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首页 / 抑制剂/激动剂 / 细胞周期 / DHFR / Folinic acid calcium salt pentahydrate/亚叶酸钙水合物

Folinic acid calcium salt pentahydrate/亚叶酸钙水合物 {[allProObj[0].p_purity_real_show]}

货号：A246079 同义名： 亚叶酸钙五水合物 / Leucovorin Calcium Pentahydrate; Leucovorin calcium salt pentahydrate

Folinic acid calcium salt pentahydrate 是一种还原型叶酸，常与甲氨蝶呤联合使用，作为化疗药物的辅助剂，降低其毒性并提高疗效。

Folinic acid calcium salt pentahydrate/亚叶酸钙水合物 化学结构 CAS号：6035-45-6
Folinic acid calcium salt pentahydrate/亚叶酸钙水合物 化学结构
CAS号：6035-45-6
Folinic acid calcium salt pentahydrate/亚叶酸钙水合物 3D分子结构
CAS号：6035-45-6
Folinic acid calcium salt pentahydrate/亚叶酸钙水合物 化学结构 CAS号：6035-45-6
Folinic acid calcium salt pentahydrate/亚叶酸钙水合物 3D分子结构 CAS号：6035-45-6
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Folinic acid calcium salt pentahydrate/亚叶酸钙水合物 纯度/质量文件 产品仅供科研

货号：A246079 标准纯度： {[allProObj[0].p_purity_real_show]}
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产品名称 DHFR ↓ 其他靶点 纯度
Pralatrexate ✔ 99%+
Pemetrexed disodium ++++

DHFR, Ki: 7.2 nM

 		99%
Pyrimethamine ++

DHFR, IC50: 15.4 nM

 		98% HPLC
Pemetrexed ++++

DHFR , Ki: 7.2 nM

 		99+%
Methotrexate +

hDHFR, IC50: 24 nM

 		99% (contain ~10%water)
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Folinic acid calcium salt pentahydrate/亚叶酸钙水合物 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].

Folinic acid calcium salt pentahydrate/亚叶酸钙水合物 细胞实验

Cell Line
Concentration Treated Time Description References
Human aortic endothelial cells (HAEC) 10 μM 1 hour To evaluate the effect of BH4 treatment on intracellular BH4 and 7,8-BH2 levels. Results showed a transient increase in intracellular BH4 followed by accumulation of 7,8-BH2. Free Radic Biol Med. 2013 Oct;63:143-50.
Human umbilical vein endothelial cells (HUVEC) 500 nM 24 h Folinic acid reversed MTX-induced p38 MAPK and Akt phosphorylation and reduced MTX-induced pro-inflammatory cell adhesion molecules (VCAM1, ICAM1, and E-selectin) expression. Front Immunol. 2023 Jun 30;14:1209490.
MCA38 colorectal cancer cell line 10 μM 48 h To evaluate the effect of FOLFOX (including folinic acid) on MCA38 cells, confirming cell death and activation of inflammatory signaling. Br J Cancer. 2013 Oct 29;109(9):2396-403.

Folinic acid calcium salt pentahydrate/亚叶酸钙水合物 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c mice Acute Toxoplasma gondii RH strain infection model Oral administration 15 mg/kg Once daily for 7 consecutive days As a positive control drug to evaluate the therapeutic effect of folinic acid on acute Toxoplasma gondii infection Parasit Vectors. 2024 Mar 1;17(1):96
BALB/c mice Acute Toxoplasma gondii infection model Oral administration 15 mg/kg Once daily for 15 consecutive days Evaluated the therapeutic effect of folinic acid on acute infection, results showed all mice in the positive control drug groups survived Front Cell Dev Biol. 2021 Jun 11;9:684393
BALB/c mice Toxoplasma gondii infection model Oral 15 mg/kg Once a day for 30 days Evaluate the safety of folinic acid in Toxoplasma gondii infection model Front Microbiol. 2019 Sep 18;10:2152
BALB/c mice Acute T. gondii infection model Oral administration 15 mg/kg Once daily for 7 consecutive days To evaluate the therapeutic effect of folinic acid on acute T. gondii infection, all mice in the positive drug groups survived. Int J Parasitol Drugs Drug Resist. 2019 Apr;9:27-34
C57Bl/6 mice Colorectal liver metastases (CRLM) model Intraperitoneal (i.p.) 90 mg kg Weekly cycles, terminated one day after the third treatment To evaluate the effect of FOLFOX (including folinic acid) on the CRLM model, finding that tumour-related factors exacerbated FOLFOX-induced liver injury. Br J Cancer. 2013 Oct 29;109(9):2396-403.

Folinic acid calcium salt pentahydrate/亚叶酸钙水合物 动物研究

Dose Mice: 7 mg/kg[3] (i.p.)
Administration i.p.

Folinic acid calcium salt pentahydrate/亚叶酸钙水合物 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 - -

Folinic acid calcium salt pentahydrate/亚叶酸钙水合物 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.

Folinic acid calcium salt pentahydrate/亚叶酸钙水合物 实验方案

计算器
存储液制备 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

Folinic acid calcium salt pentahydrate/亚叶酸钙水合物 技术信息

CAS号6035-45-6
分子式C20H31CaN7O12
分子量 601.58
SMILES Code O=CN1C(C2=O)=C(NC(N)=N2)NCC1CNC3=CC=C(C(N[C@H](C([O-])=O)CCC([O-])=O)=O)C=C3.O.O.O.O.[Ca+2].O
MDL No. MFCD00149465
别名 亚叶酸钙五水合物 ;Leucovorin Calcium Pentahydrate; Leucovorin calcium salt pentahydrate
运输蓝冰
InChI Key NPPBLUASYYNAIG-ZIGBGYJWSA-L
Pubchem ID 135802074
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, 2-8°C
溶解方案

H2O: 10 mg/mL(16.62 mM)，配合低频超声助溶

Tags: Folinic acid calcium salt | 6035-45-6 | Leucovorin calcium salt | Antifolate | Cell Cycle/DNA Damage | Metabolic Enzyme/Protease | Antifolate | Endogenous Metabolite | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Folinic acid calcium salt pentahydrate/亚叶酸钙水合物 纯度/质量文件 | Folinic acid calcium salt pentahydrate/亚叶酸钙水合物 亚型比较 | Folinic acid calcium salt pentahydrate/亚叶酸钙水合物 生物活性 | Folinic acid calcium salt pentahydrate/亚叶酸钙水合物 动物研究 | Folinic acid calcium salt pentahydrate/亚叶酸钙水合物 临床数据 | Folinic acid calcium salt pentahydrate/亚叶酸钙水合物 参考文献 | Folinic acid calcium salt pentahydrate/亚叶酸钙水合物 实验方案 | Folinic acid calcium salt pentahydrate/亚叶酸钙水合物 技术信息

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