GlpBio

Antifolate

Antifolate(叶酸拮抗剂)

Antifolates are compounds that antagonise the actions of folic acid (vitamin B9). Folic acid's primary function in the body is as a cofactor to various methyltransferases involved in serine, methionine, thymidine and purine biosynthesis. Consequently antifolates inhibit cell division, DNA/RNA synthesis and repair and protein synthesis. Some such as Proguanil, Pyrimethamine and Trimethoprim selectively inhibit folate's actions in microbial organisms such as bacteria, protozoa and fungi. The majority of antifolates work by inhibiting dihydrofolate reductase (DHFR). Many are primarily DHFR inhibitors, but Raltitrexed is an inhibitor of thymidylate synthase, and Pemetrexed inhibits both and a third enzyme. Antifolates act specifically during DNA and RNA synthesis, and thus are cytotoxic during the S-phase of the cell cycle. Thus, they have a greater toxic effect on rapidly dividing cells.

Antifolate 相关产品(33)

  • GC10137 structure
    GC10137Trimethoprim
    CAS: 738-70-5
    纯度: >99.50%

    An antibiotic

  • GC10405 structure
    GC10405Methotrexate
    CAS: 59-05-2
    纯度: >98.00%

    甲氨蝶呤（Methotrexate）是一种抗叶酸类抗代谢药，有效抑制二氢叶酸还原酶（DHFR）活性，IC50约为7nM。

  • GC11558 structure
    GC11558Levomefolate calcium
    CAS: 151533-22-1

    A biologically active form of folic acid

  • GC11610 structure
    GC11610Pemetrexed
    CAS: 150399-23-8
    纯度: >99.50% / >98.00% / >99.00%

    An antifolate with anticancer activity

  • GC12919 structure
    GC12919Pralatrexate
    CAS: 146464-95-1
    纯度: >98.00%

    A dihydrofolate reductase inhibitor

  • GC14331 structure
    GC14331Folinic acid
    CAS: 58-05-9
    纯度: >99.50%

    亚叶酸 (Leucovorin) 是一种生物叶酸，通常与甲氨蝶呤 (MTX) 一起作为救援剂给药，以降低 MTX 诱导的毒性。

  • GC15306 structure
    GC15306Calcium N5-methyltetrahydrofolate
    CAS: 26560-38-3

    N5-甲基四氢叶酸钙 (NSC173328) 是左旋叶酸的钙盐，已被提议用于治疗心血管疾病和晚期癌症，如乳腺癌和结肠直肠癌。

  • GC16203 structure
    GC16203Leucovorin Calcium
    CAS: 6035-45-6
    纯度: >98.00%

    亚叶酸钙（亚叶酸钙盐五水合物）是一种生物叶酸，通常与甲氨蝶呤 (MTX) 一起作为救援剂给药，以降低 MTX 诱导的毒性。

  • GC16680 structure
    GC16680Levoleucovorin Calcium
    CAS: 80433-71-2
    纯度: >98.00%

    A reduced folic acid

  • GC17694 structure
    GC17694Pemetrexed disodium hemipenta hydrate
    CAS: 357166-30-4
    纯度: >99.00%

    Pemetrexed disodium hemipenta hydrate 是一种新型抗叶酸剂，LY231514 的五谷氨酸的 Ki 值分别为 1.3、7.2 和 65 nM，用于抑制胸苷酸合酶 (TS)、二氢叶酸还原酶 (DHFR) 和甘氨酰胺核糖核苷酸甲酰转移酶 (GARFT)。

  • GC17867 structure
    GC17867Pyrimethamine
    CAS: 58-14-0
    纯度: >99.50%

    A dihydrofolate reductase inhibitor

  • GC18404 structure
    GC18404Lometrexol
    CAS: 106400-81-1
    纯度: >98.00% / >97.50%

    A GART inhibitor

  • GC19495 structure
    GC19495DL-Folinic Acid (calcium salt)
    CAS: 1492-18-8
    纯度: >99.00%

    A reduced folic acid

  • GC32343 structure
    GC32343Diaveridine (EGIS-5645)
    CAS: 5355-16-8
    纯度: >98.00%

    A DHFR inhibitor with antimicrobial activity

  • GC32401 structure
    GC32401EC0489
    CAS: 1096702-14-5

    EC0489是叶酸和去乙酰长春碱酰肼的偶联物，是叶酸受体(FR)的高亲和力配体。有望治疗难治性或转移性肿瘤。是一种小分子-药物偶联物(SMDC)。

  • GC33322 structure
    GC33322LY 254155
    CAS: 135503-67-2

    LY254155是一种抗叶酸剂。LY254155抑制hGARFT及与mFBP结合，Kis分别为2.1±0.2和1.7±0.1nM。

  • GC33373 structure
    GC33373LY309887
    CAS: 127228-54-0

    LY309887是一种有效的二氢叶酸还原酶(GARFT)抑制剂，Ki值为6.5nM，具有抗肿瘤活性。

  • GC34309 structure
    GC34309Cycloguanil D6 (Chlorguanide triazine D6)

    CycloguanilD6是Cycloguanil的氘代化合物标准品。

  • GC35781 structure
    GC35781Cycloguanil D6 Nitrate

    Cycloguanil D6硝酸盐是Cycloguanil的氘代化合物标准品。

  • GC36486 structure
    GC36486LSN 3213128
    CAS: 1941211-99-9
    纯度: >99.50%

    LSN 3213128 是一种选择性、非经典、口服有效的抗叶酸剂，能够有效特异性抑制氨基咪唑-4-甲酰胺核糖核苷酸甲酰转移酶 (AICARFT) 的活性，IC50 值为 16 nM，在细胞中对其 IC50 值为 19 nM。

  • GC36589 structure
    GC36589Methotrexate metabolite
    CAS: 19741-14-1
    纯度: >98.00%

    Methotrexate metabolite (DAMPA)，是 Methotrexate 的活性代谢产物。 Methotrexate 是一种叶酸 (folic acid) 拮抗剂，广泛用作免疫抑制剂和化学治疗剂。

  • GC37938 structure
    GC37938WR99210
    CAS: 47326-86-3
    纯度: >99.50%

    WR99210 是一种有效的二氢叶酸还原酶 (DHFR) 抑制剂，IC50 为 Plasmodium falciparum)。

  • GC39820 structure
    GC39820Lometrexol hydrate
    CAS: 1435784-14-7
    纯度: >99.00%

    A GART inhibitor

  • GC42789 structure
    GC42789Aminopterin
    CAS: 54-62-6
    纯度: >98.00%

    A synthetic folic acid derivative