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)

  • GC61047 structure
    GC61047Methotrexate disodium
    CAS: 7413-34-5
    纯度: >98.00%

    Methotrexate sodium, an inhibitor of tetrahydrofolate dehydrogenase, is an antineoplastic antimetabolite with immunosuppressant properties.

  • GC61058 structure
    GC61058Metoprine
    CAS: 7761-45-7
    纯度: >99.00%

    Metoprine(BW197U)是一种有效的组胺N-甲基转移酶(HMT)抑制剂。Metoprine是一种二氨基嘧啶衍生物，可以透过血脑屏障，并通过抑制HMT增加脑组胺水平。Metoprine是一种抗叶酸(antifolate)和抗肿瘤药。

  • GC62968 structure
    GC62968Fanotaprim
    CAS: 2120282-75-7

    Fanotaprim 是一种二氢叶酸还原酶 (DHFR) 抑制剂，对于 tgDHFR (Toxoplasma gondii DHFR) 和 hDHFR (human DHFR)，IC50 分别为 1.57 和 308 nM。Fanotaprim 具有研究弓形虫病的潜力。

  • GC63612 structure
    GC63612Tetroxoprim
    CAS: 53808-87-0

    Tetroxoprim 是抗菌 DHFR 的抑制剂。

  • GC65617 structure
    GC65617DHFR-IN-3
    CAS: 137553-43-6
    纯度: >99.00%

    DHFR-IN-3 是一种二氢叶酸还原酶 (DHFR) 抑制剂， 作用于大鼠肝脏和 P. carinii DHFR 的 IC50 值分别是 19 μM 和 12 μM。

  • GC66387 structure
    GC66387Lometrexol disodium
    CAS: 120408-07-3
    纯度: >98.00%

    Lometrexol (DDATHF) disodium 是一种抗嘌呤类抗叶酸 (antifolate) 药，可抑制甘氨酰胺核糖核苷酸甲酰基转移酶 (GARFT) 的活性，但不会引起可检测水平的 DNA 链断裂。Lometrexol disodium 可以进一步抑制嘌呤从头合成，导致异常的细胞增殖，凋亡 (apoptosis) 和细胞周期停滞。Lometrexol disodium 具有抗癌活性。Lometrexol disodium 还是一种有效的人丝氨酸羟甲基转移酶 1/2 (hSHMT1/2) 抑制剂。

  • GC66422 structure
    GC66422Trimethoprim-d9
    CAS: 1189460-62-5

    Trimethoprim-d9 是 Trimethoprim 的氘代物。Trimethoprim 是一种抑菌抗生素，也是一种具有口服活性的二氢叶酸还原酶 (dihydrofolate reductase) 抑制剂。Trimethoprim 对多种革兰氏阳性和革兰氏阴性需氧细菌 (Gram-positive 和 Gram-negative aerobic bacteria) 具有活性。Trimethoprim 可用于尿路感染，志贺氏菌病和肺孢子菌肺炎的研究。

  • GC69466 structure
    GC69466Mirvetuximab
    CAS: 1453084-36-0
    纯度: >99.00%

    Mirvetuximab (M9346A) 是一种 anti-FOLR1 (folate receptor 1) 单克隆抗体。Mirvetuximab 是新型叶酸受体α (FRα) 靶向 ADC (Mirvetuximab soravtansine) 的抗体分子。Mirvetuximab soravtansine 可用于卵巢癌和其他 FRα 阳性的癌症研究。

  • GC73018 structure
    GC73018Mirvetuximab soravtansine (solution)
    CAS: 1453084-37-1
    纯度: >99.00%

    Mirvetuximab soravtansine (solution)是一种抗叶酸受体α（FRα）ADC，由细胞毒性美登素类DM4组成，与人源化单克隆抗体M9346A共价连接。