Bemoradan
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MedKoo CAT#: 577826

CAS#: 112018-01-6

Description: Bemoradan, also known as WJ-22867, is a potent, long-acting orally active inodilator and cardiotonic agent. Bemoradan is a novel, potent positive inotropic agent, demonstrated biphasic inhibition of the fraction III enzyme from canine cardiac muscle. Bemoradan is well and rapidly absorbed after oral dosing, has linear pharmacokinetics and long elimination half-lives across species.

Chemical Structure

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Bemoradan
CAS# 112018-01-6
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 577826
Name: Bemoradan
CAS#: 112018-01-6
Chemical Formula: C13H13N3O3
Exact Mass: 259.10
Molecular Weight: 259.260
Elemental Analysis: C, 60.23; H, 5.05; N, 16.21; O, 18.51

Price and Availability

Size Price Availability Quantity
1mg USD 150 Ready to Ship
5mg USD 450 Ready to Ship
10mg USD 750 Ready to Ship
25mg USD 1250 Ready to Ship
50mg USD 2050 Ready to Ship
100mg USD 3650 Ready to Ship
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Synonym: Bemoradan; (±)-Bemoradan; ORF 22867; ORF-22867; ORF22867; RWJ 22867; RWJ-22867; RWJ22867;

IUPAC/Chemical Name: 7-(4-methyl-6-oxo-1,4,5,6-tetrahydropyridazin-3-yl)-2H-benzo[b][1,4]oxazin-3(4H)-one

InChi Key: XZPGINPFWXLYNW-UHFFFAOYSA-N

InChi Code: InChI=1S/C13H13N3O3/c1-7-4-11(17)15-16-13(7)8-2-3-9-10(5-8)19-6-12(18)14-9/h2-3,5,7H,4,6H2,1H3,(H,14,18)(H,15,17)

SMILES Code: CC1CC(=O)NN=C1C2=CC3=C(C=C2)NC(=O)CO3

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: To be determined

Shelf Life: >2 years if stored properly

Drug Formulation: To be determined

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target: Bemoradan is believed to act by inhibiting various enzymes and signaling pathways involved in the development and progression of diseases. Bemoradan has been shown to inhibit the activity of various kinases, including PI3K and AKT, which are involved in cancer cell proliferation and survival. It has also been shown to inhibit the activity of GSK-3β, which is involved in the accumulation of tau protein in neurodegenerative disorders.
In vitro activity: To be determined
In vivo activity: Bemoradan was found to be an extremely potent and selective inhibitor of canine PDE fraction III and a long-acting, potent, orally active inotropic vasodilator agent in various canine models. Positive inotropic activity was maintained for between 8 and 24 h after a single oral dose of bemoradan in dogs, thus making it a very potent and long-acting orally effective inotrope. Reference: J Med Chem. 1990 Jan;33(1):380-6. https://pubmed.ncbi.nlm.nih.gov/2153210/

Preparing Stock Solutions

The following data is based on the product molecular weight 259.26 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Combs DW, Rampulla MS, Bell SC, Klaubert DH, Tobia AJ, Falotico R, Haertlein B, Lakas-Weiss C, Moore JB. 6-Benzoxazinylpyridazin-3-ones: potent, long-acting positive inotrope and peripheral vasodilator agents. J Med Chem. 1990 Jan;33(1):380-6. doi: 10.1021/jm00163a061. PMID: 2153210. 2. Moore JB Jr, Combs DW, Tobia AJ. Bemoradan--a novel inhibitor of the rolipram-insensitive cyclic AMP phosphodiesterase from canine heart tissue. Biochem Pharmacol. 1991 Jul 15;42(3):679-83. doi: 10.1016/0006-2952(91)90331-x. PMID: 1650219.
In vitro protocol: To be determined
In vivo protocol: 1. Combs DW, Rampulla MS, Bell SC, Klaubert DH, Tobia AJ, Falotico R, Haertlein B, Lakas-Weiss C, Moore JB. 6-Benzoxazinylpyridazin-3-ones: potent, long-acting positive inotrope and peripheral vasodilator agents. J Med Chem. 1990 Jan;33(1):380-6. doi: 10.1021/jm00163a061. PMID: 2153210. 2. Moore JB Jr, Combs DW, Tobia AJ. Bemoradan--a novel inhibitor of the rolipram-insensitive cyclic AMP phosphodiesterase from canine heart tissue. Biochem Pharmacol. 1991 Jul 15;42(3):679-83. doi: 10.1016/0006-2952(91)90331-x. PMID: 1650219.

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1: Wu WN, Caldwell GW, Masucci JA, Gauthier AD. Evaluation of the excretion, and metabolism of the cardiotonic agent bemoradan in male rats and female beagle dogs. Eur J Drug Metab Pharmacokinet. 2001 Oct-Dec;26(4):263-71. doi: 10.1007/BF03226381. PMID: 11808869.


2: Derian CK, Santulli RJ, Rao PE, Solomon HF, Barrett JA. Inhibition of chemotactic peptide-induced neutrophil adhesion to vascular endothelium by cAMP modulators. J Immunol. 1995 Jan 1;154(1):308-17. PMID: 7995950.


3: Huang SM, Brusser L, Chien SC, Simon D, Smith IL, Abrams LS, Lasseter K. Pharmacokinetics and bioavailability of bemoradan, a long-acting inodilator in healthy males. Int J Clin Pharmacol Ther. 1994 Feb;32(2):62-4. PMID: 8004360.


4: Huang SM, Falotico R, Haertlein B, Smith IL. Simultaneous monitoring of bemoradan pharmacokinetics and hemodynamics in mongrel dogs. Biopharm Drug Dispos. 1992 Oct;13(7):539-47. doi: 10.1002/bdd.2510130707. PMID: 1489944.


5: Combs DW, Rampulla MS, Demers JP, Falotico R, Moore JB. Heteroatom analogues of bemoradan: chemistry and cardiotonic activity of 1,4-benzothiazinylpyridazinones. J Med Chem. 1992 Jan;35(1):172-6. doi: 10.1021/jm00079a023. PMID: 1732525.


6: Moore JB Jr, Combs DW, Tobia AJ. Bemoradan--a novel inhibitor of the rolipram-insensitive cyclic AMP phosphodiesterase from canine heart tissue. Biochem Pharmacol. 1991 Jul 15;42(3):679-83. doi: 10.1016/0006-2952(91)90331-x. PMID: 1650219.


7: Huang SM, Chien SC, Flor SC. A sensitive high performance liquid chromatography microassay for bemoradan, a novel cardiotonic agent, in plasma/serum using a semi-automatic liquid/solid extraction sample preparation system--AASP. Biomed Chromatogr. 1990 Mar;4(2):52-5. doi: 10.1002/bmc.1130040203. PMID: 2350597.


8: Combs DW, Rampulla MS, Bell SC, Klaubert DH, Tobia AJ, Falotico R, Haertlein B, Lakas-Weiss C, Moore JB. 6-Benzoxazinylpyridazin-3-ones: potent, long-acting positive inotrope and peripheral vasodilator agents. J Med Chem. 1990 Jan;33(1):380-6. doi: 10.1021/jm00163a061. PMID: 2153210.