Rilmenidine phosphate

Modify Date: 2024-01-02 09:23:33

Rilmenidine phosphate Structure
Rilmenidine phosphate structure
Common Name Rilmenidine phosphate
CAS Number 85409-38-7 Molecular Weight 278.242
Density N/A Boiling Point 609.1ºC at 760 mmHg
Molecular Formula C10H19N2O5P Melting Point N/A
MSDS N/A Flash Point 322.1ºC

 Use of Rilmenidine phosphate


Rilmenidine phosphate, an antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine phosphate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine phosphate induces autophagy. Rilmenidine phosphate is also an alpha 2-adrenoceptor agonist. 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[1][2][3].

 Names

Name N-(dicyclopropylmethyl)-4,5-dihydro-1,3-oxazol-2-amine,phosphoric acid
Synonym More Synonyms

 Rilmenidine phosphate Biological Activity

Description Rilmenidine phosphate, an antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine phosphate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine phosphate induces autophagy. Rilmenidine phosphate is also an alpha 2-adrenoceptor agonist. 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[1][2][3].
Related Catalog
In Vitro Rilmenidine phosphate (25-100 μM; 24 hours) inhibits K562 cell proliferation[2].Rilmenidine provides antihypertensive efficacy comparable with that of diuretics, beta-blockers, calcium channel blockers, and angiotensin-converting enzyme (ACE) inhibitors[3]. Cell Proliferation Assay[2] Cell Line: K562 cells Concentration: 25, 50, 100 μM Incubation Time: 24 hours Result: Dose-dependently inhibited K562 colony formation.
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[4]. Rilmenidine phosphate decreases levels of mutant huntingtin[4].
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.

[4]. 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.

 Chemical & Physical Properties

Boiling Point 609.1ºC at 760 mmHg
Molecular Formula C10H19N2O5P
Molecular Weight 278.242
Flash Point 322.1ºC
Exact Mass 278.103149
PSA 121.19000
LogP 0.04870
Storage condition -20℃
Water Solubility Freely soluble in water, slightly soluble in alcohol, practically insoluble in methylene chloride.

 Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
RP6744000
CAS REGISTRY NUMBER :
85409-38-7
LAST UPDATED :
199512
DATA ITEMS CITED :
2
MOLECULAR FORMULA :
C10-H16-N2-O.H3-O4-P
MOLECULAR WEIGHT :
278.28

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
295 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
CDREEA Cardiovascular Drug Reviews. (Raven Press, 1185 Avenue of the Americas, New York, NY 10036) V.6- 1988- Volume(issue)/page/year: 8,56,1990
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
375 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
CDREEA Cardiovascular Drug Reviews. (Raven Press, 1185 Avenue of the Americas, New York, NY 10036) V.6- 1988- Volume(issue)/page/year: 8,56,1990

 Safety Information

HS Code 2934999090

 Customs

HS Code 2934999090
Summary 2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

 Synonyms

2-Oxazolamine, N-(dicyclopropylmethyl)-4,5-dihydro-, phosphate (1:1)
N-(Dicyclopropylmethyl)-4,5-dihydro-1,3-oxazol-2-amine phosphate (1:1)
Rilmenidine phosphate
2-Oxazolamine, 4,5-dihydro-N-(dicyclopropylmethyl)-, phosphate (1:1)
S 3341-3 {Phosphate}
Rilmenidine dihydrogen phosphate
S 3341-3
EINECS 287-106-2
4,5-Dihydro-N-(dicyclopropylmethyl)-2-oxazolamine phosphate (1:1)
Hyperium
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