Bioactivity | 2,4-Diamino-6-hydroxypyrimidine is a specific GTP cyclohydrolase I inhibitor (the rate-limiting enzyme in de novo pterin synthesis). 2,4-Diamino-6-hydroxypyrimidine blocks Tetrahydrobiopterin (BH4) synthesis and suppresses NO production[1][2]. |
Target | GTP cyclohydrolase I |
Invitro | 2,4-Diamino-6-hydroxypyrimidine (DAHP) exhibits a dose-dependent reduction in NO production in both chicken peritoneal macrophages (PECs) and the avian MC29 virus-transformed macrophage cell line, HD11[1].2,4-Diamino-6-hydroxypyrimidine (DAHP; 5 mM; 24 hours) treatment significantly reduces both BH4 and VCAM-1 levels during the time course in HUVEC cells. 2,4-Diamino-6-hydroxypyrimidine reduces VCAM-1 and GTPCH protein synthesis at least partially via suppressing the NF-κB level in the nucleus of HUVEC[2].2,4-Diamino-6-hydroxypyrimidine (DAHP) is first identified as an inhibitor of the biopterin-dependent growth of the protozoan Crithidia fasciculate[2]. |
In Vivo | When 2,4-Diamino-6-hydroxypyrimidine (DAHP) is administered for 4 days at the dose of 3 g/kg/day in mice, serotonin decreased in the duodenum and colon to approximately 46% and 40% of the control levels, respectively. 2,4-Diamino-6-hydroxypyrimidine causes a rapid decrease (T1/2 of less than 12 hr) in the BH4 levels in all tissues examined, except in the brain. The BH4 level returned to within the normal range less than 24 hr after cessation of the administration of 2,4-Diamino-6-hydroxypyrimidine[3]. |
Name | 2,4-Diamino-6-hydroxypyrimidine |
CAS | 56-06-4 |
Formula | C4H6N4O |
Molar Mass | 126.12 |
Appearance | Solid |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
Reference | [1]. Sung YJ, et al. 2,4-Diamino-6-hydroxypyrimidine, an inhibitor of GTP cyclohydrolase I, suppresses nitric oxide production by chicken macrophages. Int J Immunopharmacol. 1994 Feb;16(2):101-8. [2]. Kazuhisa Ikemoto, et al. 2,4-Diamino-6-hydroxypyrimidine (DAHP) suppresses cytokine-induced VCAM-1 expression on the cell surface of human umbilical vein endothelial cells in a BH(4)-independent manner. Biochim Biophys Acta. Jul-Aug 2008;1780(7-8):960-5. [3]. T Kobayashi, et al. Gastrointestinal serotonin: depletion due to tetrahydrobiopterin deficiency induced by 2,4-diamino-6-hydroxypyrimidine administration. J Pharmacol Exp Ther. 1991 Feb;256(2):773-9. |