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Efonidipine (hydrochloride) [CAS 111011-53-1]

Efonidipine (hydrochloride) [CAS 111011-53-1]

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QM-0000379

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  • Description

    Efonidipine Hcl (NZ-105) is a dual T-type and L-type calcium channel blocker (CCB) . IC50 value: Target: calcium channel blocker in vitro: Efonidipine and nifedipine, but not other examined CCBs, also increased the N (6), 2'-O-dibutyryladenosine 3',5'-cyclic monophosphate (dbcAMP) -induced StAR mRNA, which reflects the action of adrenocorticotropic hormone, and efonidipine and R (-) -efonidipine enhanced the dbcAMP-induced DHEA-S production in NCI-H295R adrenocortical carcinoma cells [1]. I (Ca (T) ) was blocked mainly by a tonic manner by nifedipine, by a use-dependent manner by mibefradil, and by a combination of both manners by efonidipine. IC50s of these Ca2+ channel antagonists to I (Ca (T) ) and L-type Ca2+ channel current (I (Ca (L) ) ) were 1.2 micromol/l and 0.14 nmol/l for nifedipine; 0.87 and 1.4 micromol/l for mibefradil, and 0.35 micromol/l and 1.8 nmol/l for efonidipine, respectively [4]. in vivo: Twenty hypertensive patients on chronic hemodialysis were given efonidipine 20-60 mg twice daily and amlodipine 2.5-7.5 mg once daily for 12 weeks each in a random crossover manner. The average blood pressure was comparable between the efonidipine and amlodipine periods (151 + or - 15/77 + or - 8 versus 153 + or - 15/76 + or - 8 mmHg) . The pulse rate did not change significantly during the administration periods [2]. In the UM-X7.1 group, EFO treatment significantly attenuated the decrease of LVEF without affecting blood pressure compared with the vehicle group. EFO treatment decreased heart rate (by approximately 10%) in both groups [3].

  • CAS Number

    [111011-53-1]

  • Molecular Formula

    C34H39ClN3O7P

  • Molecular Weight

    668.12

  • Smiles

    CC1=C(P2(OCC(C)(C)CO2)=O)C(C3=CC([N+]([O-])=O)=CC=C3)C(C(OCCN(C4=CC=CC=C4)CC5=CC=CC=C5)=O)=C(C)N1.[H]Cl

  • Target

    Calcium Channel

  • Isoform

    L-type calcium channel; T-type calcium channel

  • Solubility

    DMSO : 8.5 mg/mL (ultrasonic; warming)

  • Shipping Conditions

    Room temperature

  • Hazard Statement

    H302-H315-H319-H335

  • Precautions

    P261-P264-P270-P271-P280-P302+P352-P304+P340-P305+P351+P338-P330-P362+P364-P403+P233-P405-P501
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Efonidipine (hydrochloride) [CAS 111011-53-1]

Efonidipine (hydrochloride) is a premium-grade research compound supplied by Quantimol for laboratory and scientific applications.