Rilmenidine hemifumarate

Rilmenidine hemifumarate, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine hemifumarate is an alpha 2-adrenoceptor agonist. Rilmenidine hemifumarate induces autophagy. Rilmenidine hemifumarate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine hemifumarate modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells.

Product information

CAS Number: 207572-68-7

Molecular Weight: 476.57

Formula: C24H36N4O6

Chemical Name: (E)-but-2-enedioic acid;N-(dicyclopropylmethyl)-4, 5-dihydro-1, 3-oxazol-2-amine

Smiles: OC(=O)C=CC(O)=O.C1CC1C(NC1=NCCO1)C1CC1.C1CC1C(NC1=NCCO1)C1CC1

InChiKey: LZFATBMLSYHRTC-WXXKFALUSA-N

InChi: InChI=1S/2C10H16N2O.C4H4O4/c2*1-2-7(1)9(8-3-4-8)12-10-11-5-6-13-10;5-3(6)1-2-4(7)8/h2*7-9H,1-6H2,(H,11,12);1-2H,(H,5,6)(H,7,8)/b;;2-1+

Technical Data

Appearance: Solid Power

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

Solubility: H2O : 50 mg/mL (209.84 mM; Need ultrasonic) DMSO : 3 mg/mL (12.59 mM; Need ultrasonic)

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: ≥360 days 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

How to use

In Vitro:

Rilmenidine provides antihypertensive efficacy comparable with that of diuretics, beta-blockers, calcium channel blockers, and angiotensin-converting enzyme (ACE) inhibitors. Rilmenidine (25-100 μM; 24 hours) inhibits K562 cell proliferation.

In Vivo:

Rilmenidine-treated N171-82Q mice (i.p.; 4-times a week) displays significant improved forelimb grip strength and all limbs grip strength from 12 to 22 weeks of age. Rilmenidine decreases levels of mutant huntingtin.

References:

1. Reid JL. Rilmenidine: a clinical overview. Am J Hypertens. 2000;13(6 Pt 2):106S-111S.
2. Srdic-Rajic T, et al. Rilmenidine suppresses proliferation and promotes apoptosis via the mitochondrial pathway in human leukemic K562 cells. Eur J Pharm Sci. 2016;81:172-180.
3. Reid JL. Rilmenidine: a clinical overview. Am J Hypertens. 2000;13(6 Pt 2):106S-111S.

Products are for research use only. Not for human use.