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Folinic acid calcium salt pentahydrate

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Chemical Structure| 6035-45-6 同义名 : 亚叶酸钙五水合物 ;Leucovorin Calcium Pentahydrate;Leucovorin calcium salt pentahydrate
CAS号 : 6035-45-6
货号 : A246079
分子式 : C20H31CaN7O12
纯度 : 98%
分子量 : 601.578
MDL号 : MFCD00149465
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 :

H2O: 10 mg/mL(16.62 mM)，配合低频超声助溶
动物实验配方：

PO 0.5% CMC-Na 80 mg/mL clear

生物活性
描述 The biologically active form of folic acid is tetrahydrofolate which is essential for DNA synthesis. Tetrahydrofolate is oxidised to dihydrofolate during DNA synthesis and is regenerated to its active form by the enzyme dihydrofolate reductase. Inhibition of this enzyme prevents DNA synthesis and causes failure of cell renewal. This leads to breaks in epithelial surfaces resulting in oropharyngeal and intestinal ulceration. Methotrexate (MTX) is the most powerful antagonist to inhibit dihydrofolate reductase. Folinic acid is an analogue of tetrahydrofolate and so bypasses the dihydrofolate reductase block. It thus supplies the tetrahydrofolate compounds needed for DNA synthesis [3]. Treatment with folinic acid calcium pentahydrate (CF) could cause improved development in the heart and vessels in MTX-treated embryos, which proved that MTX induced the malformations by inhibiting dihydrofolate reductase (DHFR). The transcript levels of genes such as hand2, mef2a, mef2c, and flk-1 were reduced in MTX-treated embryos. Compared with the MTX-treated group, the transcript levels of hand2, mef2a, mef2c, and flk-1 were increased in the MTX + CF group [4]. Folinic Acid Calcium Pentahydrate may also be useful in the treatment of acute methotrexate overdose [3].
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
NCT00720109 Adult B Acute Lymphoblastic Le... 展开 >>ukemia With t(9;22)(q34;q11.2); BCR-ABL1 Childhood B Acute Lymphoblastic Leukemia With t(9;22)(q34;q11.2); BCR-ABL1 Untreated Adult Acute Lymphoblastic Leukemia Untreated Childhood Acute Lymphoblastic Leukemia 收起 << Phase 2 Phase 3 Completed - -
NCT01256398 Acute Lymphoblastic Leukemia ... 展开 >> Adult B Acute Lymphoblastic Leukemia With t(9;22)(q34.1;q11.2); BCR-ABL1 Untreated Adult Acute Lymphoblastic Leukemia 收起 << Phase 2 Active, not recruiting - -
NCT00720109 - Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.66mL

0.33mL

0.17mL

8.31mL

1.66mL

0.83mL

16.62mL

3.32mL

1.66mL
参考文献

[1]Correale P, Cusi MG, et al. Dendritic cell-mediated cross-presentation of antigens derived from colon carcinoma cells exposed to a highly cytotoxic multidrug regimen with gemcitabine, oxaliplatin, 5-fluorouracil, and leucovorin, elicits a powerful human antigen-specific CTL response with antitumor activity in vitro. J Immunol. 2005 Jul 15;175(2):820-8.

[2]Van der Wilt CL, Pinedo HM, et al. Elevation of thymidylate synthase following 5-fluorouracil treatment is prevented by the addition of leucovorin in murine colon tumors. Cancer Res. 1992 Sep 15;52(18):4922-8.

[3] Calcium leucovorin - folinic acid rescue. Drug Ther Bull. 1978 Feb 3;16(3):11-2.

[4]Sun S, Gui Y, Wang Y, Qian L, Liu X, Jiang Q, Song H. Effects of methotrexate on the developments of heart and vessel in zebrafish. Acta Biochim Biophys Sin (Shanghai). 2009 Jan;41(1):86-96. doi: 10.1093/abbs/gmn010.