IC50: 76-112 μM for GTP cyclohydrolase I 6,7-Dimethyltetrahydropterin is a GTP cyclohydrolase I inhibitor. GTP cyclohydrolase I catalyzes the formation of D-erythro-7,8-dihydroneopterin (dihydroneopterin) triphosphate and formate from GTP. Dihydroneopterin triphosphate has been identified as a critical intermediate in the biosynthesis of folic acid, pteridines in insects and amphibians, and tetrahydrobiopterin. Tetrahydrobiopterin is the obligatory cofactor for tyrosine and tryptophan hydroxylase, which are rate-limiting enzymes for biogenic amine synthesis. Tetrahydrobiopterin is the cofactor for phenylalanine hydroxylase as well, which converts Lphenylalanine to L-tyrosine. In vitro: Previous study identified 6,7-dimethyltetrahydropterin as a noncompetitive inhibitor of GTP cyclohydrolase. However, no substrate inhibition of the enzyme was detected 1mM GTP, which is about 8-fold the Km value of the enzyme . Another study found that phenylalanine hydroxylase could be inhibited by 6,7-dimethyltetrahydropterin, its cofactor. The rate of inactivation, which was irreversible, increased with the concentration of 6,7-dimethyltetrahydropterin. Moreover, 6,7-dimethyltetrahydropterin was found to be unstable when the solution was exposed to air but was stabilized by dithiothreitol the aerobic oxidation of which was significantly accelerated by 6,7-dimethyltetrahydropterin . In vivo: Up to now, there is no animal in vivo data reported. Clinical trial: So far, no clinical study has been conducted.

Product information

CAS Number: 167423-51-0

Molecular Weight: 231.68

Formula: C8H14ClN5O

Chemical Name: (6S,7R)-2-amino-6,7-dimethyl-1,4,5,6,7,8-hexahydropteridin-4-one

Smiles: Cl.C[C@H]1NC2NC(N)=NC(=O)C=2N[C@H]1C

InChiKey: GIHYTRGUZVYCQX-RFKZQXLXSA-N

InChi: InChI=1S/C8H13N5O.ClH/c1-3-4(2)11-6-5(10-3)7(14)13-8(9)12-6;/h3-4,10H,1-2H3,(H4,9,11,12,13,14);1H/t3-,4+;/m0./s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

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