AR-12463

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

Hodoodo CAT#: H524246

CAS#: 100557-04-8

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.


Chemical Structure

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AR-12463
CAS# 100557-04-8

Theoretical Analysis

Hodoodo Cat#: H524246
Name: AR-12463
CAS#: 100557-04-8
Chemical Formula: C17H28N6O
Exact Mass: 332.23
Molecular Weight: 332.440
Elemental Analysis: C, 61.42; H, 8.49; N, 25.28; O, 4.81

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @hodoodo.com or click below button.
Note: Price will be listed if it is available in the future.

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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:

Biological target:
In vitro activity:
In vivo activity:

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
Formulation protocol:
In vitro protocol:
In vivo protocol:

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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.