Barnidipine (hydrochloride) (Synonyms: YM 09730-5) |
| Catalog No.GC13289 |
Barnidipine(염산염)(Mepirodipine hydrochloride)은 [3H] initrendipine 결합 부위(Ki\u003d0.21 nmol/l)에 대해 높은 친화성을 갖는 L형 칼슘 길항제(CaA)이며 CaA 수용체에 대해 선택적인 작용을 합니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 104757-53-1
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Barnidipine is a calcium-channel blocker.
A calcium channel, an ion channel which displays selective permeability to calcium ions, is sometimes synonymous as voltage-dependent calcium channel, although there are also ligand-gated calcium channels.
In vitro: The effects of barnidipine on L-type Ca(2+) current (I(Ca(L))) were investigated in rat ventricular cardiomyocytes. It was found that barnidipine reduced I(Ca(L)) in a concentration and voltage dependent manne. Barnidipine induced a leftward shift of the steady-state inactivation curve of I(Ca(L)) [1].
In vivo: A previous study was conducted to investigate the influence of barnidipine treatment on early stage hypertension by determining the mesenteric and renal arteries as well as the kidney in L-NAME-induced hypertensive rats. Barnidipine was applied to rats after 2 weeks of L-NAME administration, and continued for the next 3 weeks concomitantly with L-NAME. Histopathological studies verified structural alterations in the arteries and the kidney. Moreover, a decrease in endothelial nitric oxide synthase expression was observed both in the arteries and kidney of hypertensive rats with barnidipine treatment [2].
Clinical trial: In patients with hypertension and type 2 diabetes mellitus, it was found that barnidipine treatment led to a significant reduction in blood pressure. Data recorded with ABPM also showed a similar trend. Barnidipine + losartan could reduce the levels of Hs-CRP, TNF-α, sVCAM-1, sICAM-1, and isoprostanes [3].
References:
[1] Wegener JW, Meyrer H, Rupp J, Nawrath H. Barnidipine block of L-type Ca(2+) channel currents in rat ventricular cardiomyocytes. Br J Pharmacol. 2000 Aug;130(8):2015-23.
[2] Alp Yildirim FI, Eker Kizilay D, Ergin B, Balci Ekmeki, Topal G, Kucur M, Demirci Tansel C, Uyde Doan BS. Barnidipine ameliorates the vascular and renal injury in L-NAME-induced hypertensive rats. Eur J Pharmacol. 2015 Oct 5;764:433-42.
[3] Derosa G, Mugellini A, Pesce RM, D'Angelo A, Maffioli P. Barnidipine compared to lercanidipine in addition to losartan on endothelial damage and oxidative stress parameters in patients with hypertension and type 2 diabetes mellitus. BMC Cardiovasc Disord. 2016 Apr 12;16:66.
| Cas No. | 104757-53-1 | SDF | |
| Synonyms | YM 09730-5 | ||
| Chemical Name | (4S)-3,5-pyridinedicarboxylic acid, 3-methyl 5-[(3S)-1-(phenylmethyl)-3-pyrrolidinyl] ester, monohydrochloride | ||
| Canonical SMILES | CC1=C(C(O[C@@H]2CN(CC3=CC=CC=C3)CC2)=O)[C@H](C(C(OC)=O)=C(C)N1)C4=CC([N+]([O-])=O)=CC=C4.Cl | ||
| Formula | C27H29N3O6 • HCl | M.Wt | 528 |
| Solubility | ≥ 16.3mg/mL in DMSO with gentle warming | Storage | 4°C, away from moisture and light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.8939 mL | 9.4697 mL | 18.9394 mL |
| 5 mM | 0.3788 mL | 1.8939 mL | 3.7879 mL |
| 10 mM | 0.1894 mL | 0.947 mL | 1.8939 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 24 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *