Antifolates agents work by antagonizing (blocking) the actions of folic acid (vitamin B9).Antifolates have a cytotoxic effect on cells during the S-phase of the cell cycle, acting specifically during DNA and RNA synthesis. Antifolates that target folate metabolism have been crucial in the development of medications for the treatment of inflammatory, microbial, parasitic, and cancerous diseases.
Antifolates prevent cell division, DNA/RNA synthesis and repair, and protein synthesis because folate (folic acid) cofactors are necessary for the synthesis and metabolism of amino acids. Some drugs, including proguanil, pyrimethamine, and trimethoprim, specifically block the effects of folate on bacteria, protozoa, and fungi. Dihydrofolate reductase (DHFR), thymidylate synthase (TS), GARFTase, and AICARFTase are examples of prominent antifolate enzyme targets and the antifolates that specifically target these enzymes.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V80022 | Antitumor agent-99 | Antitumor agent-99 (compound 7) is an anticancer agent targeting FRα/β and PCFT. | |
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V77116 | Cycloguanil-d6 (Chlorguanide triazine-d6) | Cycloguanil-d66 is the deuterated compound standard of Cycloguanil. | |
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V52100 | Fanotaprim (VYR-006) | 2120282-75-7 | Fanotaprim is a dihydrofolate reductase (DHFR) inhibitor (antagonist) with IC50s of 1.57 and 308 nM for tgDHFR (Toxoplasma gondii DHFR) and hDHFR (human DHFR), respectively. |
|
V80562 | Levomefolate-13C5 calcium (5-Methyltetrahydrofolic Acid-13C5 (calcium salt)) | Levomefolate-13C5 (calcium) is a 13C (carbon 13)-labeled Levomefolate (calcium). | |
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V56538 | Methotrexate metabolite-d3 (DAMPA-d3) | 1794780-00-9 | Methotrexate metabolite-d3 is the deuterium labelled form of Methotrexate metabolite. |
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V52603 | Proguanil-d4 (proguanil-d4) | 1189805-15-9 | Proguanil-d4 is the deuterium labelled form of Proguanil. |
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V56376 | Proguanil-d4 hydrochloride | 1189671-34-8 | Proguanil-d4 ( HCl) is the deuterium labelled form of Proguanil HCl. |
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V52542 | Pyrimethamine-d3 (Pyrimethamine-d3) | 1189936-99-9 | Pyrimethamine-d3 is the deuterium labelled form of Pyrimethamine. |
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V35227 | Talotrexin (PT523) | 113857-87-7 | Talotrexin (PT523) is an analog of Aminopterin , a non-polyglutamic acid classical antifolate. |
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V35207 | Tetroxoprim (HE 781) | 53808-87-0 | Tetroxoprim is an inhibitor (blocker/antagonist) of the antibacterial DHFR. |
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V35013 | Trimethoprim lactate (Trimethoprim lactate) | 23256-42-0 | Trimethoprim lactate is an antibacterial antibiotic and an orally bioactive dihydrofolate reductase inhibitor. |
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V56323 | Trimethoprim-d3 (trimethoprim d3) | 1189923-38-3 | Trimethoprim-d3 is the deuterated form of Trimethoprim. |
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V52820 | Trimethoprim-d9 (Trimethoprim d9) | 1189460-62-5 | Trimethoprim-d9 is the deuterium labelled form of Trimethoprim. |
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V41272 | Pemetrexed | 137281-23-3 | Pemetrexed (LY-231514;LY231514;HSDB7316;HSDB-7316; trade name Alimta), a synthetic pyrimidine-based antifolate, is antimetabolite anticancer drug that inhibits TS, DHFR and GARFT with Ki of 1.3 nM, 7.2 nM and 65 nM, respectively. |
|
V21971 | Pemetrexed disodium heptahydrate | 357166-29-1 | Pemetrexed disodium heptahydrate (LY231514;HSDB7316; LY-231514;HSDB-7316; Alimta), the heptahydrated disodium salt of Pemetrexed and a pyrimidine-based antifolate, is an antifolate and antimetabolite anticancer medication. |
|
V2074 | Calcium Levofolinate ( CL307782) | 80433-71-2 | Calcium Levofolinate (also known as Calcium Folinate; Calcium levofolinate; CL307782), a calcium salt of andthe enantiomerically active form of folinic acid, is widely used asan adjuvantin cancer chemotherapy, e. |
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V50929 | Aditoprime (Aditoprim) | 56066-63-8 | Aditoprime (Aditoprim) is a novel and potent bacterial inhibitor of dihydrofolate reductase (DHFR) that prevents dihydrofolic acid from becoming tetrahydrofolic acid. |
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