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(R)-Carvedilol 95093-99-5

(R)-Carvedilol 95093-99-5

CAS No.: 95093-99-5

(R)-Carvedilol is an optically active and R-enantiomer of Carvedilol, which is a nonselective ß-adrenergic blocker with
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(R)-Carvedilol is an optically active and R-enantiomer of Carvedilol, which is a nonselective ß-adrenergic blocker with a1-blocking activity. It treats congestive heart failure by acting as an antihypertensive medication./p>

Physicochemical Properties


Molecular Formula C₂₄H₂₆N₂O₄
Molecular Weight 406.47
Exact Mass 406.189
CAS # 95093-99-5
Related CAS # Carvedilol;72956-09-3; (S)-Carvedilol; 95094-00-1; Carvedilol phosphate hemihydrate; 610309-89-2; (R)-Carvedilol-d4; 2747915-92-8
PubChem CID 185394
Appearance White to off-white solid
Density 1.25g/cm3
Boiling Point 655.2ºC at 760 mmHg
Melting Point 114-115ºC
Flash Point 350.1ºC
Index of Refraction 1.657
LogP 4.128
Hydrogen Bond Donor Count 3
Hydrogen Bond Acceptor Count 5
Rotatable Bond Count 10
Heavy Atom Count 30
Complexity 508
Defined Atom Stereocenter Count 1
SMILES

O(C1C=CC=C2C=1C1C=CC=CC=1N2)C[C@H](O)CNCCOC1C=CC=CC=1OC

InChi Key OGHNVEJMJSYVRP-QGZVFWFLSA-N
InChi Code

InChI=1S/C24H26N2O4/c1-28-21-10-4-5-11-22(21)29-14-13-25-15-17(27)16-30-23-12-6-9-20-24(23)18-7-2-3-8-19(18)26-20/h2-12,17,25-27H,13-16H2,1H3/t17-/m1/s1
Chemical Name

(2R)-1-(9H-carbazol-4-yloxy)-3-[2-(2-methoxyphenoxy)ethylamino]propan-2-ol
Synonyms

(R)-Carvedilol; (R) Carvedilol; (R)-BM 14190
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)

Biological Activity


Targets β/α-1 adrenergic receptor
References

[1]. Protective effects of S-carvedilol on doxorubicin-induced damages to human umbilical vein endothelial cells and rats. J Appl Toxicol. 2019 Aug;39(8):1233-1244.

Additional Infomation See also: Carvedilol (annotation moved to).

Solubility Data


Solubility (In Vitro) DMSO: ~220 mg/mL (~541.3 mM)
Solubility (In Vivo) Solubility in Formulation 1: ≥ 5.5 mg/mL (13.53 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 55.0 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: 5.5 mg/mL (13.53 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 55.0 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.

Solubility in Formulation 3: ≥ 5.5 mg/mL (13.53 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 55.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.4602 mL 12.3010 mL 24.6021 mL
5 mM 0.4920 mL 2.4602 mL 4.9204 mL
10 mM 0.2460 mL 1.2301 mL 2.4602 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.