Compounds > cs 0777
Page last updated: 2024-11-12

cs 0777

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

CS 0777: a sphingosine-1-phosphate receptor modulator [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID11371290
CHEMBL ID1951587
SCHEMBL ID1454408
MeSH IDM0569941

Synonyms (14)

Synonym
SCHEMBL1454408
cs-0777 ,
cs 0777
1192731-63-7
CHEMBL1951587
(2r)-2-amino-2-methyl-4-{1-methyl-5-[4-(4-methylphenyl)butanoyl]pyrrol-2-yl}butan-1-ol
YXEQXPNSBUIRDZ-OAQYLSRUSA-N
kch74qg79a ,
unii-kch74qg79a
827344-05-8
1-butanone, 1-(5-((3r)-3-amino-4-hydroxy-3-methylbutyl)-1-methyl-1h-pyrrol-2-yl)-4-(4-methylphenyl)-
Q27282183
(r)-1-(5-(3-amino-4-hydroxy-3-methylbutyl)-1-methyl-1h-pyrrol-2-yl)-4-(p-tolyl)butan-1-one
STARBLD0033600

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
"Pharmacokinetic (PK) and pharmacodynamic (PD) modeling was conducted for the reduction of peripheral lymphocytes after oral administration of CS-0777 to healthy rats, monkeys and experimental autoimmune encephalomyelitis (EAE) induced rats."( Evaluation of species difference in peripheral lymphocyte reduction effect of CS-0777, a sphingosine 1-phosphate receptor modulator, based on a pharmacokinetic/pharmacodynamic model analysis.
Doi-Komuro, H; Goto, M; Inaba, SI; Inoue, R; Izumi, T; Kagari, T; Oshima, K; Shimozato, T; Tanaka, H; Tanaka-Takanaka, K; Tomisato, W; Yuita, H, 2016)		0.43

Bioavailability

ExcerptReferenceRelevance
" After oral administration of [14C]CS-0777, CS-0777 was well absorbed in rats and monkeys with total recoveries of over 90% of the dose, majorly in feces."( Pharmacokinetics and disposition of CS-0777, a sphingosine 1-phosphate receptor modulator, in rats and monkeys.
Goto, M; Ikeda, T; Inaba, S; Iwabuchi, H; Izumi, T; Takahashi, M; Tanaka, H, 2015)		0.42

Dosage Studied

ExcerptRelevanceReference
" Subsequently, simulations were utilized to design a multiple ascending dose study with adaptive dosing regimens that would meet targeted pharmacodynamic (PD) response thresholds (eg, minimum 40% reduction in lymphocytes) while maintaining CD4 counts above a reasonable safety threshold."( Use of an exposure-response model to aid early drug development of an oral sphingosine 1-phosphate receptor modulator.
Carrothers, TJ; Inaba, S; Moberly, JB; Rohatagi, S; Shimozato, T; Truitt, KE; Zahir, H, 2009)		0.35
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (33)

Assay IDTitleYearJournalArticle
AID645304Oral bioavailability in Sprague-Dawley rat assessed as CS-0777-phosphate at 0.1 mg/kg2011ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5
Discovery of CS-0777: A Potent, Selective, and Orally Active S1P1 Agonist.
AID645096Lymphopenic activity in Lewis rat assessed as recovery of blood lymphocytes at 1 mg/kg, po after 48 hrs relative to control2011ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5
Discovery of CS-0777: A Potent, Selective, and Orally Active S1P1 Agonist.
AID645100Reduction of cumulative disease score in Lewis rat EAE model at 1 mg/kg, po administered daily for 20 days measured after 8 to 21 days relative to control2011ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5
Discovery of CS-0777: A Potent, Selective, and Orally Active S1P1 Agonist.
AID645104Tmax in Sprague-Dawley rat at 1 mg/kg, po2011ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5
Discovery of CS-0777: A Potent, Selective, and Orally Active S1P1 Agonist.
AID1054249Half life of the compound2013Bioorganic & medicinal chemistry letters, Dec-01, Volume: 23, Issue:23
Modulators of the Sphingosine 1-phosphate receptor 1.
AID645114Volume of distribution at steady state in Sprague-Dawley rat at 1 mg/kg, iv2011ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5
Discovery of CS-0777: A Potent, Selective, and Orally Active S1P1 Agonist.
AID645112Total body clearance in Sprague-Dawley rat at 1 mg/kg, iv2011ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5
Discovery of CS-0777: A Potent, Selective, and Orally Active S1P1 Agonist.
AID645101Cmax in Sprague-Dawley rat at 0.1 mg/kg, po2011ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5
Discovery of CS-0777: A Potent, Selective, and Orally Active S1P1 Agonist.
AID645107AUC (0 to infinity) in Sprague-Dawley rat at 0.1 mg/kg, po2011ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5
Discovery of CS-0777: A Potent, Selective, and Orally Active S1P1 Agonist.
AID645102Cmax in Sprague-Dawley rat at 1 mg/kg, po2011ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5
Discovery of CS-0777: A Potent, Selective, and Orally Active S1P1 Agonist.
AID645299Tmax in Sprague-Dawley rat assessed as CS-0777-phosphate at 1 mg/kg, po2011ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5
Discovery of CS-0777: A Potent, Selective, and Orally Active S1P1 Agonist.
AID645296Cmax in Sprague-Dawley rat assessed as CS-0777-phosphate at 0.1 mg/kg, po2011ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5
Discovery of CS-0777: A Potent, Selective, and Orally Active S1P1 Agonist.
AID645303AUC (0 to infinity) in Sprague-Dawley rat assessed as CS-0777-phosphate at 1 mg/kg, po2011ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5
Discovery of CS-0777: A Potent, Selective, and Orally Active S1P1 Agonist.
AID645298Tmax in Sprague-Dawley rat assessed as CS-0777-phosphate at 0.1 mg/kg, po2011ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5
Discovery of CS-0777: A Potent, Selective, and Orally Active S1P1 Agonist.
AID645300Half life in Sprague-Dawley rat assessed as CS-0777-phosphate at 0.1 mg/kg, po2011ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5
Discovery of CS-0777: A Potent, Selective, and Orally Active S1P1 Agonist.
AID645098Lymphopenic activity in Lewis rat assessed as recovery in blood lymphocyte counts at 1 mg/kg, po after 5 days2011ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5
Discovery of CS-0777: A Potent, Selective, and Orally Active S1P1 Agonist.
AID645095Lymphopenic activity in Lewis rat assessed as recovery of blood lymphocytes at 0.1 mg/kg, po after 48 hrs relative to control2011ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5
Discovery of CS-0777: A Potent, Selective, and Orally Active S1P1 Agonist.
AID645105Half life in Sprague-Dawley rat at 0.1 mg/kg, po2011ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5
Discovery of CS-0777: A Potent, Selective, and Orally Active S1P1 Agonist.
AID645110Oral bioavailability in Sprague-Dawley rat at 1 mg/kg2011ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5
Discovery of CS-0777: A Potent, Selective, and Orally Active S1P1 Agonist.
AID645099Reduction of cumulative disease score in Lewis rat EAE model at 0.1 mg/kg, po administered daily for 20 days measured after 8 to 21 days relative to control2011ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5
Discovery of CS-0777: A Potent, Selective, and Orally Active S1P1 Agonist.
AID645093Lymphopenic activity in Lewis rat assessed as reduction in blood lymphocyte counts at 0.1 mg/kg, po after 12 hrs relative to control2011ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5
Discovery of CS-0777: A Potent, Selective, and Orally Active S1P1 Agonist.
AID645113Volume of distribution at steady state in Sprague-Dawley rat at 0.1 mg/kg, iv2011ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5
Discovery of CS-0777: A Potent, Selective, and Orally Active S1P1 Agonist.
AID645111Total body clearance in Sprague-Dawley rat at 0.1 mg/kg, iv2011ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5
Discovery of CS-0777: A Potent, Selective, and Orally Active S1P1 Agonist.
AID645305Oral bioavailability in Sprague-Dawley rat assessed as CS-0777-phosphate at 1 mg/kg2011ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5
Discovery of CS-0777: A Potent, Selective, and Orally Active S1P1 Agonist.
AID645297Cmax in Sprague-Dawley rat assessed as CS-0777-phosphate at 1 mg/kg, po2011ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5
Discovery of CS-0777: A Potent, Selective, and Orally Active S1P1 Agonist.
AID645302AUC (0 to infinity) in Sprague-Dawley rat assessed as CS-0777-phosphate at 0.1 mg/kg, po2011ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5
Discovery of CS-0777: A Potent, Selective, and Orally Active S1P1 Agonist.
AID645108AUC (0 to infinity) in Sprague-Dawley rat at 1 mg/kg, po2011ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5
Discovery of CS-0777: A Potent, Selective, and Orally Active S1P1 Agonist.
AID645109Oral bioavailability in Sprague-Dawley rat at 0.1 mg/kg2011ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5
Discovery of CS-0777: A Potent, Selective, and Orally Active S1P1 Agonist.
AID645106Half life in Sprague-Dawley rat at 1 mg/kg, po2011ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5
Discovery of CS-0777: A Potent, Selective, and Orally Active S1P1 Agonist.
AID645097Lymphopenic activity in Lewis rat assessed as recovery in blood lymphocyte counts at 0.1 mg/kg, po after 5 days2011ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5
Discovery of CS-0777: A Potent, Selective, and Orally Active S1P1 Agonist.
AID645103Tmax in Sprague-Dawley rat at 0.1 mg/kg, po2011ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5
Discovery of CS-0777: A Potent, Selective, and Orally Active S1P1 Agonist.
AID645094Lymphopenic activity in Lewis rat assessed as reduction in blood lymphocyte counts at 1 mg/kg, po after 12 hrs relative to control2011ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5
Discovery of CS-0777: A Potent, Selective, and Orally Active S1P1 Agonist.
AID645301Half life in Sprague-Dawley rat assessed as CS-0777-phosphate at 1 mg/kg, po2011ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5
Discovery of CS-0777: A Potent, Selective, and Orally Active S1P1 Agonist.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (10)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (10.00)29.6817
2010's9 (90.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 18.24

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index18.24 (24.57)
Research Supply Index2.56 (2.92)
Research Growth Index5.62 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (18.24)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials2 (20.00%)5.53%
Reviews1 (10.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other7 (70.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
pyrroles
1H-pyrrole : A tautomer of pyrrole that has the double bonds at positions 2 and 4.. pyrrole : A five-membered monocyclic heteroarene comprising one NH and four CH units which forms the parent compound of the pyrrole group of compounds. Its five-membered ring structure has three tautomers. A 'closed class'.. azole : Any monocyclic heteroarene consisting of a five-membered ring containing nitrogen. Azoles can also contain one or more other non-carbon atoms, such as nitrogen, sulfur or oxygen.		5.5482pyrrole;
secondary amine
levamisole
Levamisole: An antihelminthic drug that has been tried experimentally in rheumatic disorders where it apparently restores the immune response by increasing macrophage chemotaxis and T-lymphocyte function. Paradoxically, this immune enhancement appears to be beneficial in rheumatoid arthritis where dermatitis, leukopenia, and thrombocytopenia, and nausea and vomiting have been reported as side effects. (From Smith and Reynard, Textbook of Pharmacology, 1991, p435-6). levamisole : A 6-phenyl-2,3,5,6-tetrahydroimidazo[2,1-b][1,3]thiazole that has S configuration. It is used (generally as the monohydrochloride salt) to treat parasitic worm infections in pigs, sheep and cattle and was formerly used in humans as an adjuvant to chemotherapy for the treatment of various cancers. It is also widely used as an adulterant to coccaine.		2.17106-phenyl-2,3,5,6-tetrahydroimidazo[2,1-b][1,3]thiazoleantinematodal drug;
antirheumatic drug;
EC 3.1.3.1 (alkaline phosphatase) inhibitor;
immunological adjuvant;
immunomodulator
fingolimod hydrochloride
Fingolimod Hydrochloride: A sphingosine-derivative and IMMUNOSUPPRESSIVE AGENT that blocks the migration and homing of LYMPHOCYTES to the CENTRAL NERVOUS SYSTEM through its action on SPHINGOSINE 1-PHOSPHATE RECEPTORS. It is used in the treatment of MULTIPLE SCLEROSIS.. fingolimod hydrochloride : The hydrochloride salt of 2-amino-2-[2-(4-octylphenyl) ethyl]-1,3-propanediol (fingolimod).		2.0810hydrochlorideimmunosuppressive agent;
prodrug;
sphingosine-1-phosphate receptor agonist
fingolimod
fingolimod : An aminodiol that consists of propane-1,3-diol having amino and 2-(4-octylphenyl)ethyl substituents at the 2-position. It is a sphingosine 1-phosphate receptor modulator used for the treatment of relapsing-remitting multiple sclerosis. A prodrug, fingolimod is phosphorylated by sphingosine kinase to active metabolite fingolimod-phosphate, a structural analogue of sphingosine 1-phosphate.		3.1810aminodiol;
primary amino compound		antineoplastic agent;
CB1 receptor antagonist;
immunosuppressive agent;
prodrug;
sphingosine-1-phosphate receptor agonist
D-fructopyranose
[no description available]		2.5120cyclic hemiketal;
D-fructose;
fructopyranose		sweetening agent
sphingosine
sphing-4-enine : A sphingenine in which the C=C double bond is located at the 4-position.. sphingenine : A 2-aminooctadecene-1,3-diol having (2S,3R)-configuration.. sphingoid : Sphinganine, its homologs and stereoisomers, and the hydroxy and unsaturated derivatives of these compounds.. 2-aminooctadec-4-ene-1,3-diol : A 2-aminooctadecene-1,3-diol having its double bond at position 4.		4.1431sphing-4-eninehuman metabolite;
mouse metabolite
sphingosine 1-phosphate
sphingosine 1-phosphate: RN given refers to (R-(R*,S*-(E)))-isomer; RN for cpd without isomeric designation not available 8/89. sphingosine 1-phosphate : A phosphosphingolipid that consists of sphingosine having a phospho group attached at position 1		3.8521sphingoid 1-phosphatemouse metabolite;
signalling molecule;
sphingosine-1-phosphate receptor agonist;
T-cell proliferation inhibitor;
vasodilator agent
1-deoxy-1-morpholinofructose
[no description available]		2.5120
ponesimod
ponesimod: structure in first source		3.1810
fty 720p
[no description available]		2.0610
siponimod
siponimod: S1P receptor modulator		3.1810
ConditionIndicatedRelationship StrengthStudiesTrials
Lymphocytopenia
[description not available]		02.0710
MS (Multiple Sclerosis)
[description not available]		02.0710
Lymphopenia
Reduction in the number of lymphocytes.		02.0710
Multiple Sclerosis
An autoimmune disorder mainly affecting young adults and characterized by destruction of myelin in the central nervous system. Pathologic findings include multiple sharply demarcated areas of demyelination throughout the white matter of the central nervous system. Clinical manifestations include visual loss, extra-ocular movement disorders, paresthesias, loss of sensation, weakness, dysarthria, spasticity, ataxia, and bladder dysfunction. The usual pattern is one of recurrent attacks followed by partial recovery (see MULTIPLE SCLEROSIS, RELAPSING-REMITTING), but acute fulminating and chronic progressive forms (see MULTIPLE SCLEROSIS, CHRONIC PROGRESSIVE) also occur. (Adams et al., Principles of Neurology, 6th ed, p903)		02.0710