| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
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| 靶点 |
Thymidylate Synthase
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|---|---|
| 体外研究 (In Vitro) |
当单独使用甲氨蝶呤 (MTX) 时，异常细胞 (Abs) 和微核双核细胞 (MNBN) 的百分比呈浓度依赖性增加。核分裂指数 (NDI) 随着 MTX 浓度的升高而下降。同样，在所有实验中，添加 50 μg/mL 亚叶酸显着降低了 MNBN (40-68%) 和 Abs (36-77%) 的百分比。此外，在 5 μg/mL 亚叶酸下，观察到抑制作用（MNBN 为 12% 至 54%，Abs 为 20% 至 61%）[1]。
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| 体内研究 (In Vivo) |
在甲氨蝶呤 (MTX) 之后给予甲酰四氢叶酸（7.0 mg/kg；腹膜内注射；每隔一天；持续 3 周；Balb/c 幼年溶液）药物，似乎可以逆转 MTX 的生长抑制（长期关注 MTX 喂养的兔子）给予右旋普利 (5–20 mg/kg) 时，动脉粥样硬化进展缓慢 [2]。地拉普利（1-2 mg/kg，口服，每天一次，持续 5 周）在动物模型中研究高血压时：喂食兔子胆固醇 [2]
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| 动物实验 |
Animal/Disease Models: 24 3weeks old Balb/c young growing male mice (11.88±0.25 g) [2]
Doses: 7.0 mg/kg Route of Administration: intraperitoneal (ip) injection; every other day; for 3 weeks Experimental Results: After MTX administration appears to reverse this growth inhibition. |
| 参考文献 |
[1]. Keshava, C., et al., Inhibition of methotrexate-induced chromosomal damage by folinic acid in V79 cells. Mutat Res, 1998. 397(2): p. 221-8.
[2]. Iqbal MP, et al. Effect of methotrexate and folinic acid on skeletal growth in mice. Acta Paediatr. 2003 Dec;92(12):1438-44. |
| 分子式 |
C20H23N7O7
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|---|---|
| 分子量 |
473.446
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| 精确质量 |
473.1659
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| 元素分析 |
C, 50.74; H, 4.90; N, 20.71; O, 23.65
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| CAS号 |
58-05-9
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| 相关CAS号 |
Folinic acid calcium;1492-18-8;Folinic acid calcium salt pentahydrate;6035-45-6;Folinic acid disodium;163254-40-8;Folinic acid calcium hydrate;1097832-14-8;Folinic acid-d4 calcium hydrate
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| 外观&性状 |
Solid powder
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| SMILES |
C1C(N(C2=C(N1)N=C(NC2=O)N)C=O)CNC3=CC=C(C=C3)C(=O)N[C@@H](CCC(=O)O)C(=O)O
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| InChi Key |
VVIAGPKUTFNRDU-ABLWVSNPSA-N
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| InChi Code |
InChI=1S/C20H23N7O7/c21-20-25-16-15(18(32)26-20)27(9-28)12(8-23-16)7-22-11-3-1-10(2-4-11)17(31)24-13(19(33)34)5-6-14(29)30/h1-4,9,12-13,22H,5-8H2,(H,24,31)(H,29,30)(H,33,34)(H4,21,23,25,26,32)/t12?,13-/m0/s1
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| 化学名 |
(2S)-2-[[4-[(2-amino-5-formyl-4-oxo-3,6,7,8-tetrahydropteridin-6-yl)methylamino]benzoyl]amino]pentanedioic acid
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| 别名 |
Leucovorin; Folinic acid; HSDB-6544; HSDB6544; HSDB 6544
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| HS Tariff Code |
2934.99.9001
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| 存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| 溶解度 (体外) |
DMSO: 95~250 mg/mL (200.7~528.1 mM)
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|---|---|
| 溶解度 (体内) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.39 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.39 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.39 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. 1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL； 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果，工作液请现配现用！ 6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
| 制备储备液 | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1122 mL | 10.5608 mL | 21.1216 mL | |
| 5 mM | 0.4224 mL | 2.1122 mL | 4.2243 mL | |
| 10 mM | 0.2112 mL | 1.0561 mL | 2.1122 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液)：对于大多数产品，InvivoChem推荐用DMSO配置母液 (比如：5、10、20mM或者10、20、50 mg/mL浓度），个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息，或者很难将产品溶解在溶液中，请联系我们;
3、建议使用下列计算器进行相关计算（摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等）;
4、母液配好之后，将其分装到常规用量，并储存在-20°C或-80°C，尽量减少反复冻融循环。
计算结果:
工作液浓度： mg/mL；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度，请首先与我们联系。
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH2O，混匀澄清。
(1) 请确保溶液澄清之后，再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶；
(2) 一定要按顺序加入溶剂 (助溶剂) 。
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04060017 | Active Recruiting |
Drug: Levoleucovorin Calcium Other: Placebo |
Autism Spectrum Disorder Language Disorders |
Rossignol Medical Center | September 22, 2020 | Phase 2 |
| NCT02839915 | Active Recruiting |
Other: Placebo Drug: Folinic Acid |
Autism Spectrum Disorder | Rossignol Medical Center | August 13, 2020 | Phase 2 |
| NCT03750786 | Active Recruiting |
Drug: Arfolitixorin Drug: Leucovorin |
Colo-rectal Cancer | Isofol Medical AB | December 18, 2018 | Phase 3 |
| NCT00082706 | Active Recruiting |
Drug: Leucovorin Drug: 5-Fluorouracil (5-FU) |
Bladder Cancer Urethral Cancer |
M.D. Anderson Cancer Center | April 23, 2003 | Phase 2 |
| NCT00217737 | Active Recruiting |
Drug: Oxaliplatin Drug: Leucovorin Calcium |
Lynch Syndrome Stage IIA Colon Cancer AJCC v7 |
National Cancer Institute (NCI) |
August 4, 2005 | Phase 3 |
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