Rilmenidine phosphate

Rilmenidine phosphate, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine phosphate is an alpha 2-adrenoceptor agonist. Rilmenidine phosphate induces autophagy. Rilmenidine phosphate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine phosphate 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: 85409-38-7

Molecular Weight: 278.24

Formula: C10H19N2O5P

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

Smiles: OP(O)(O)=O.C1COC(NC(C2CC2)C2CC2)=N1

InChiKey: ZJCOWRFWZOAVFY-UHFFFAOYSA-N

InChi: 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)

Technical Data

Appearance: Solid Power

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

Solubility: DMSO : 5 mg/mL (17.97 mM; ultrasonic and warming and heat to 80°C). H2O : 62.5 mg/mL (224.63 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: ≥12 months 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 phosphate (25-100 μM; 24 hours) inhibits K562 cell proliferation.

In Vivo:

Rilmenidine phosphate-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 phosphate 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. Rose C, et al. Rilmenidine attenuates toxicity of polyglutamine expansions in a mouse model of Huntington's disease. Hum Mol Genet. 2010;19(11):2144-2153.

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