|(1R,3S,Z)-5-((E)-2-((1R,3aS,7aR)-1-((2R,5R,E)-5,6-二甲基庚-3-烯-2-基)-7a-甲基六氢-1H-茚-4(2H)-亚基)亚乙基)-4-亚甲基环己烷-1,3-二醇|CsnPharm

CAS No.: 54573-75-0

Doxercalciferol/度骨化醇 Catalog No. CSN12209

Synonyms: 1.alpha.-Hydroxyvitamin D2;1α-Hydroxyvitamin D2;1alpha-Hydroxyvitamin D2

Doxercalciferol is a synthetic vitamin D2 analog, suppressing parathyroid synthesis and secretion, used to treat secondary hyperparathyroidism and metabolic bone disease.

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技术信息

生物活性

描述Doxercalciferol (DOX) is a Vitamin D2 analog, acts as an activator of Vitamin D receptor, and prevent renal disease. DOX had a beneficial effect on age-related bone deteriorations in aging mice by promoting osteoblast activity and cartilage regeneration and inhibiting osteoclast-specific genes expression^[3]. Doxercalciferol (0.083, 0.167 or 0.333 μg/kg, i.p.) elevates serum phosphorus at Week 6 in 5/6 nephrectomized (NX) rats. Doxercalciferol (0.167 and 0.333 μg/kg) also increases serum calcium and Ca × P at Weeks 2 and 6, and enhances increased pulse wave velocity (PWV) at Week 6 in 5/6 nephrectomized (NX) rats. Doxercalciferol blocks PTH from rising at 0.083 μg/kg, and lowers serum PTH to the SHAM level^[4]. Doxercalciferol was administered intraperitoneally at 150 ng, 3 times per week (Monday, Wednesday, Friday) for 6 weeks. Rats on HS diet with doxercalciferol administration had significant decrease in cardiac hypertrophy and improved cardiac function compared to the HS + vehicle. In addition, there was a significant decrease in plasma brain natriuretic peptide (BNP) level and tissue atrial natriuretic factor (ANF) mRNA level with doxercalciferol treatment. Doxercalciferol also significantly reduced the level of protein kinase C-α (PKCα)^[5]. Doxercalciferol (125 ng/kg, i.p. thrice per week) increases expression of VDR mRNA level and renal expression of TRPV5 in NON mice fed a HF diet. Doxercalciferol also improves proteinuria, prevents loss of podocytes, and accumulation of extracellular matrix proteins in HF diet-induced mice^[6].
临床研究
NCT号适应症或疾病临床期招募状态预计完成时间地点
NCT01717989 - - Completed - -
NCT01717989 - - Completed - -
NCT01181531 - - Completed - -
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参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.4234 mL
- 12.1169 mL
- 24.2337 mL
- 5 mM
- 0.4847 mL
- 2.4234 mL
- 4.8467 mL
- 10 mM
- 0.2423 mL
- 1.2117 mL
- 2.4234 mL

技术信息

CAS号

54573-75-0

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C28H44O2

运输

蓝冰

分子量

412.65

别名

1.alpha.-Hydroxyvitamin D2;1α-Hydroxyvitamin D2;1alpha-Hydroxyvitamin D2;1-hydroxy Vitamin D2;Hectorol;1-Hydroxyergocalciferol;TSA 840;度骨化醇

溶解度

DMSO	155.0 mg/mL (375.6 mM)
Water	insoluble

动物实验配方

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NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT01717989	-	-	Completed	-	-
NCT01717989	-	-	Completed	-	-
NCT01181531	-	-	Completed	-	-
NCT01181531	Hyperparathyroidism, Secondary	Phase 4	Completed	-	-
NCT00135304	Secondary Hyperparathyroidism	Phase 4	Completed	-	-
NCT00977080	Chronic Kidney Disease ... more >> Secondary Hyperparathyroidism Hemodialysis Collapse <<	Phase 4	Completed	-	-
NCT00977080	-	-	Completed	-	-
NCT02282813	Chronic Kidney Disease ... more >> Hyperparathyroidism, Secondary Vitamin D Deficiency Collapse <<	Phase 3	Completed	-	-
NCT01799317	Bone Mineralization Defect	Phase 4	Unknown	June 2014	United States, California ... more >> Loma Linda University Recruiting Loma Linda, California, United States, 92354 Contact: Shobbha Sahney, MD 909-558-8242 ssahney@llu.edu Principal Investigator: Shobha Sahney, MD Childrens Hospital Los Angeles Recruiting Los Angeles, California, United States, 90027 Contact: Kevin Lemley, MD 323-361-2295 klemley@chla.usc.edu Principal Investigator: Kevin Lemley, MD Collapse <<
NCT02282813	-	-	Completed	-	-
NCT01100723	-	-	Completed	-	-
NCT01100723	Secondary Hyperparathyroidism ... more >> Chronic Kidney Disease Collapse <<	Phase 4	Completed	-	United States, Virginia ... more >> Lynchburg Nephrology Associates, P.L.L.C. Lynchburg, Virginia, United States, 24501 Collapse <<
NCT00560300	Secondary Hyperparathyroidism ... more >> Renal Osteodystrophy Collapse <<	Phase 2	Completed	-	-
NCT00749736	Chronic Kidney Disease	Phase 4	Completed	-	United States, Indiana ... more >> Indiana University School of Medicine Indianapolis, Indiana, United States, 46202 Collapse <<
NCT00257920	Chronic Kidney Disease, Stage ... more >>5 Secondary Hyperparathyroidism Collapse <<	Phase 4	Completed	-	United States, Nebraska ... more >> Bellevue, Nebraska, United States, 68123 Omaha, Nebraska, United States, 68131 Collapse <<
NCT00257920	-	-	Completed	-	-
NCT00454350	Secondary Hyperparathyroidism	Phase 4	Completed	-	United States, Minnesota ... more >> Minneapolis, Minnesota, United States Collapse <<
NCT00502268	Coronary Calcification ... more >> Endstage Renal Disease Parathyroid Hormone Collapse <<	Phase 4	Withdrawn(study never initiate... more >>d) Collapse <<	-	United States, North Carolina ... more >> Davita East Charlotte Dialysis Unit Charlotte, North Carolina, United States, 28208 Collapse <<
NCT00463021	Secondary Hyperparathyroidism	Phase 4	Completed	-	United States, California ... more >> Downey, California, United States Paramount, California, United States United States, Florida Hudson, Florida, United States United States, Georgia Augusta, Georgia, United States Decatur, Georgia, United States United States, Pennsylvania Pittsburgh, Pennsylvania, United States United States, Tennessee Nashville, Tennessee, United States United States, Virginia Norfolk, Virginia, United States Collapse <<
NCT00123461	Secondary Hyperparathyroidism ... more >> Renal Failure Chronic Renal Insufficiency Collapse <<	Phase 4	Completed	-	United States, Arizona ... more >> AKDHC Medical Research Services Phoenix, Arizona, United States, 85012 United States, California UCLA Diabetes Reseach Center Alhambra, California, United States Apex Research of Riverside Riverside, California, United States, 92501 United States, District of Columbia George Washington University Hospital Washington, District of Columbia, United States, 20037 United States, Florida Discovery Medical Research Group Ocala, Florida, United States, 34471 Nephrology Associates Palm Beach Gardens, Florida, United States, 33410 United States, Georgia Georgia Kidney Associates, Inc. Marietta, Georgia, United States, 30060 United States, Michigan Michigan Kidney Consultants, P.C. Pontiac, Michigan, United States, 48341 United States, Minnesota Twin Cities Clinical Research Brooklyn Center, Minnesota, United States, 55430 United States, New York Montefiore Medical Center Bronx, New York, United States University of Rochester Medical Center Rochester, New York, United States, 14642 United States, North Carolina Wake Nephrology Associates, PA Raleigh, North Carolina, United States Wake Forest University School of Medicine Winston-Salem, North Carolina, United States United States, North Dakota Altru Health System Research Center Grand Forks, North Dakota, United States, 58201 United States, Pennsylvania DaVita Lewiston Dialysis Center Lewiston, Pennsylvania, United States, 17044 Temple University Philadelphia, Pennsylvania, United States United States, Virginia Virginia Commonwealth University Richmond, Virginia, United States Puerto Rico Instituto Renal del Este Caguas, Puerto Rico, 00725 Jose Cangiano, MD San Juan, Puerto Rico, 00918 Collapse <<
NCT00646282	Hyperparathyroidism, Secondary	Phase 4	Terminated(slow enrollment and... more >> discontinued once original principal investigator left Emory) Collapse <<	-	United States, Georgia ... more >> Emory University Atlanta, Georgia, United States, 30322 Collapse <<
NCT00528788	-	-	Completed	-	-
NCT00528788	Hyperparathyroidism, Secondary... more >> Kidney Failure, Chronic Collapse <<	Phase 4	Completed	-	United States, North Carolina ... more >> Duke University Medical Center Dialysis Unit Durham, North Carolina, United States, 27705 Collapse <<
NCT00022412	Prostate Cancer	Phase 2	Completed	-	United States, Iowa ... more >> Holden Comprehensive Cancer Center at University of Iowa Iowa City, Iowa, United States, 52242-1002 United States, New York James P. Wilmot Cancer Center at University of Rochester Medical Center Rochester, New York, United States, 14642 United States, Wisconsin Veterans Affairs Medical Center - Madison Madison, Wisconsin, United States, 53705 Meriter Hospital Madison, Wisconsin, United States, 53715 University of Wisconsin Comprehensive Cancer Center Madison, Wisconsin, United States, 53792-6164 Medical College of Wisconsin Cancer Center Milwaukee, Wisconsin, United States, 53226-3596 Collapse <<
NCT00052832	Leukemia Myel... more >>odysplastic Syndromes Myelodysplastic/Myeloproliferative Diseases Collapse <<	Phase 2	Completed	-	United States, Wisconsin ... more >> University of Wisconsin Comprehensive Cancer Center Madison, Wisconsin, United States, 53792 Collapse <<
NCT00285467	Renal Osteodystrophy	Not Applicable	Completed	-	United States, Indiana ... more >> Indiana University School of Medicine Indianapolis, Indiana, United States, 46202 Collapse <<
NCT00582582	Prostate Cancer	Phase 2	Terminated(Lack of drug supply... more >> for doxercalciferol for this study) Collapse <<	-	United States, Wisconsin ... more >> University of Wisconsin Madison, Wisconsin, United States, 53792-5669 Collapse <<
NCT00511017	Solid Tumors	Phase 1	Terminated(Slow accrual.)	-	United States, Texas ... more >> UT MD Anderson Cancer Center Houston, Texas, United States, 77030 Collapse <<
NCT00646282	-	-	Terminated(slow enrollment and... more >> discontinued once original principal investigator left Emory) Collapse <<	-	-
NCT00285467	-	-	Completed	-	-
NCT00601107	Moderate to Severe Chronic Pla... more >>que Psoriasis Collapse <<	Phase 2	Completed	-	-
NCT00889629	Chronic Kidney Disease ... more >> Kidney Transplantation Collapse <<	Phase 4	Unknown	January 2010	United States, New York ... more >> SUNY Downstate Medical Center Recruiting Brooklyn, New York, United States, 11234 Contact: Sima Terebelo, MPH, RPA-C 718-270-8216 Principal Investigator: Mariana Markell, MD Sub-Investigator: Sima Terebelo, MPH, RPA-C Collapse <<
NCT00418600	Secondary Hyperparathyroidism	Phase 4	Completed	-	United States, Arkansas ... more >> Hot Springs, Arkansas, United States United States, California Downey, California, United States Tarzana, California, United States United States, Georgia Atlanta, Georgia, United States United States, Ohio Cincinnati, Ohio, United States United States, Pennsylvania Pittsburgh, Pennsylvania, United States United States, Texas Houston, Texas, United States United States, Washington Spokane, Washington, United States Collapse <<
NCT00601107	-	-	Completed	-	-
NCT00792857	Chronic Kidney Disease ... more >> Secondary Hyperparathyroidism Chronic Renal Insufficiency Chronic Renal Failure Collapse <<	Phase 1	Completed	-	United States, Arizona ... more >> Pivotal Reseach Centers Peoria, Arizona, United States, 85381 United States, Massachusetts Western New England Renal and Transplant Associates Springfield, Massachusetts, United States, 01107 United States, Ohio University of Cincinnati Cincinnati, Ohio, United States, 45206 United States, Pennsylvania Northeast Clinical Research Allentown, Pennsylvania, United States, 18103-6379 United States, Tennessee Vanderbilt University Nashville, Tennessee, United States, 37232 United States, Texas Southwest Houston Research Ltd. Houston, Texas, United States, 77099 Collapse <<
NCT02859896	Secondary Hyperparathyroidism-... more >>Chronic Kidney Disease Collapse <<	Phase 3	Recruiting	April 2, 2020	-

Doxercalciferol/度骨化醇 Catalog No. CSN12209

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