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A7091358

Efonidipine , 10mMinDMSO , 111011-63-3

CAS NO.:111011-63-3

Empirical Formula: C34H38N3O7P

Molecular Weight: 631.66

MDL number:

Pack Size Price Stock Quantity
1ml RMB446.40 In Stock
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Update time: 2022-07-08

PRODUCT Properties

Melting point: 169-170℃
Boiling point: 746.9±60.0 °C(Predicted)
Density  1.30±0.1 g/cm3(Predicted)
storage temp.  Store at -20°C
solubility  DMF:30.0(Max Conc. mg/mL);47.49(Max Conc. mM)
Ethanol:40.0(Max Conc. mg/mL);63.32(Max Conc. mM)
form  A crystalline solid
pka 4.03±0.50(Predicted)
color  Off-white to light yellow

Description and Uses

Efonidipine(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].

Safety

Symbol(GHS) 
GHS07,GHS08
Signal word  Danger
Hazard statements  H315-H317-H319-H335-H360
Precautionary statements  P201-P261-P280-P305+P351+P338-P308+P313

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