YM976
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 532993

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.


Price and Availability

Size
Price

10mg
USD 270
Size
Price

20mg
USD 495
Size
Price

YM976, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received. Delivery time: overnight (USA/Canada); 3-5 days (worldwide).


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 532993
Name: YM976
CAS#: 191219-80-4
Chemical Formula: C17H16ClN3O
Exact Mass: 313.0982
Molecular Weight: 313.79
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


Technical Data

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).

Harmonized System Code:
293490


References

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.