CS-0777-P - CAS 840523-39-9
Catalog number: 840523-39-9
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
Molecular Weight:
Sphingosine 1 Phosphate Receptor
CS-0777 is a selective sphingosine 1-phosphate receptor modulator agonist. It is in clinical trials for the treatment of multiple sclerosis, but no recent development was reported.
CS-0777; CS0777; CS 0777. 1-(5-((3R)-3-amino-3-methyl-4-(phosphonooxy)butyl)-1-methyl-1H-pyrrol-2-yl)-4-(4-methylphenyl)-1-Butanone
Soluble in DMSO
-20℃ Freezer
Multiple sclerosis
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Canonical SMILES:
Current Developer:
Originator Daiichi Sankyo Company
1.Discovery of CS-0777: A Potent, Selective, and Orally Active S1P1 Agonist.
Nishi T1, Miyazaki S1, Takemoto T1, Suzuki K1, Iio Y1, Nakajima K1, Ohnuki T1, Kawase Y1, Nara F1, Inaba S1, Izumi T1, Yuita H2, Oshima K2, Doi H2, Inoue R2, Tomisato W2, Kagari T2, Shimozato T2. ACS Med Chem Lett. 2011 Mar 2;2(5):368-72. doi: 10.1021/ml100301k. eCollection 2011.
CS-0777 (3) is phosphorylated in vivo, and the phosphate of CS-0777 (CS-0777-P) (4) acts as a selective S1P receptor-1 (S1P1) modulator. We report herein the synthesis of CS-0777 and CS-0777-P, pharmacological effects such as S1P1 and S1P3 agonist activity in vitro, peripheral blood lymphocyte lowering effects and the suppressive effect on experimental autoimmune encephalomyelitis (EAE), and also the pharmacokinetics in rats. CS-0777-P had ∼320-fold greater agonist activity for human S1P1 (EC50; 1.1 nM) relative to S1P3 (EC50; 350 nM). Following administration of single oral doses of 0.1 and 1 mg/kg of CS-0777 in rats, lymphocyte counts decreased significantly, with a nadir at 12 h postdose and recovery to vehicle control levels by 5 days postdose. In the EAE model compared to the vehicle-treated group, significant decreases in the cumulative EAE scores were observed for the 0.1 and 1 mg/kg CS-0777 groups in rats. CS-0777 is currently in clinical trials for the treatment of multiple sclerosis (MS).
2.Identification of a metabolizing enzyme in human kidney by proteomic correlation profiling.
Sakurai H1, Kubota K, Inaba S, Takanaka K, Shinagawa A. Mol Cell Proteomics. 2013 Aug;12(8):2313-23. doi: 10.1074/mcp.M112.023853. Epub 2013 May 14.
Molecular identification of endogenous enzymes and biologically active substances from complex biological sources remains a challenging task, and although traditional biochemical purification is sometimes regarded as outdated, it remains one of the most powerful methodologies for this purpose. While biochemical purification usually requires large amounts of starting material and many separation steps, we developed an advanced method named "proteomic correlation profiling" in our previous study. In proteomic correlation profiling, we first fractionated biological material by column chromatography, and then calculated each protein's correlation coefficient between the enzyme activity profile and protein abundance profile determined by proteomics technology toward fractions. Thereafter, we could choose possible candidates for the enzyme among proteins with a high correlation value by domain predictions using informatics tools. Ultimately, this streamlined procedure requires fewer purification steps and reduces starting materials dramatically due to low required purity compared with conventional approaches.
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