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| 500mg |
Celiprolol is a potent, third generation, selective and oral β-adrenoceptor blocker with partial β2 agonist activity. It is known to have not only an antihypertensive effect but also an antioxidant effect through releasing nitric oxide.
| ln Vitro |
In Xenopus laevis oocytes, celiprolol (0-3 mM, 90 min) is taken up by the human intestine transporter OATP-A/1A2 [5]. P-glycoprotein is one of several transporters that help celiprolol (10 μM, 0–50 min) traverse human intestinal epithelial (Caco-2) cells [6].
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| ln Vivo |
In Otsuka Long-Evans Tokushima fat (OLETF) rats, celiprolol (oral, 100 mg/kg/day for 31 days) enhances arterial endothelial function and restores it 4 weeks following arterial endothelial denudation in OLETF rats[2]. After five weeks of treatment with 10 mg/kg/day of drinking water, celiprolol increases eNOS by stimulating the PI3K-Akt pathway and inhibits oxidative stress, NF-κB, and signal transduction. It also improves cardiovascular remodeling in hypertensive rats treated with deoxycorticosterone acetate (DOCA) salt [3].
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| Animal Protocol |
Animal/Disease Models: Type II male Otsuka Lang-Evans Tokushima fat (OLETF) diabetic rat [2]
Doses: 100 mg/kg/day for 31 days Route of Administration: Oral Experimental Results: Improved acetylcholine-induced NO dependence Sexual arterial dilation. Improves tone-related basal NO release and acetylcholine-induced NO-dependent relaxation in arterial and plasma NOx. Animal/Disease Models: Deoxycorticosterone acetate (DOCA)-salt hypertensive rats [3] Doses: 10 mg/kg/d for 5 weeks Route of Administration: Drinking water treatment Experimental Results: Activation of eNOS phosphorylation through the PI3K-Akt signaling pathway . Regulates VCAM-1 expression and is related to inhibiting NF-κB phosphorylation. Reduce ROS production by inhibiting the expression of NAD(P)H oxidase subunits p22phox, p47phox, gp91phox and nox1. |
| References |
[1]. James J Nawarskas, et, al. Celiprolol: A Unique Selective Adrenoceptor Modulator. Cardiol Rev. Sep/Oct 2017; 25(5): 247-253.
[2]. Toshio Hayashi, et al. beta1 antagonist and beta2 agonist, celiprolol, restores the impaired endothelial dependent and independent responses and decreased TNFalpha in rat with type II diabetes. Life Sci. 2007 Jan 16;80(6):592-9. [3]. Naohiko Kobayashi, et al. Celiprolol activates eNOS through the PI3K-Akt pathway and inhibits VCAM-1 Via NF-kappaB induced by oxidative stress. Hypertension. 2003 Nov;42(5):1004-13. [4]. R G Van Inwegen, et al. Effects of celiprolol (REV 5320), a new cardioselective beta-adrenoceptor antagonist, on in vitro adenylate cyclase, alpha- and beta-adrenergic receptor binding and lipolysis. Arch Int Pharmacodyn Ther. 1984 Nov;272(1):40-55. [5]. Yukio Kato, et al. Involvement of influx and efflux transport systems in gastrointestinal absorption of celiprolol. J Pharm Sci. 2009 Jul;98(7):2529-39. [6]. J. Karlsson, et al. Transport of celiprolol across human intestinal epithelial (Caco-2) cells: mediation of secretion by multiple transporters including P-glycoprotein. Br J Pharmacol. 1993 Nov; 110(3): 1009–1016. |
| Molecular Formula |
C20H33N3O4
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|---|---|
| Molecular Weight |
379.49372
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| CAS # |
56980-93-9
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| Related CAS # |
Celiprolol-d9 hydrochloride;1215535-20-8;Celiprolol hydrochloride;57470-78-7
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| SMILES |
O=C(NC1=CC=C(OCC(O)CNC(C)(C)C)C(C(C)=O)=C1)N(CC)CC
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| InChi Key |
JOATXPAWOHTVSZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H33N3O4/c1-7-23(8-2)19(26)22-15-9-10-18(17(11-15)14(3)24)27-13-16(25)12-21-20(4,5)6/h9-11,16,21,25H,7-8,12-13H2,1-6H3,(H,22,26)
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| Chemical Name |
3-(3-acetyl-4-(3-(tert-butylamino)-2-hydroxypropoxy)phenyl)-1,1-diethylurea
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| Synonyms |
Edsivo RHC-5320A RHC 5320A RHC5320A
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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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6351 mL | 13.1756 mL | 26.3512 mL | |
| 5 mM | 0.5270 mL | 2.6351 mL | 5.2702 mL | |
| 10 mM | 0.2635 mL | 1.3176 mL | 2.6351 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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