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Valganciclovir HCl

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Chemical Structure| 175865-59-5 同义名 : Valganciclovir (hydrochloride);Ro 107-9070/194;Valganciclovir hydrochloride
CAS号 : 175865-59-5
货号 : A247777
分子式 : C14H23ClN6O5
纯度 : 98%
分子量 : 390.823
MDL号 : MFCD08460118
存储条件:

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 50 mg/mL(127.94 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 50 mg/mL(127.94 mM)

动物实验配方:
生物活性
描述 Cytomegalovirus (CMV) is a herpes virus that causes disease in severely immunocompromized patients. The ganciclovir prodrug valganciclovir, avalyl ester of ganciclovir, is rapidly converted to ganciclovir during the first pass process in the gut wall and is used to treat CMV infection. In vitro, valganciclovir inhibited the uptake of glycylsarcosine in a dose-dependent manner with IC50 values of 1.69 ± 0.30 mM in Caco-2 cells and 0.046 ± 0.005 mM in SKPT cells, respectively. Likewise, it inhibited the uptake of the dipeptide in a dose-dependent manner with IC50 values of 2.84 ± 0.42 mM in PEPT1-expressing cells and 0.176 ± 0.012 mM in PEPT2-expressing cells[3]. For patients with CMV viremia, valganciclovir (900 mg b.i.d. for 7 days) was effective as pre-emptive therapy with rate of viral clearance at 28 days of 89.5%[4].
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
NCT02227641 Patients Undergoing Allogeneic... 展开 >> Stem Cell Transplantation 收起 << Phase 1 Phase 2 Unknown March 2017 Germany ... 展开 >> Medical Center Augsburg Recruiting Augsburg, Germany, 86156 Contact: Christoph Schmid, MD, PhD    0049 821 4002736       Principal Investigator: Christoph Schmid, MD, PhD          Charité University Hospital Berlin Recruiting Berlin, Germany, 13353 Contact: Armin H Gerbitz, MD, PhD    ++49 30 450565256    armin.gerbitz@charite.de    Contact: Lutz Uharek, MD, PhD       lutz.uharek@charite.de    Sub-Investigator: Lutz Uharek, MD, PhD          Principal Investigator: Armin Gerbitz, MD, PhD          Universitiy Hospital Erlangen Recruiting Erlangen, Germany, 91054 Contact: Anita Kremer, MD, PhD    ++49 9131 8543183    anita.kremer@uk-erlangen.de    Contact: Bernd Spriewald, MD, PhD    ++49 9131 8543116    bernd.spriewald@uk-erlangen.de    Sub-Investigator: Katja San Niccolo, MD          University of Mainz Recruiting Mainz, Germany, 55131 Contact: Eva Wagner, MD          Principal Investigator: Eva Wagner, MD          University of Munich LMU Recruiting Munich, Germany, 81377 Contact: Johanna Tischer, MD    0049 89 70954240       Principal Investigator: Johanna Tischer, MD          University of Regensburg Not yet recruiting Regensburg, Germany, 93053 Contact: Ernst Holler, MD, PhD    0049 941 9445570       Principal Investigator: Ernst Holler, MD, PhD 收起 <<
NCT00078559 Kidney Transplantation ... 展开 >> Kidney Disease 收起 << Phase 1 Phase 2 Completed - United States, Wisconsin ... 展开 >> University of Wisconsin - Department of Medicine Madison, Wisconsin, United States, 53792-1735 收起 <<
NCT02188719 Liver Transplantation Phase 1 Recruiting January 2022 United States, California ... 展开 >> University of California, San Francisco Recruiting San Francisco, California, United States, 94143 Contact: Monique Koenigsberg    415-502-3016    Monique.Koenigsberg@ucsf.edu    Principal Investigator: Sandy Feng, MD, PhD          United States, Illinois Northwestern University Recruiting Chicago, Illinois, United States, 55905 Contact: Patrice Al-Saden    312-503-1058    palsaden@northwestern.edu    Principal Investigator: Josh Levitsky, MD          United States, Minnesota Mayo Clinic Recruiting Rochester, Minnesota, United States, 55905 Contact: Julie Gecox Hanson, CCRP    507-293-6592    Gecox.Julie@mayo.edu    Principal Investigator: Timucin Taner, MD, PhD 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.56mL

0.51mL

0.26mL

12.79mL

2.56mL

1.28mL

25.59mL

5.12mL

2.56mL

参考文献

[1]Chawla JS, Ghobadi A, et al. Oral valganciclovir versus ganciclovir as delayed pre-emptive therapy for patients after allogeneic hematopoietic stem cell transplant: a pilot trial (04-0274) and review of the literature. Transpl Infect Dis. 2012 Jun;14(3):259-67.

[2]Sugawara M, Huang W, et al. Transport of valganciclovir, a ganciclovir prodrug, via peptide transporters PEPT1 and PEPT2. J Pharm Sci. 2000 Jun;89(6):781-9.

[3]Sugawara M, Huang W, Fei YJ, Leibach FH, Ganapathy V, Ganapathy ME. Transport of valganciclovir, a ganciclovir prodrug, via peptide transporters PEPT1 and PEPT2. J Pharm Sci. 2000 Jun;89(6):781-9

[4]Chawla JS, Ghobadi A, et al. Oral valganciclovir versus ganciclovir as delayed pre-emptive therapy for patients after allogeneic hematopoietic stem cell transplant: a pilot trial (04-0274) and review of the literature. Transpl Infect Dis. 2012 Jun;14(3):259-67