CI-930 | CAS#86798-59-6 | PDE-III inhibitor

MedKoo Cat#: 145011 | Name: CI-930

Description:

WARNING: This product is for research use only, not for human or veterinary use.

CI-930 is a PDE-III inhibitor with a wide-spectrum activity. The anti-aggregating action of CI-930 may be exerted by dual mechanisms, both increasing cAMP contents and selectively inhibiting TXA2 synthesis in platelets. CI-930 inhibited platelet aggregation triggered by AA, U-46619, ADP, collagen and PAF, with the IC50 values of 0.91, 0.73, 2.12, 2.35 and 7.15 mumols/L, respectively.

Chemical Structure

CI-930

CAS#86798-59-6

Theoretical Analysis

MedKoo Cat#: 145011

Name: CI-930

CAS#: 86798-59-6

Chemical Formula: C14H14N4O

Exact Mass: 254.1168

Molecular Weight: 254.29

Elemental Analysis: C, 66.13; H, 5.55; N, 22.03; O, 6.29

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.

Bulk Inquiry

Related CAS #

No Data

Synonym

CI-930; CI 930; CI930;

IUPAC/Chemical Name

6-(4-(1H-imidazol-1-yl)phenyl)-5-methyl-4,5-dihydropyridazin-3(2H)-one

InChi Key

AEZZPAQOEUQNBB-UHFFFAOYSA-N

InChi Code

1S/C14H14N4O/c1-10-8-13(19)16-17-14(10)11-2-4-12(5-3-11)18-7-6-15-9-18/h2-7,9-10H,8H2,1H3,(H,16,19)

SMILES Code

CC1CC(=O)NN=C1C2=CC=C(C=C2)N3C=CN=C3

Appearance

To be determined

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

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 254.29 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.

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

1: Jiang YY, Fu CD, Liao LM, Huang TG, Chen XS, Long K. Effects of CI-930 on hemostasis, thrombosis, and AA-induced hemodynamic reaction. Zhongguo Yao Li Xue Bao. 1991 Jul;12(4):331-5. PMID: 1807082. 2: Chen XS, Zeng HW, Jiang YY, Wan WQ, Long K. Effects of CI-930, a novel phosphodiesterase III inhibitor, on platelet aggregation and arachidonic acid metabolism. Zhongguo Yao Li Xue Bao. 1990 Jul;11(4):338-43. PMID: 1966575. 3: Mancini D, Keren G, Sonnenblick EH, LeJemtel TH. CI-930, a new cardiotonic and vasodilating agent: hemodynamic comparison to dobutamine and long-term clinical effects. Am Heart J. 1988 Oct;116(4):1008-16. doi: 10.1016/0002-8703(88)90152-4. PMID: 3177174. 4: Johnson-Mills K, Arauz E, Coffey RG, Krzanowski JJ Jr, Polson JB. Effect of CI-930 [3-(2H)-pyridazinone-4,5-dihydro-6-[4-(1H-imidazolyl) phenyl]-5-methyl- monohydrochloride] and rolipram on human coronary artery smooth muscle cell proliferation. Biochem Pharmacol. 1998 Oct 15;56(8):1065-73. doi: 10.1016/s0006-2952(98)00239-1. PMID: 9776320. 5: Yuan QM, Zhao ZH, Xu BS. Efficacy and safety of tranexamic acid in reducing blood loss in scoliosis surgery: a systematic review and meta-analysis. Eur Spine J. 2017 Jan;26(1):131-139. doi: 10.1007/s00586-016-4899-0. Epub 2016 Nov 29. PMID: 27900553. 6: Murali S, Uretsky BF, Valdes AM, Kolesar JA, Reddy PS. Acute hemodynamic and hormonal effects of CI-930, a new phosphodiesterase inhibitor, in severe congestive heart failure. Am J Cardiol. 1987 Jun 1;59(15):1356-60. doi: 10.1016/0002-9149(87)90919-2. PMID: 3591691. 7: Lewis GM, Caccese RG, Heaslip RJ, Bansbach CC. Effects of rolipram and CI-930 on IL-2 mRNA transcription in human Jurkat cells. Agents Actions. 1993;39 Spec No:C89-92. doi: 10.1007/BF01972730. PMID: 8273597. 8: Lee KC, Clas DM, Gorczyca WP, Silver PJ, Ezrin AM. Comparisons of the depressor, inotropic and renal effects of milrinone and CI-930 to different pure vasodilators and diuretics in conscious instrumented dogs. Drugs Exp Clin Res. 1991;17(7):323-36. PMID: 1686584. 9: Jafri SM, Burlew BS, Goldberg AD, Olson S, Froelich JW, Goldstein S. Hemodynamic, pharmacokinetic and clinical response to CI-930 in congestive heart failure due to ischemic or dilated cardiomyopathy. Am J Cardiol. 1987 May 1;59(12):1126-30. doi: 10.1016/0002-9149(87)90860-5. PMID: 3578054. 10: Sircar I, Duell BL, Cain MH, Burke SE, Bristol JA. Cardiotonic agents. 4. Synthesis and biological evaluation of N-substituted 2,4,4a,5-tetrahydro-3H-indeno[1,2-c]pyridazin-3-ones: rigid structures derived from CI-930 and analogues. J Med Chem. 1986 Nov;29(11):2142-8. doi: 10.1021/jm00161a003. PMID: 3783575. 11: Silver PJ. Biochemical aspects of inhibition of cardiovascular low (Km) cyclic adenosine monophosphate phosphodiesterase. Am J Cardiol. 1989 Jan 3;63(2):2A-8A. doi: 10.1016/0002-9149(89)90384-6. PMID: 2535910. 12: O'Byrne KK, Haddock CK, Poston WS. Parenting style and adolescent smoking. J Adolesc Health. 2002 Jun;30(6):418-25. doi: 10.1016/s1054-139x(02)00370-1. PMID: 12039511. 13: Robicsek SA, Blanchard DK, Djeu JY, Krzanowski JJ, Szentivanyi A, Polson JB. Multiple high-affinity cAMP-phosphodiesterases in human T-lymphocytes. Biochem Pharmacol. 1991 Jul 25;42(4):869-77. doi: 10.1016/0006-2952(91)90047-9. PMID: 1651080. 14: Lindgren S, Rascón A, Andersson KE, Manganiello V, Degerman E. Selective inhibition of cGMP-inhibited and cGMP-noninhibited cyclic nucleotide phosphodiesterases and relaxation of rat aorta. Biochem Pharmacol. 1991 Jul 15;42(3):545-52. doi: 10.1016/0006-2952(91)90317-x. PMID: 1650216. 15: Howell RE, Jenkins LP, Howell DE. Inhibition of lipopolysaccharide-induced pulmonary edema by isozyme-selective phosphodiesterase inhibitors in guinea pigs. J Pharmacol Exp Ther. 1995 Nov;275(2):703-9. PMID: 7473157. 16: Harris AL, Connell MJ, Ferguson EW, Wallace AM, Gordon RJ, Pagani ED, Silver PJ. Role of low Km cyclic AMP phosphodiesterase inhibition in tracheal relaxation and bronchodilation in the guinea pig. J Pharmacol Exp Ther. 1989 Oct;251(1):199-206. PMID: 2552074. 17: Xiong Y, Westhead EW, Slakey LL. Role of phosphodiesterase isoenzymes in regulating intracellular cyclic AMP in adenosine-stimulated smooth muscle cells. Biochem J. 1995 Jan 15;305 ( Pt 2)(Pt 2):627-33. doi: 10.1042/bj3050627. PMID: 7832782; PMCID: PMC1136408. 18: Dundore RL, Habeeb PG, Pratt PF, Becker LT, Clas DM, Buchholz RA. Differential hemodynamic responses to selective inhibitors of cyclic nucleotide phosphodiesterases in conscious rats. J Cardiovasc Pharmacol. 1992 Jun;19(6):937-44. doi: 10.1097/00005344-199206000-00015. PMID: 1376816. 19: Pan X, Arauz E, Krzanowski JJ, Fitzpatrick DF, Polson JB. Synergistic interactions between selective pharmacological inhibitors of phosphodiesterase isozyme families PDE III and PDE IV to attenuate proliferation of rat vascular smooth muscle cells. Biochem Pharmacol. 1994 Aug 17;48(4):827-35. doi: 10.1016/0006-2952(94)90062-0. PMID: 7521642. 20: LeJemtel TH, Keren G, Reis D, Sonnenblick EH. The role of novel inotropic agents in the treatment of heart failure. J Cardiovasc Pharmacol. 1986;8 Suppl 9:S47-54. PMID: 2433542.