| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
Barnidipine HCl targets L-type voltage-gated calcium channels, specifically inhibiting calcium ion influx into myocardial and smooth muscle cells. This inhibition leads to relaxation of vascular smooth muscle, reduction in total peripheral resistance, and a decrease in blood pressure. It is a calcium channel blocker belonging to the dihydropyridine (DHP) group.
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|---|---|
| ln Vitro |
In vitro, barnidipine HCl acts as an L-type calcium antagonist with high affinity for [3H]nitrendipine binding sites (Ki = 0.21 nmol/L). It inhibits potassium-induced tonic contraction in pig coronary arteries with an IC50 of 0.35 nM. Its calcium channel blocking activity is measured in isolated tissue preparations.
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| ln Vivo |
In vivo, barnidipine HCl is used to treat hypertension. It reduces blood pressure by decreasing peripheral vascular resistance. It is a long-acting calcium channel blocker with once-daily dosing.
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| Enzyme Assay |
The in vitro receptor binding assay for barnidipine HCl involves measuring its affinity for L-type calcium channels. This is typically done using a radioligand binding assay with [3H]nitrendipine and membrane preparations from tissues rich in calcium channels. The Ki is determined.
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| Cell Assay |
In vitro cellular assays for barnidipine HCl are performed on vascular smooth muscle cells or cardiac myocytes. The functional effect is measured by its ability to inhibit calcium-induced contraction or to reduce the contractility of cardiac myocytes. The IC50 for these effects is determined.
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| Animal Protocol |
In vivo animal experiments for barnidipine HCl are conducted in hypertensive rat models. Blood pressure is measured before and after oral administration of the drug. The reduction in systolic and diastolic blood pressure is recorded over time to establish the dose-response relationship and duration of action.
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| ADME/Pharmacokinetics |
Barnidipine HCl has well-characterized pharmacokinetic properties. It is a long-acting calcium channel blocker. It is absorbed after oral administration and has a prolonged duration of action. It is metabolized in the liver and excreted in urine.
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| Toxicity/Toxicokinetics |
Barnidipine HCl is generally well-tolerated. Common side effects include headache, flushing, dizziness, and peripheral edema, which are related to its vasodilatory action. It is contraindicated in patients with severe hypotension or cardiogenic shock.
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| References | |
| Additional Infomation |
Barnidipine hydrochloride is a dihydropyridine compound.
Barnidipine HCl is the hydrochloride salt of barnidipine, used for the treatment of hypertension. It is a dihydropyridine calcium channel blocker. It is an API (Active Pharmaceutical Ingredient). |
| Molecular Formula |
C27H30CLN3O6
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|---|---|
| Molecular Weight |
528.0
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| Exact Mass |
527.182
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| Elemental Analysis |
C, 61.42; H, 5.73; Cl, 6.71; N, 7.96; O, 18.18
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| CAS # |
104757-53-1
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| Related CAS # |
Barnidipine;104713-75-9;Barnidipine-d5 hydrochloride
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| PubChem CID |
443868
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| Appearance |
Light yellow to yellow solid powder
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| Boiling Point |
614.5ºC at 760 mmHg
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| Melting Point |
223-226°C
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| Flash Point |
325.4ºC
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| Vapour Pressure |
4.94E-15mmHg at 25°C
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| LogP |
5.412
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
37
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| Complexity |
917
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| Defined Atom Stereocenter Count |
2
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| SMILES |
O=C(C1=C(C)NC(C)=C(C(OC)=O)C1C2=CC=CC([N+]([O-])=O)=C2)O[C@@H]3CN(CC4=CC=CC=C4)CC3.[H]Cl
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| InChi Key |
XEMPUKIZUCIZEY-YSCHMLPRSA-N
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| InChi Code |
InChI=1S/C27H29N3O6.ClH/c1-17-23(26(31)35-3)25(20-10-7-11-21(14-20)30(33)34)24(18(2)28-17)27(32)36-22-12-13-29(16-22)15-19-8-5-4-6-9-19/h4-11,14,22,25,28H,12-13,15-16H2,1-3H31H/t22-,25-/m0./s1
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| Chemical Name |
3-((S)-1-benzylpyrrolidin-3-yl) 5-methyl (S)-2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate hydrochloride
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| Synonyms |
Mepirodipine HClY198561 YM 09730 YM730Y-198561 YM-09730 YM-730Y 198561 YM09730-5 YM09730 YM 730 Barnidipine Hydrochloride Barnidipine HCl
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~473.48 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.94 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.94 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | 0.9470 mL | 1.8939 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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