WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H524245
CAS#: 100557-06-0
Description: AR-12456 is a trapidil derivative. AR 12456 protects against serum hyperlipidemia in guinea pigs. AR 12456 has a strong antilipidemic action in guinea pigs fed a cholesterol-rich diet.
Hodoodo Cat#: H524245
Name: AR 12456
CAS#: 100557-06-0
Chemical Formula: C17H30N6O
Exact Mass: 334.25
Molecular Weight: 334.460
Elemental Analysis: C, 61.05; H, 9.04; N, 25.13; O, 4.78
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Synonym: AR 12456; AR-12456; AR12456
IUPAC/Chemical Name: 2-((5-(diethylamino)-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)(hexyl)amino)ethanol
InChi Key: NWCVGIMEZSWINX-UHFFFAOYSA-N
InChi Code: InChI=1S/C17H30N6O/c1-4-7-8-9-10-22(11-12-24)16-13-15(21(5-2)6-3)20-17-18-14-19-23(16)17/h13-14,24H,4-12H2,1-3H3
SMILES Code: c1c(nc2ncnn2c1N(CCCCCC)CCO)N(CC)CC
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
Biological target: | |
In vitro activity: | |
In vivo activity: |
The following data is based on the product molecular weight 334.46 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
Formulation protocol: | |
In vitro protocol: | |
In vivo protocol: |
1: Corsini A, Grignaffini P, Beitz J, Mest H, Bellosta S, Fumagalli R, Paoletti R. Effect of trapidil derivative AR 12456 on intracellular cholesterol homeostasis in human hepatoma cell line Hep G2. Cytotechnology. 1993 Jan;11(Suppl 1):S15-7. doi: 10.1007/BF00746043. PubMed PMID: 22358683.
2: Corsini A, Grignaffini P, Beitz J, Mest HJ, Bellosta S, Fumagalli R, Paoletti R. Effect of trapidil derivative AR 12456 on intracellular cholesterol homeostasis in human hepatoma cell line Hep G2. Cytotechnology. 1993;11 Suppl 1:S15-7. PubMed PMID: 7763747.
3: Beitz J, Corsini A, Bellosta S, Bernini F, Fumagalli R, Mest HJ, Paoletti R. Influence of trapidil and derivatives on cholesterol synthesis and esterification in cultured cells. Pharmacol Res. 1991 Oct;24(3):235-42. PubMed PMID: 1956868.
4: Beitz J, Riedel A, Beitz A, Giessler C, Kittel A, Mest HJ. The trapidil derivative AR 12456 protects against serum hyperlipidemia in guinea pigs. J Lipid Mediat. 1991 Mar-Apr;3(2):177-86. PubMed PMID: 1665714.
5: Corsini A, Beitz J, Granata A, Fumagalli R, Mest HJ, Paoletti R. Trapidil derivatives and low density lipoprotein metabolism by human skin fibroblasts and by human hepatoma cell line Hep G2. Pharmacol Res. 1989 Sep-Oct;21(5):521-31. PubMed PMID: 2594609.
6: Markwardt F, Nilius B. Effects of trapidil-derivatives on calcium channel currents in isolated ventricular cells from mice. Naunyn Schmiedebergs Arch Pharmacol. 1988 Apr;337(4):454-8. PubMed PMID: 2457174.
7: Heinroth-Hoffmann I, Hauser A, Taube C, Mest HJ. Effects of trapidil and trapidil derivatives on arachidonic acid and prostaglandin endoperoxide analogue U 46619-induced blood pressure changes in rats. Biomed Biochim Acta. 1988;47(10-11):S145-8. PubMed PMID: 3248102.
8: Beitz J, Corsini A, Granata A, Fumagalli R, Mest HJ, Paoletti R. Effect of derivatives of trapidil on the expression of LDL receptors. Biomed Biochim Acta. 1988;47(10-11):S153-6. PubMed PMID: 2854727.
9: Heinroth-Hoffmann I, Hauser A, Mest HJ. Inhibition of thromboxane A2 production by trapidil and trapidil derivatives in the arachidonic acid-injected rat. Prostaglandins Leukot Med. 1987 Dec;30(2-3):87-92. PubMed PMID: 2827194.
10: Block HU, Hoffmann-Heinroth I, Taube C, Niebisch M, Mest HJ. Inhibition of thromboxane B2 formation of blood platelets by trapidil and other s-triazolo(1,5-a)pyrimidine derivatives. Prostaglandins Leukot Med. 1987 Dec;30(2-3):77-86. PubMed PMID: 2827193.
11: Dienel A, Andreas K, Schmidt J. Influence of nootropic drugs on drinking behaviour in ethanol-preferring mice and ethanol-induced increase of seizure susceptibility. Biomed Biochim Acta. 1985;44(5):767-71. PubMed PMID: 4062922.
12: Hering S, Bodewei R, Schubert B, Krause EG, Wollenberger A. Trapidil and other 5-triazolo-(1, 5-alpha)-pyrimidine derivatives as calcium channel blockers in 108CC5 cells. Biomed Biochim Acta. 1985;44(5):K37-41. PubMed PMID: 2415119.