| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| Other Sizes |
|
Purity: ≥98%
Regadenoson (CVT3146), a novel and potent A2A adenosine receptor agonist, is a coronary vasodilator that is commonly used in pharmacologic stress testing. It quickly causes hyperemia and keeps it going long enough for radionuclide myocardial perfusion imaging. The medication's selectivity makes it better than other stressors like adenosine, which are less selective and consequently have more adverse effects.
| Targets |
A2AR ( Ki = 290 nM )
|
|---|---|
| ln Vitro |
Regadenoson exhibits a comparatively low binding affinity (hA2A Ki=290 nM) for human A2A receptors, along with a selectivity that is over 30-fold greater than that of the A2B and A3AR subtypes, and 13-fold greater than that of the A1AR. While regadenoson acts as a full and strong agonist to cause coronary vasodilation, it acts as a weak partial agonist to cause cAMP accumulation in PC12 cells[1].
|
| ln Vivo |
Intravenous bolus injection of regadenoson results in a dose-dependent decrease in coronary vascular resistance and an increase in myocardial blood flow in a dog model. Regadenoson was demonstrated to cause a dose-dependent rise in heart rate and a drop in mean arterial pressure at higher dosages in a rat heart model. Additionally, serum norepinephrine and epinephrine increased by more than two times when regadenoson was administered. According to clinical data, regadenoson has an estimated clearance of 37.8 L/h and a volume of distribution of 11.5 L and 78.7 L (at steady-state). Its renal excretion accounts for 58% of its total elimination, and its terminal half-life ranges from 33 to 108 minutes[2].
|
| Animal Protocol |
Mongrel dogs (23-27 kg)
0.1, 0.175, 0.25, 0.5, 1.0, 2.5, 5 µg/kg Peripheral intravenous injection; single |
| References |
| Molecular Formula |
C15H18N8O5
|
|---|---|
| Molecular Weight |
390.35402
|
| Exact Mass |
390.14
|
| Elemental Analysis |
C, 46.15; H, 4.65; N, 28.71; O, 20.49
|
| CAS # |
313348-27-5
|
| Related CAS # |
Regadenoson-d3; 313348-27-5 (free); 875148-45-1 (hydrate)
|
| Appearance |
Solid powder
|
| SMILES |
CNC(=O)C1=CN(N=C1)C2=NC(=C3C(=N2)N(C=N3)[C@H]4[C@@H]([C@@H]([C@H](O4)CO)O)O)N
|
| InChi Key |
LZPZPHGJDAGEJZ-AKAIJSEGSA-N
|
| InChi Code |
InChI=1S/C15H18N8O5/c1-17-13(27)6-2-19-23(3-6)15-20-11(16)8-12(21-15)22(5-18-8)14-10(26)9(25)7(4-24)28-14/h2-3,5,7,9-10,14,24-26H,4H2,1H3,(H,17,27)(H2,16,20,21)/t7-,9-,10-,14-/m1/s1
|
| Chemical Name |
1-[6-amino-9-[(2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]purin-2-yl]-N-methylpyrazole-4-carboxamide
|
| Synonyms |
CVT-3146; CVT 3146; CVT3146; Lexiscan
|
| 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: 50~78 mg/mL (128.1~199.8 mM)
Ethanol: ~2 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.40 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 (6.40 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 (6.40 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 | 2.5618 mL | 12.8090 mL | 25.6180 mL | |
| 5 mM | 0.5124 mL | 2.5618 mL | 5.1236 mL | |
| 10 mM | 0.2562 mL | 1.2809 mL | 2.5618 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02130453 | Active Recruiting |
Drug: Regadenoson Ischemia |
Ischemia | M.D. Anderson Cancer Center | August 28, 2014 | Phase 4 |
| NCT04521569 | Recruiting | Drug: Ramosetron Drug: Placebo |
University of Maryland, Baltimore | June 22, 2020 | March 27, 2023 | Early Phase 1 |
| NCT04316676 | Recruiting | Drug: Regadenoson Diagnostic Test: CT-FFR |
Coronary Artery Disease | Emory University | June 16, 2021 | Not Applicable |
| NCT05583721 | Recruiting | Drug: [13N]NH3 Drug: Lexiscan |
Sickle Cell Disease | St. Jude Children's Research Hospital |
October 10, 2023 | Phase 2 |
| NCT04604782 | Recruiting | Drug: Regadenoson | Myocardial Ischemia Coronary Artery Disease |
GE Healthcare | May 20, 2021 | Phase 1 Phase 2 |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA