Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DM8GZWC)

Drug Name

DS-4574 Drug Info

Synonyms

DS 4574; DS-4574; 118314-35-5; 6-(2-Cyclohexylethyl)-(1,3,4)thiadiazolo(3,2-a)-1,2,3-triazolo(4,5-d)pyrimidin-9(1H)-one; (1,3,4)Thiadiazolo(3,2-a)-1,2,3-triazolo(4,5-d)pyrimidin-9(1H)-one, 6-(2-cyclohexylethyl)-; [1,3,4]Thiadiazolo[3,2-a]-1,2,3-triazolo[4,5-d]pyrimidin-9(3H)-one,6-(2-cyclohexylethyl)-; AC1L4LXR; ACMC-20c9t1; AC1Q6E9S; SCHEMBL156066; CTK4B0638; DTXSID80152096; AKOS030534249; 6-(2-cyclohexylethyl)[1,3,4]thiadiazolo[3,2-a][1,2,3]triazolo[4,5-d]pyrimidin-9(2h)-one; LS-150402

Indication

Disease Entry	ICD 11	Status	REF
Asthma	CA23	Discontinued in Phase 2	[1]

Cross-matching ID

PubChem CID: 159491
CAS Number: CAS 118314-35-5
TTD Drug ID: DM8GZWC

Molecule-Related Drug Atlas

Molecule Type:

DTT

Drug Status:

Approved Drug(s)

Clinical Trial Drug(s)

Discontinued Drug(s)

Investigative Drug(s)

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Drug(s) Targeting Leukotriene CysLT1 receptor (CYSLTR1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Montelukast	DMD157S	Allergic asthma	CA23.0	Approved	[3]
Zafirlukast	DMHNQOG	Asthma	CA23	Approved	[4]
Pranlukast	DMYHDCA	Allergic rhinitis	CA08.0	Approved	[5]
Cinalukast	DMFIC0M	Asthma	CA23	Approved	[6]
KP-496	DMCO8UZ	Asthma	CA23	Phase 2	[7]
BAY-X-7195	DM2XE80	Asthma	CA23	Phase 2	[8]
Masilukast	DMDTI0L	Asthma	CA23	Phase 2	[9]
LM-1507.NA	DMW6VA0	Asthma	CA23	Phase 2	[10]
Iralukast	DMQ3RWN	Asthma	CA23	Phase 2	[11]
YM-57158	DMS31YW	Allergic rhinitis	CA08.0	Phase 1	[12]
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Drug(s) Targeting Leukotriene CysLT2 receptor (CYSLTR2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
BAY-X-7195	DM2XE80	Asthma	CA23	Phase 2	[8]
AS-35	DMC2WI7	Asthma	CA23	Discontinued in Phase 2	[13]
Sulukast	DMBSLZV	Asthma	CA23	Discontinued in Phase 2	[14]
ICI-198615	DM0195G	Asthma	CA23	Terminated	[15]
MDL-43291	DMBIDQX	Asthma	CA23	Terminated	[16]
LY-290154	DMPZ7AO	Asthma	CA23	Terminated	[17]
FPL-55712	DMF1CDK	Asthma	CA23	Terminated	[18]
LTE4	DMCPB0Q	Discovery agent	N.A.	Investigative	[19]
LTC4	DM702WR	Discovery agent	N.A.	Investigative	[20]
LTD4	DMIUZX3	Discovery agent	N.A.	Investigative	[20]
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Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

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Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Leukotriene CysLT1 receptor (CYSLTR1)	TTGKOY9	CLTR1_HUMAN	Modulator	[2]
Leukotriene CysLT2 receptor (CYSLTR2)	TT0PZR5	CLTR2_HUMAN	Modulator	[2]

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References

1	Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000587)
2	Inhibitory effect of DS-4574, a mast cell stabilizer with peptidoleukotriene receptor antagonism, on gastric acid secretion in rats. Eur J Pharmacol. 1994 Apr 1;255(1-3):229-34.
3	Protective potential of montelukast against hepatic ischemia/reperfusion injury in rats. J Surg Res. 2010 Mar;159(1):588-94.
4	Inhibitory effects of zafirlukast on respiratory bursts of human neutrophils. Drugs Exp Clin Res. 2002;28(4):133-45.
5	Beneficial effects of leukotriene receptor antagonists in the prevention of cedar pollinosis in a community setting. J Investig Allergol Clin Immunol. 2009;19(3):195-203.
6	Prolonged protection against exercise-induced bronchoconstriction by the leukotriene D4-receptor antagonist cinalukast. J Allergy Clin Immunol. 1997 Feb;99(2):210-5.
7	Effects of KP-496, a novel dual antagonist for leukotriene D4 and thromboxane A2 receptors, on contractions induced by various agonists in the guinea pig trachea. Allergol Int. 2006 Dec;55(4):403-10.
8	The effect of a novel leukotriene C4/D4 antagonist, BAY-x-7195, on experimental allergic reactions. Prostaglandins. 1995 Nov-Dec;50(5-6):269-85.
9	Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
10	Pharmacological differences among CysLT(1) receptor antagonists with respect to LTC(4) and LTD(4) in human lung parenchyma. Biochem Pharmacol. 2002 Apr 15;63(8):1537-46.
11	Pharmacological characterization of the cysteinyl-leukotriene antagonists CGP 45715A (iralukast) and CGP 57698 in human airways in vitro. Br J Pharmacol. 1998 Feb;123(3):590-8.
12	In vitro pharmacologic profile of YM158, a new dual antagonist for LTD4 and TXA2 receptors. J Pharmacol Exp Ther. 1998 Nov;287(2):633-9.
13	Inhibition of radiolabeled leukotriene-binding by AS-35 in guinea pig lung membrane fraction. Jpn J Pharmacol. 1992 Apr;58(4):357-64.
14	The pharmacological evaluation of LY 170680, a novel leukotriene D4 and E4 antagonist in the guinea-pig. Br J Pharmacol. 1989 Sep;98(1):259-67.
15	Heterogeneity of binding sites for ICI 198,615 in human lung parenchyma. Biochem Pharmacol. 1992 Oct 6;44(7):1411-5.
16	Conformationally restricted leukotriene receptor antagonists: [(octahydro-2-oxo-7-tetradecylidene-2H-1-benzopyran-8-yl)thio]ace tic acids. Pharmacology. 1990;40(5):271-6.
17	DOI: 10.1021/op060036x
18	Effect of the leukotriene receptor antagonists FPL 55712, LY 163443, and MK-571 on the elimination of cysteinyl leukotrienes in the rat. Br J Pharmacol. 1991 Apr;102(4):865-70.
19	Differential signaling of cysteinyl leukotrienes and a novel cysteinyl leukotriene receptor 2 (CysLT agonist, N-methyl-leukotriene C in calcium reporter and beta arrestin assays. Mol Pharmacol. 2011 Feb;79(2):270-8.
20	Molecular cloning and characterization of a second human cysteinyl leukotriene receptor: discovery of a subtype selective agonist. Mol Pharmacol. 2000 Dec;58(6):1601-8.