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CS-0777-P

CAT: 0804-HY-14977Size: 1 EachDry Ice: NoHazardous: No
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CAT#:0804-HY-14977Size:1 Each
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Description
CS-0777-P, the phosphorylated form of CS-0777, acts as a potent and selective modulator of the S1P receptor-1 (S1P1) . It exhibits approximately 320-fold higher agonist activity for human S1P1 compared to S1P3, with an EC50 of 1.1 nM. In pharmacological studies, CS-0777-P demonstrated significant effects in vitro as an S1P1 and S1P3 agonist, leading to lowered peripheral blood lymphocyte counts and suppressive effects on experimental autoimmune encephalomyelitis (EAE) in rats. Pharmacokinetic studies in rats revealed rapid lymphocyte count reductions following oral administration, making CS-0777 a promising candidate currently undergoing clinical trials for the treatment of multiple sclerosis (MS) [1].
CAS Number
840523-39-9
UNSPSC
12352005
Target
LPL Receptor
Type
Reference compound
Related Pathways
GPCR/G Protein
Applications
COVID-19-immunoregulation
Field of Research
Inflammation/Immunology
Assay Protocol
https://www.medchemexpress.com/cs-0777-p.html
Smiles
O=P(O)(O)OC[C@](C)(N)CCC1=CC=C(C(CCCC2=CC=C(C=C2)C)=O)N1C
Molecular Formula
C21H31N2O5P
Molecular Weight
422.46
References & Citations
[1]Takahide Nishi *?, Shojiro Miyazaki ?, Toshiyasu Takemoto ?, Keisuke Suzuki ?, Yukiko Iio ?, Katsuyoshi Nakajima ?, Takashi Ohnuki ?, Yumi Kawase ?, Futoshi Nara ?, Shinichi Inaba §, Takashi Izumi §, Hiroshi Yuita , Keiko Oshima , Hiromi Doi , Ryotaku Inoue , Wataru Tomisato , Takashi Kagari , and Takaichi Shimozato * .Discovery of CS-0777: A Potent, Selective, and Orally Active S1P1 Agonist ACS Med. Chem. Lett., 2011, 2 (5), pp 368-372 DOI: 10.1021/ml100301k Publication Date (Web) : March 2, 2011
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported

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