WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H532993
CAS#: 191219-80-4
Description: YM976 is an orally active PDE4 inhibitor (IC50 = 2.2 nM). YM976 has low emetogenic activity, suggested to be due to poor brain penetration.
Hodoodo Cat#: H532993
Name: YM976
CAS#: 191219-80-4
Chemical Formula: C17H16ClN3O
Exact Mass: 313.10
Molecular Weight: 313.790
Elemental Analysis: C, 65.07; H, 5.14; Cl, 11.30; N, 13.39; O, 5.10
Synonym: YM976; YM 976; YM-976.
IUPAC/Chemical Name: 4-(3-chlorophenyl)-1,7-diethyl-1H,2H-pyrido[2,3-d]pyrimidin-2-one
InChi Key: MNHXYNNKDDXKNP-UHFFFAOYSA-N
InChi Code: InChI=1S/C17H16ClN3O/c1-3-13-8-9-14-15(11-6-5-7-12(18)10-11)20-17(22)21(4-2)16(14)19-13/h5-10H,3-4H2,1-2H3
SMILES Code: O=C1N(CC)C2=NC(CC)=CC=C2C(C3=CC=CC(Cl)=C3)=N1
Appearance: Light yellow to yellow 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: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
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: | |
| In vitro activity: | |
| In vivo activity: |
The following data is based on the product molecular weight 313.79 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 |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
1: Mokrý J, Urbanová A, Medvedová I, Kertys M, Mikolka P, Kosutová P, Mokrá D. Effects of Selective Inhibition of PDE4 by YM976 on Airway Reactivity and Cough in Ovalbumin-Sensitized Guinea Pigs. Adv Exp Med Biol. 2016;921:61-70. doi: 10.1007/5584_2016_237. PubMed PMID: 27130219.
2: Jia WH, Yang P, Li J, Tian ZL. [Effects of selective phosphodiesterase 4 inhibitor on expression of aquaporin 5 in airway mucus hypersecretion model of rats]. Zhonghua Yi Xue Za Zhi. 2013 Feb 26;93(8):619-22. Chinese. PubMed PMID: 23663346.
3: Yaghi A, Zaman A, Cox G, Dolovich MB. Ciliary beating is depressed in nasal cilia from chronic obstructive pulmonary disease subjects. Respir Med. 2012 Aug;106(8):1139-47. doi: 10.1016/j.rmed.2012.04.001. Epub 2012 May 17. PubMed PMID: 22608352.
4: Xu Y, Zhang Y, Cardell LO. Nicotine enhances murine airway contractile responses to kinin receptor agonists via activation of JNK- and PDE4-related intracellular pathways. Respir Res. 2010 Jan 29;11:13. doi: 10.1186/1465-9921-11-13. PubMed PMID: 20113502; PubMed Central PMCID: PMC2845563.
5: Kowalczyk P, Kinjo T, Kowalczyk M, Walaszek Z, Hanausek M, Slaga TJ. Effect of phosphodiesterase antagonists on glucocorticoid mediated growth inhibition in murine skin cell lines. Eur J Pharmacol. 2009 May 21;610(1-3):29-36. doi: 10.1016/j.ejphar.2009.03.039. Epub 2009 Mar 21. PubMed PMID: 19306867.
6: Crowe SF, Neath J, Hale MW. The type 4 phosphodiesterase inhibitors rolipram and YM976 facilitate recall of the weak version of the passive avoidance task in the day-old chick. Pharmacol Biochem Behav. 2009 Apr;92(2):224-30. doi: 10.1016/j.pbb.2008.11.014. Epub 2008 Dec 7. PubMed PMID: 19100761.
7: Wang X, Li JQ, Chen L, Wang HX, Sun BB, Wang T, Xu D, Wen FQ. [Effects of phosphodiesterase-4 inhibitor on the mucin secretion in airway stimulated with acrolein: experiment with rats]. Zhonghua Yi Xue Za Zhi. 2008 Nov 18;88(42):2988-93. Chinese. PubMed PMID: 19080078.
8: Kitta T, Tanaka H, Mitsui T, Moriya K, Nonomura K. Type 4 phosphodiesterase inhibitor suppresses experimental bladder inflammation. BJU Int. 2008 Nov;102(10):1472-6. doi: 10.1111/j.1464-410X.2008.07662.x. Epub 2008 Apr 10. PubMed PMID: 18410434.
9: Yamamoto S, Sugahara S, Naito R, Ichikawa A, Ikeda K, Yamada T, Shimizu Y. The effects of a novel phosphodiesterase 7A and -4 dual inhibitor, YM-393059, on T-cell-related cytokine production in vitro and in vivo. Eur J Pharmacol. 2006 Jul 10;541(1-2):106-14. Epub 2006 May 12. PubMed PMID: 16780833.
10: Moriuchi H, Nakahara T, Maruko T, Sakamoto K, Ishii K. Relaxant effect of YM976, a novel phosphodiesterase 4 inhibitor, on bovine tracheal smooth muscle. Eur J Pharmacol. 2003 May 30;470(1-2):57-64. PubMed PMID: 12787831.
11: Aoki M, Fukunaga M, Sugimoto T, Hirano Y, Kobayashi M, Honda K, Yamada T. Studies on mechanisms of low emetogenicity of YM976, a novel phosphodiesterase type 4 inhibitor. J Pharmacol Exp Ther. 2001 Sep;298(3):1142-9. PubMed PMID: 11504812.
12: Aoki M, Yamamoto S, Kobayashi M, Ohga K, Kanoh H, Miyata K, Honda K, Yamada T. Antiasthmatic effect of YM976, a novel PDE4 inhibitor, in guinea pigs. J Pharmacol Exp Ther. 2001 Apr;297(1):165-73. PubMed PMID: 11259541.
13: Aoki M, Fukunaga M, Kitagawa M, Hayashi K, Morokata T, Ishikawa G, Kubo S, Yamada T. Effect of a novel anti-inflammatory compound, YM976, on antigen-induced eosinophil infiltration into the lungs in rats, mice, and ferrets. J Pharmacol Exp Ther. 2000 Dec;295(3):1149-55. PubMed PMID: 11082452.
14: Aoki M, Kobayashi M, Ishikawa J, Saita Y, Terai Y, Takayama K, Miyata K, Yamada T. A novel phosphodiesterase type 4 inhibitor, YM976 (4-(3-chlorophenyl)-1,7-diethylpyrido[2,3-d]pyrimidin-2(1H)-one), with little emetogenic activity. J Pharmacol Exp Ther. 2000 Oct;295(1):255-60. PubMed PMID: 10991987.
