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MedKoo Cat#: 524246 | Name: AR-12463

Description:

WARNING: This product is for research use only, not for human or veterinary use.

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.

Chemical Structure

AR-12463
AR-12463
CAS#100557-04-8

Theoretical Analysis

MedKoo Cat#: 524246

Name: AR-12463

CAS#: 100557-04-8

Chemical Formula: C17H28N6O

Exact Mass: 332.2325

Molecular Weight: 332.44

Elemental Analysis: C, 61.42; H, 8.49; N, 25.28; O, 4.81

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
No Data
Synonym
AR 12463; AR-12463; AR12463;
IUPAC/Chemical Name
Ethanol, 2-(pentyl(5-(1-piperidinyl)(1,2,4)triazolo(1,5-a)pyrimidin-7-yl)amino)-
InChi Key
JANOITYENFDMAC-UHFFFAOYSA-N
InChi Code
InChI=1S/C17H28N6O/c1-2-3-5-10-22(11-12-24)16-13-15(21-8-6-4-7-9-21)20-17-18-14-19-23(16)17/h13-14,24H,2-12H2,1H3
SMILES Code
C1CCN(CC1)c1cc(N(CCO)CCCCC)n2ncnc2n1
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

Preparing Stock Solutions

The following data is based on the product molecular weight 332.44 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.

Recalculate based on batch purity %
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
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. 1: Langner A, Melzig MF, Kempa S, Krause A. [The use of lymphocyte cultures for the investigation of drug biotransformation]. Pharmazie. 1995 Feb;50(2):130-8. German. PubMed PMID: 7700967. 2: 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. 3: Fahr F, Neubert R, Hahn HJ, Pönicke K. [Improvement of the disolution behavior of problem drugs. 22. Preformulations of AR 12463 in absorption models]. Pharmazie. 1991 Sep;46(9):673. German. PubMed PMID: 1798735. 4: Langner A, Grahlmann D, Pfeifer S. [Comparison of the biotransformation of the trapidil (Rocornal) derivative AR 12463 in humans, rats, dogs, and rabbits]. Pharmazie. 1991 Mar;46(3):228-30. German. PubMed PMID: 1881950. 5: Beitz J, Krüger J, Beitz A, Pawelski K, Szymanski C, Rath FW, Mest HJ. Influence of the trapidil derivative AR 12463 on serum and tissue lipids and development of aortic lesions during experimental atherosclerosis in rabbits. Biomed Biochim Acta. 1991;50(1):101-7. PubMed PMID: 1859385. 6: Langner A, Nerlich C, Grahlmann D. [Biotransformation of the trapidil (Rocornal) derivative AR 12,463 by the isolated, perfused rat liver and rat hepatocyte suspension cultures]. Pharmazie. 1990 Jul;45(8):636. German. PubMed PMID: 2080221. 7: Pfeifer S, Langner A, Grahlmann D, Franke P, Gründemann E, Tenor E. [Biotransformation of the trapidil (rocornal) derivative AR 12463 in the rat]. Pharmazie. 1990 Jul;45(8):609-14. German. PubMed PMID: 2080211. 8: Bartels T, Beitz J, Hein W, Schumann M, Laag L, Beitz A, Szymanski C, Mest HJ. [Changes in the spongiosa density in the femoral head of rabbits in atherosclerosis]. Beitr Orthop Traumatol. 1990 Jun;37(6):291-7. German. PubMed PMID: 2386471. 9: 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. 10: 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. 11: 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. 12: Block HU, Dunemann A, Niebisch M, Mest HJ. Influence of the antianginal drug trapidil and its derivative AR 12463 on arachidonic acid liberation and thromboxane formation in thrombin-stimulated platelets. Biomed Biochim Acta. 1988;47(10-11):S141-4. PubMed PMID: 3248101. 13: Block HU, Gabbasov ZA, Pozin EY, Popov EG, Mest HJ. Inhibition of cytosolic Ca++ mobilization in human platelets by the antianginal drug trapidil and its derivative AR 12463. Biomed Biochim Acta. 1988;47(12):1093-7. PubMed PMID: 2855396. 14: 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. 15: Beitz A, Taube C, Beitz J, Goos H, Graff J, Nohring J, Lindenau KF, Mest HJ. Influence of drugs on the TXA2/PGI2 balance and on the atherogenic index in myocardial ischemia in dogs. Biomed Biochim Acta. 1988;47(10-11):S149-52. PubMed PMID: 2470353. 16: 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. 17: 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. 18: Taube C, Steinborn C, Mest HJ. [The effect of trapidil and the trapidil derivative AR 12463 on blood pressure and thromboxane formation in spontaneously hypertensive rats]. Pharmazie. 1987 May;42(5):334-6. German. PubMed PMID: 3671447. 19: Giessler C, Fahr A, Tertov VV, Kudryashov SA, Orekhov AN, Smirnov VN, Mest HJ. Trapidil derivatives as potential antiatherosclerotic drugs. Arzneimittelforschung. 1987 May;37(5):538-41. PubMed PMID: 3040019. 20: Taube C, Steinborn C, Mest HJ. Trapidil derivative AR 12463 lowers blood pressure and thromboxane formation in spontaneously hypertensive rats. Prog Clin Biol Res. 1987;242:107-11. PubMed PMID: 3671378.