nM Calcitriol significantly reduced cell viability.
Mol Med. 2021 Sep 23;27(1):118.
AC16 cells
10 nM
24 h
To study the effect of Calcitriol on TNF-α-induced AC16 cell death, results showed that Calcitriol significantly increased cell viability.
Cells. 2022 May 18;11(10):1676.
AC16 cells
100 nM
24 h
To study the effect of Calcitriol on TNF-α-induced AC16 cell death, results showed that high-dose Calcitriol significantly increased cell viability.
Cells. 2022 May 18;11(10):1676.
SW480 cells
100 nM
Calcitriol inhibited the proliferation and migration capacity of SW480 cells
Front Pharmacol. 2021 Nov 16;12:727704.
LoVo cells
100 nM
Calcitriol inhibited the proliferation and migration capacity of LoVo cells
Front Pharmacol. 2021 Nov 16;12:727704.
HL-1 atrial myocytes
1 nM and 10 nM
48 h
To investigate whether Calcitriol downregulates FGFR1 expression through histone deacetylase (HDAC) activation. Results showed that Calcitriol significantly reduced FGFR1 expression in HL-1 cells.
J Biomed Sci. 2018 May 18;25(1):42.
osteoclast
1 nM, 10 nM, 100 nM
overnight
Calcitriol inhibited the fusion ability and the number of TRAP-positive differentiated osteoclasts in a dose-dependent manner.
Nutrients. 2018 Aug 25;10(9):1164.
preosteoblast 7F2 cells
1 nM, 10 nM, 100 nM
overnight
Calcitriol had no significant effect on Wnt 10b and Wnt 16 expression in preosteoblast 7F2 cells.
Nutrients. 2018 Aug 25;10(9):1164.
Calcitriol/骨化三醇 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
CD1 Elite mice
Traumatic brain injury (TBI) model
Gavage
0.5 µg/kg, 1 µg/kg, 3 µg/kg
Once daily for 14 days
To evaluate the neuroprotective effects of Calcitriol in TBI mice. The results showed that Calcitriol significantly ameliorated neurological deficits and histopathological changes following TBI, promoted the autophagic process, and activated Nrf2 signaling, thereby mitigating TBI-induced oxidative damage.
Mol Med. 2021 Sep 23;27(1):118.
C57BL/6 mice
4-nitroquinoline-1-oxide (4NQO) induced oral carcinogenesis model
Intraperitoneal injection
0.1 μg
Monday, Wednesday, and Friday for 16 weeks, 10 weeks, or 26 weeks
To evaluate the impact of Calcitriol on oral carcinogenesis at different stages of intervention and durations of exposure. Results showed that Calcitriol administered concurrently with 4NQO for 16 weeks significantly reduced premalignant lesions by 57%, while 26 weeks of Calcitriol treatment showed the highest renal CYP24A1 expression and the highest incidence of invasive SCC.
Neoplasia. 2019 Apr;21(4):376-388
Kunming mice
Myocardial infarction model
Oral gavage
0.0375 µg/kg, 0.075 µg/kg, 0.15 µg/kg
Once daily for 4 weeks
To study the effect of Calcitriol on cardiac function and remodeling in MI mice, results showed that Calcitriol significantly improved cardiac function and reversed adverse cardiac remodeling.
Cells. 2022 May 18;11(10):1676.
Nude mice
SW480 cell-derived xenograft model
Intraperitoneal injection
50 μg/kg
Three times a week for 2 weeks
Calcitriol significantly inhibited the growth of SW480 cell-derived xenograft tumors
Front Pharmacol. 2021 Nov 16;12:727704.
C57BL/6J mice
5/6 nephrectomy CKD model
Oral gavage
25 IU/kg, 150 IU/kg
Daily for one month
Calcitriol significantly promoted the growth of both trabecular and cortical bone in CKD mice, especially at the 150 IU/kg dose.
Displacement of 1-alpha, 25-(OH)[3H]D3 from human VDR expressed in COS1 cells, IC50=0.8 nM
17924616
COS7 cells
Function assay
24 h
Agonist activity at human VDR in COS7 cells assessed as induction of transcriptional transactivation after 24 hrs by mouse osteopontin luciferase reporter gene assay, EC50=0.5 nM
17904370
CV1 cells
Function assay
Activity on human VDR-mediated transcription of osteocalcin VDRE fused to thymidine kinase promoter/growth hormone reporter gene in CV1 cells, ED50=0.7 nM
17149880
HEK293 cells
Function assay
24 h
Agonist activity at human VDR in HEK293 cells assessed as induction of transcriptional transactivation after 24 hrs by mouse osteopontin luciferase reporter gene assay, EC50=1 nM
17904370
human A498 cells
0.01 μM
Function assay
4 h
Induction of CYP24 mRNA expression in human A498 cells at 0.01 μM after 4 hrs by RT-PCR analysis
21392983
human Caco-2 cells
Function assay
Effect on VDR transcriptional activity in human Caco-2 cells in presence of 5% fetal calf serum, EC50=3.52 nM
18054230
human HaCaT cells
Function assay
24 h
Transactivation of VDR in human HaCaT cells after 24 hrs by luciferase reporter gene assay, EC50=0.3215 μM
26367019
human HaCaT cells
Function assay
Inhibition of colony formation of human HaCaT cells
22404326
human HCT116
Cytotoxic assay
120 h
Cytotoxicity against human HCT116 assessed as decrease in cell count after 120 hrs, IC50=1e-05 μM
22926068
human HCT116 cells
20-40 μM
Function assay
24 h
Agonist activity at RAR (unknown origin) expressed in human HCT116 cells co-expressing RARE at 20 to 40 uM after 24 hrs by luciferase reporter gene assay
23276449
human HeLa cells
Function assay
16 h
Transactivation of GAL4-fused VDR ligand binding domain expressed in human HeLa cells after 16 hrs by luciferase reporter gene assay, EC50=1 nM
22957834
human HL60 cells
Function assay
Induction of human HL60 differentiation assessed as cells reducing nitro blue tetrazolium, ED50=1 nM
21902235
human HN12 cells
Proliferation assay
72 h
Antiproliferative activity against human HN12 cells assessed as decrease in cell number after 72 hrs by WST assay, IC50=0.553 μM
24900339
human HOS cells
Function assay
24 h
Activity at human VDR expressed in human HOS cells transfected with pGL3-hOc, pCDNA-hVDR and phRL-TK assessed as assessed as transcriptional activation measured 24 hrs post infection by luciferase reporter gene assay, EC50=1e-05 μM
21889334
human HOS/SF cells
Function assay
24 h
Transactivation of VDR-mediated osteocalcin promoter in human HOS/SF cells after 24 hrs by luciferase reporter gene assay, EC50=2.6e-05 μM
24900728
human MCF7 cells
Function assay
Agonist activity at zebrafish gal4-VDR LBD expressed in human MCF7 cells by luciferase reporter gene based transactivation assay, EC50=5.5 nM
22180837
human PBMC
Function assay
24 h
Inhibition of LPS-induced TNFalpha production in human PBMC after 24 hrs by ELISA, IC5=2.9e-05 μM
19309155
human PBMC
Function assay
24 h
Inhibition of LPS-induced IL12/23p40 production in human PBMC after 24 hrs by ELISA, IC50=1 nM
19309155
human peripheral blood mononuclear cells
Proliferation assay
In vitro inhibition of phytohemagglutininin-induced stimulation of human peripheral blood mononuclear cells proliferation, ED50=2.7 nM
11000014
human T47D cells
Proliferation assay
72 h
Antiproliferative activity against human T47D cells assessed as decrease in cell number after 72 hrs by WST assay, IC50=1.3 nM
24900339
human THP1 cells
Function assay
Activation of VDR in human THP1 cells assessed as increase in cathelicidin antimicrobial peptide mRNA expression by RT-PCR, EC50=10 nM
19309155
mouse C3H10T1/2 cells
0.5-5 μM
Function assay
24 h
Inhibition of Hedgehog signaling pathway in mouse C3H10T1/2 cells assessed as down regulation of Gli1 at 0.5 to 5 uM after 24 hrs by RT-PCR analysis
22226657
mouse LM05e cells
Proliferation assay
72 h
Antiproliferative activity against mouse LM05e cells assessed as decrease in cell number after 72 hrs by WST assay, IC50=3e-05 μM
24900339
mouse SVEC cells
Proliferation assay
72 h
Antiproliferative activity against mouse SVEC cells assessed as decrease in cell number after 72 hrs by WST assay, IC50=0.52 nM
24900339
rat osteosarcoma cells
Function assay
Induction of VDR-mediated 24-hydroxylase transcription in rat osteosarcoma cells by luciferase reporter gene assay, ED50=0.2 nM
21902235
rat ROS 17/2.8 cells
Function assay
16 h
Activity at VDR in rat ROS 17/2.8 cells assessed as transcriptional activation of 24-hydroxylase gene promoter after 16 hrs by luciferase reporter gene assay, EC50=0.2 nM
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