58-05-9
基本信息
5-甲醯-5,6,7,8-四氫葉酸
菊白葉酸
5-甲酰-5,6,7,8-四氢叶酸
LEUCOVORIN
5-formyl-5,6,7,8-tetrahydropteroyl-l-glutamicacid
leucoverin
5-formyl-5,6,7,8-tetrahydrofolate
5-formyltetrahydrofolate
5-formyltetrahydrofolic acid
N5-formyl-5,6,7,8-tetrahydrofolate
N5-formyl-tetrahydrofolate
2-[4-[(2-amino-5-formyl-4-oxo-1,6,7,8-tetrahydropteridin-6-yl)methylamino]benzoyl]aminopentanedioic acid
N5-Formyl-H4F
(6R,S)-5-Formyltetrahydrofolate
10-Formyl-7,8-dihydrofolic acid
5-Formyl-5,6,7,8-tetrahydrofolic acid
5-Formyltetrahydropteroylglutamic acid
Glutamic acid, N-[p-[[(2-amino-5-formyl-5,6,7,8-tetrahydro-4-hydroxy-6-pteridinyl)methyl]amino]benzoyl]-, L- (8CI)
Leucal
levoleucovorin
L-Glutamic acid, N-[4-[[(2-amino-5-formyl-1,4,5,6,7,8-hexahydro-4-oxo-6-pteridinyl)methyl]amino]benzoyl]- (9CI)
l-Leucovorin
物理化学性质
| 熔点 | 245°C (rough estimate) |
| 比旋光度 | D20 +14.26° (c = 3.42 as anhydr Ca salt) |
| 沸点 | 573.92°C (rough estimate) |
| 密度 | 1.4485 (rough estimate) |
| 折射率 | 1.6800 (estimate) |
| 储存条件 | under inert gas (nitrogen or Argon) at 2–8 °C |
| 酸度系数(pKa) | 3.1, 4.8, 10.4(at 25℃) |
| 水溶解性 | >1350g/L(25 ºC) |
| CAS 数据库 | 58-05-9(CAS DataBase Reference) |
安全数据
| 危险性符号(GHS) |  GHS07 |
| 警示词 | 警告 |
| 危险性描述 | H302-H315-H319-H335 |
| 防范说明 | P261-P280-P301+P312-P302+P352-P305+P351+P338 |
| 毒害物质数据 | 58-05-9(Hazardous Substances Data) |
化学品安全说明书(MSDS)
(2S)-2-[[4-[(2-Amino-5-formyl-4-oxo-1,6,7,8-tetrahydropteridin-6-yl)methylamino]benzoyl]amino]pentanedioic acid(58-05-9).msds常见问题列表
亚叶酸（Leucovorin），化学名N-[4-[(2-氨基-5-甲酰基-1,4,5,6,7,8-六氢-4-氧代-6-蝶啶基)甲基]氨基]苯甲酰-L-谷氨酸，目前已被广泛应用于癌症的联合化疗。
亚叶酸通过叶酸盐的摄取吸收途径进入人体。一旦进入细胞它便迅速代谢为5-亚甲基四氢叶酸酯。5-亚甲基四氢叶酸酯是叶酸的活性形式，可以参与尿嘧啶转换为胸腺嘧啶的单碳转移反应。亚叶酸因此能够对抗叶酸拮抗剂引起的四氢叶酸酯形成受阻。
亚叶酸（亚叶酸钙）是还原型叶酸（folate）的一种特殊形式，给予CFD的儿童高剂量亚叶酸干预，可以改善他们的神经和发育异常。叶酸代谢异常与儿童自闭症发生有关。叶酸相关通路的基因多态性可能导致叶酸代谢异常。研究发现产前和受孕期间补充叶酸能够降低子代自闭症的发病风险。
左旋亚叶酸作为抗肿瘤的解毒剂和抗巨幼细胞贫血的辅助用药，其剂量是亚叶酸的1/2，左旋亚叶酸不需要被二氢叶酸还原酶还原即可参加利用叶酸盐作为一碳单位来源的反应，且左旋亚叶酸可以主动或被动地通过细胞膜；左旋亚叶酸基本作用和叶酸相同，但效果优于叶酸，同时左旋亚叶酸也具有刺激白细胞生长成熟的作用，能改善巨幼细胞性贫血。
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Human Endogenous Metabolite
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MTX alone induces a concentration-related increase in % micronucleated binucleated cells (MNBN) and % aberrant cells (Abs). There is a decrease in nuclear division index (NDI) with increase in MTX concentration. Similarly, the mitotic index (MI) also decreases in all concentrations of MTX tested. The addition of Folinic acid at 50 μg/ mL significantly reduces % MNBN (40-68%) and % Abs (36-77%). Inhibition is also seen at 5 μg/ mL Folinic acid (12 to 54% for MNBN and 20 to 61% for Abs) .
Folinic acid (7.0 mg/kg; intraperitoneal injection; every second day; for 3 weeks; Balb/c young growing male mice) treatment following methotrexate (MTX) administration appears to reverse this growth inhibition (Chronic administration of MTX induces suppression of skeletal growth in mice).
| Animal Model: | 24 Balb/c young growing male mice aged 3 weeks (11.88 ± 0.25 g) |
| Dosage: | 7.0 mg/kg |
| Administration: | Intraperitoneal injection; every second day; for 3 weeks |
| Result: | Following methotrexate (MTX) administration appears to reverse this growth inhibition. |