D-AMETHOPTERIN HYDRATE, 95
D-AMETHOPTERIN HYDRATE, 95 Basic information
- Product Name:
- D-AMETHOPTERIN HYDRATE, 95
- Synonyms:
-
- D-AMETHOPTERIN HYDRATE, 95
- L-Glutamic acid, N-4-(2,4-diamino-6-pteridinyl)methylmethylaminobenzoyl-, monohydrate
- Methotrexate monohydrate
- (S)-2-(4-(((2,4-Diaminopteridin-6-yl)methyl)(methyl)amino)benzamido)pentanedioic acid hydrate
- Methotrexate hydrate, DHFR inhibitor
- CAS:
- 6745-93-3
- MF:
- C20H22N8O5
- MW:
- 0
- EINECS:
- 257-482-2
- Mol File:
- 6745-93-3.mol
D-AMETHOPTERIN HYDRATE, 95 Chemical Properties
- Melting point:
- 195 °C (dec.)(lit.)
Safety Information
- Hazard Codes
- T
- Risk Statements
- 46-60-61-25-36/37/38
- Safety Statements
- 53-22-26-36/37/39-45
- RIDADR
- UN 1544 6.1/PG 3
- RTECS
- MA1224000
- Toxicity
- LD50 i.v. in rats: 14 mg/kg (Scherf)
D-AMETHOPTERIN HYDRATE, 95 Usage And Synthesis
Uses
Methotrexate (Amethopterin) monohydrate, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate monohydrate, also an immunosuppressant and antineoplastic agent, is used for the research of rheumatoid arthritis and a number of different cancers (such as acute lymphoblastic leukemia)[1][2][3].
Definition
ChEBI: Methotrexate hydrate is a member of folic acids.
in vivo
Methotrexate (Amethopterin) monohydrate reduces thymus and spleen indices of mice. Methotrexate monohydrate markedly decreases white blood cells, thymic and splenic lymphocytes at dose ≥5 mg/kg. However, there is a significant difference between the treatment plus control group and the model group (p<0.01). The combination of grape seed proanthocyanidins and Siberian ginseng eleutherosides obviously diminishes the effects of Methotrexate monohydrate exposure on indices of thymus and spleens in mice[2].
Methotrexate (MTX) monohydrate (2 mg/kg; i.p.; once in a week for 5 weeks) is effective in Freund's complete adjuvant-induced arthritis. The combination of Methotrexate monohydrate (1 mg/kg; i.p.; once in a week for 5 weeks) and Curcumin (30 mg/kg and 100 mg/kg, thrice a week for 5 weeks; i.p.) shows a significant anti-arthritic action and protection from hematological toxicity[4].
IC 50
Traditional Cytotoxic Agents
References
[1] Tian H, et al. Understanding the mechanisms of action of methotrexate: implications for the treatment of rheumatoid arthritis. Bull NYU Hosp Jt Dis. 2007;65(3):168-73. PMID:17922664
[2] Swierkot J, et al. Methotrexate in rheumatoid arthritis. Pharmacol Rep. 2006 Jul-Aug;58(4):473-92. PMID:16963793
[3] Ehab Tousson, et al. The Effect of L-carnitine on Amethopterin-induced Toxicity in Rat Large Intestine.
[4] Banji D, et al. Evaluation of the concomitant use of methotrexate and curcumin on Freund's complete adjuvant-induced arthritis and hematological indices in rats. Indian J Pharmacol. 2011;43(5):546-550. DOI:10.4103/0253-7613.84970
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