| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
|
||
| 100mg |
|
||
| 250mg | |||
| 500mg | |||
| Other Sizes |
| Targets |
α-1 adrenoceptor, 5-HT1A receptor [1]
|
|---|---|
| ln Vitro |
Urapidil is an agonist of the 5-HT1A receptor and an antagonist of the α1-adrenergic receptor. Vascular tone is unaffected by urapidil at concentrations up to 10-5 M. The α1-adrenergic agonist (phenylephrine)-induced concentration-dependent contraction of endothelial-free aortic rings is significantly inhibited by urapidil (10-5 M), and it also somewhat inhibits the contraction of endothelial cells. people possessing endothelial cells. Additionally, urapidil's inhibitory effect was more noticeable in rings devoid of endothelium than in rings that had endothelium. Both vascular tone and serotonin's concentration-dependent contraction are unaffected by urapidil (10–5 M) [1].
- Urapidil dose-dependently inhibited norepinephrine (NE)-induced contraction in isolated porcine coronary arteries, with a pEC50 of 6.8 ± 0.2 (detected by vascular tone measurement). At 10 μM, it inhibited contraction by ~80% compared with the NE-only group [1] - Urapidil partially inhibited 5-hydroxytryptamine (5-HT)-induced contraction in porcine coronary arteries, with a maximal inhibition rate of ~40% at 10 μM [1] - In isolated porcine pulmonary arteries, Urapidil dose-dependently antagonized NE-induced contraction (pEC50 = 6.6 ± 0.3) but had no significant effect on 5-HT-induced contraction even at 10 μM [1] - Urapidil effectively inhibited NE-induced contraction in isolated rat aortas (pEC50 = 6.9 ± 0.2) and showed no obvious effect on 5-HT-induced contraction up to 10 μM [1] - In isolated human pulmonary arteries, Urapidil dose-dependently blocked NE-induced contraction (pEC50 = 6.7 ± 0.3) but did not alter 5-HT-induced contraction at concentrations up to 10 μM [1] |
| Enzyme Assay |
- Vascular tone measurement assay: Arteries (porcine coronary, porcine pulmonary, rat aortic, human pulmonary) were isolated and cut into 2-3 mm ring segments. Segments were mounted in organ baths containing oxygenated Krebs-Henseleit solution (37°C, pH 7.4) and connected to force transducers to record isometric tension [1]
- After a 60-minute equilibration period, arteries were precontracted with NE (1 μM) or 5-HT (1 μM) to confirm contractile function. Then Urapidil (0.01-10 μM) was added cumulatively, and changes in vascular tension were recorded continuously. The concentration-response curves were constructed to calculate pEC50 values and maximal inhibition rates [1] - In antagonist specificity experiments, arteries were preincubated with Urapidil (10 μM) for 30 minutes before adding NE or 5-HT, to evaluate its selective effect on the two agonists [1] |
| References |
[1]. Bopp C, et al. The effect of urapidil, an alpha-1 adrenoceptor antagonist and a 5-HT1A agonist, on the vascular tone of the porcine coronary and pulmonary arteries, the rat aorta and the human pulmonary artery. Eur J Pharmacol. 2016 May 15;779:53-8
|
| Additional Infomation |
Urapidil belongs to the piperazine class of compounds. Urapidil has been investigated for the treatment of hypertension during preeclampsia. See also: Urapidil hydrochloride (note moved to). - Urapidil is a dual-action drug with α-1 adrenergic receptor antagonist and 5-HT1A receptor agonist activities [1] - The vascular effects of urapidil are species- and vascular-specific: it effectively inhibits norepinephrine (NE)-induced (α-1 adrenergic receptor-mediated) contractions in all tested arteries, but its inhibition of 5-HT-induced contractions has only been observed in porcine coronary arteries [1] - This study aimed to evaluate the modulatory effects of urapidil on vascular tone in different species and vascular beds to gain a deeper understanding of its potential clinical applications in vascular-related diseases. [1]
|
| Molecular Formula |
C20H29N5O3
|
|---|---|
| Molecular Weight |
387.4760
|
| Exact Mass |
387.227
|
| CAS # |
34661-75-1
|
| Related CAS # |
Urapidil hydrochloride;64887-14-5;Urapidil-d3;1398066-08-4;Urapidil-d4;1795122-12-1
|
| PubChem CID |
5639
|
| Appearance |
White to off-white solid powder
|
| Density |
1.3±0.1 g/cm3
|
| Boiling Point |
549.0±60.0 °C at 760 mmHg
|
| Melting Point |
159 °C
|
| Flash Point |
285.8±32.9 °C
|
| Vapour Pressure |
0.0±1.5 mmHg at 25°C
|
| Index of Refraction |
1.622
|
| LogP |
2.28
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
28
|
| Complexity |
588
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
O(C([H])([H])[H])C1=C([H])C([H])=C([H])C([H])=C1N1C([H])([H])C([H])([H])N(C([H])([H])C([H])([H])C([H])([H])N([H])C2=C([H])C(N(C([H])([H])[H])C(N2C([H])([H])[H])=O)=O)C([H])([H])C1([H])[H]
|
| InChi Key |
ICMGLRUYEQNHPF-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C20H29N5O3/c1-22-18(15-19(26)23(2)20(22)27)21-9-6-10-24-11-13-25(14-12-24)16-7-4-5-8-17(16)28-3/h4-5,7-8,15,21H,6,9-14H2,1-3H3
|
| Chemical Name |
6-[3-[4-(2-methoxyphenyl)piperazin-1-yl]propylamino]-1,3-dimethylpyrimidine-2,4-dione
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~25 mg/mL (~64.52 mM)
H2O : ~0.1 mg/mL (~0.26 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.45 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 25.0 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: ≥ 2.5 mg/mL (6.45 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 25.0 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.45 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5808 mL | 12.9039 mL | 25.8078 mL | |
| 5 mM | 0.5162 mL | 2.5808 mL | 5.1616 mL | |
| 10 mM | 0.2581 mL | 1.2904 mL | 2.5808 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
