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MedKoo Cat#: 574535 | Name: Rilmenidine phosphate

Description:

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

Rilmenidine phosphate is an Imidazoline I1-receptor agonist used in the treatment of hypertension.

Chemical Structure

Rilmenidine phosphate
Rilmenidine phosphate
CAS#85409-38-7

Theoretical Analysis

MedKoo Cat#: 574535

Name: Rilmenidine phosphate

CAS#: 85409-38-7

Chemical Formula: C10H19N2O5P

Exact Mass: 0.0000

Molecular Weight: 278.24

Elemental Analysis: C, 43.17; H, 6.88; N, 10.07; O, 28.75; P, 11.13

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
Rilmenidine phosphate, S 3341-3
IUPAC/Chemical Name
N-(Dicyclopropylmethyl)-4,5-dihydro-2-oxazolamine Phosphate
InChi Key
ZJCOWRFWZOAVFY-UHFFFAOYSA-N
InChi Code
InChI=1S/C10H16N2O.H3O4P/c1-2-7(1)9(8-3-4-8)12-10-11-5-6-13-10;1-5(2,3)4/h7-9H,1-6H2,(H,11,12);(H3,1,2,3,4)
SMILES Code
O=P(O)(O)O.C1(NC(C2CC2)C3CC3)=NCCO1
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
Shelf Life
>3 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 278.24 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: Perera ND, Sheean RK, Lau CL, Shin YS, Beart PM, Horne MK, Turner BJ. Rilmenidine promotes MTOR-independent autophagy in the mutant SOD1 mouse model of amyotrophic lateral sclerosis without slowing disease progression. Autophagy. 2018;14(3):534-551. doi: 10.1080/15548627.2017.1385674. Epub 2017 Dec 17. PubMed PMID: 28980850; PubMed Central PMCID: PMC5915012. 2: Rubinsztein DC, Bento CF, Deretic V. Therapeutic targeting of autophagy in neurodegenerative and infectious diseases. J Exp Med. 2015 Jun 29;212(7):979-90. doi: 10.1084/jem.20150956. Epub 2015 Jun 22. Review. PubMed PMID: 26101267; PubMed Central PMCID: PMC4493419. 3: Lim K, Jackson KL, Burke SL, Head GA. The Effects of Rilmenidine and Perindopril on Arousal Blood Pressure during 24 Hour Recordings in SHR. PLoS One. 2016 Dec 21;11(12):e0168425. doi: 10.1371/journal.pone.0168425. eCollection 2016. PubMed PMID: 28002478; PubMed Central PMCID: PMC5176293. 4: INN Common stem: -onidine. Prescrire Int. 2017 Apr;26(181):92. PubMed PMID: 30730657. 5: Mercer LD, Higgins GC, Lau CL, Lawrence AJ, Beart PM. MDMA-induced neurotoxicity of serotonin neurons involves autophagy and rilmenidine is protective against its pathobiology. Neurochem Int. 2017 May;105:80-90. doi: 10.1016/j.neuint.2017.01.010. Epub 2017 Jan 23. PubMed PMID: 28122248. 6: Kawada T, Hayama Y, Nishikawa T, Yamamoto H, Tanaka K, Sugimachi M. Even weak vasoconstriction from rilmenidine can be unmasked in vivo by opening the baroreflex feedback loop. Life Sci. 2019 Feb 15;219:144-151. doi: 10.1016/j.lfs.2019.01.009. Epub 2019 Jan 7. PubMed PMID: 30630007. 7: Underwood BR, Green-Thompson ZW, Pugh PJ, Lazic SE, Mason SL, Griffin J, Jones PS, Rowe JB, Rubinsztein DC, Barker RA. An open-label study to assess the feasibility and tolerability of rilmenidine for the treatment of Huntington's disease. J Neurol. 2017 Dec;264(12):2457-2463. doi: 10.1007/s00415-017-8647-0. Epub 2017 Oct 26. PubMed PMID: 29075837; PubMed Central PMCID: PMC5688221. 8: Montastruc JL, Macquin-Mavier I, Tran MA, Damase-Michel C, Koenig-Berard E, Valet P. Recent advances in the pharmacology of rilmenidine. Am J Med. 1989 Sep 18;87(3C):14S-17S. Review. PubMed PMID: 2571291. 9: Nascimento AR, Machado MV, Gomes F, Vieira AB, Gonçalves-de-Albuquerque CF, Lessa MA, Bousquet P, Tibiriçá E. Central Sympathetic Modulation Reverses Microvascular Alterations in a Rat Model of High-Fat Diet-Induced Metabolic Syndrome. Microcirculation. 2016 May;23(4):320-9. doi: 10.1111/micc.12280. PubMed PMID: 27086551. 10: Vucicevic J, Srdic-Rajic T, Pieroni M, Laurila JM, Perovic V, Tassini S, Azzali E, Costantino G, Glisic S, Agbaba D, Scheinin M, Nikolic K, Radi M, Veljkovic N. A combined ligand- and structure-based approach for the identification of rilmenidine-derived compounds which synergize the antitumor effects of doxorubicin. Bioorg Med Chem. 2016 Jul 15;24(14):3174-83. doi: 10.1016/j.bmc.2016.05.043. Epub 2016 May 24. PubMed PMID: 27265687. 11: Lewis SJ, Jarrott B, Doyle AE. Rapid eye movement (REM)-sleep during and after continuous infusion of the oxazoline derivate S3341: a comparison with clonidine. J Hypertens Suppl. 1984 Dec;2(3):S45-7. PubMed PMID: 6599698. 12: Srdic-Rajic T, Nikolic K, Cavic M, Djokic I, Gemovic B, Perovic V, Veljkovic N. Rilmenidine suppresses proliferation and promotes apoptosis via the mitochondrial pathway in human leukemic K562 cells. Eur J Pharm Sci. 2016 Jan 1;81:172-80. doi: 10.1016/j.ejps.2015.10.017. Epub 2015 Oct 24. PubMed PMID: 26598394. 13: Nikolic K, Veljkovic N, Gemovic B, Srdic-Rajic T, Agbaba D. Imidazoline-1 receptor ligands as apoptotic agents: pharmacophore modeling and virtual docking study. Comb Chem High Throughput Screen. 2013 May;16(4):298-319. PubMed PMID: 23360165. 14: Weerasuriya K, Shaw E, Turner P. Preliminary clinical pharmacological studies of S3341, a new hypotensive agent, and comparison with clonidine in normal males. Eur J Clin Pharmacol. 1984;27(3):281-6. PubMed PMID: 6150856. 15: Mahieux F. Rilmenidine and vigilance. Review of clinical studies. Am J Med. 1989 Sep 18;87(3C):67S-72S. Review. PubMed PMID: 2571296. 16: Groenewoud G, Potgieter L, Meyer B. Bioequivalence evaluation of rilmenidine in healthy volunteers. Arzneimittelforschung. 2009;59(5):233-7. doi: 10.1055/s-0031-1296390. PubMed PMID: 19537523. 17: Genissel P, Bromet N. Pharmacokinetics of rilmenidine. Am J Med. 1989 Sep 18;87(3C):18S-23S. PubMed PMID: 2782323. 18: Dresse A, Scuvée-Moreau J. Influence of the alpha-2 agonist oxaminozoline (S3341) on firing rate of central noradrenergic and serotonergic neurons in the rat. Comparison with clonidine. Arch Int Physiol Biochim. 1986 Jun;94(2):99-106. PubMed PMID: 2430542. 19: Lewis SJ, Jarrott B, Doyle AE. Rapid eye movement sleep and the associated cardiovascular changes during and after continuous 10-day infusion of clonidine in normotensive rats: comparison with lofexidine and S3341. J Cardiovasc Pharmacol. 1987 Jun;9(6):711-8. PubMed PMID: 2442539. 20: Montastruc JL, Macquin-Mavier I, Damase-Michel C, Dard B, Tran MA, Valet P. [Current data on the pharmacology of rilmenidine]. Arch Mal Coeur Vaiss. 1989 Dec;82 Spec No 5:25-9. Review. French. PubMed PMID: 2517006.

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