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Cat. No.: HY-14977

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CS-0777-P

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).

For research use only. We do not sell to patients.

CAS No.: 840523-39-9
Formula: C₂₁H₃₁N₂O₅P
Molecular Weight:422.46

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (266 KB)

CS-0777-P Chemical Structure

CAS No.: 840523-39-9

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- Cellular Effect
Chemical Information
Protocols (1)
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

All LPL Receptor Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO-K1	EC₅₀	1.1 nM Compound: 4, CS-0777-P	Agonist activity at human S1P1 receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay Agonist activity at human S1P1 receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay	[PMID: 24900318]
CHO-K1	EC₅₀	1.1 nM Compound: 4, CS-0777-P	Agonist activity at human S1P1 receptor expressed in CHO-K1 cells assessed as induction of GTPgammaS binding Agonist activity at human S1P1 receptor expressed in CHO-K1 cells assessed as induction of GTPgammaS binding	[PMID: 22405291]
CHO-K1	EC₅₀	1.8 nM Compound: 4, CS-0777-P	Agonist activity at rat S1P1 receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay Agonist activity at rat S1P1 receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay	[PMID: 24900318]
CHO-K1	EC₅₀	1.8 nM Compound: 4, CS-0777-P	Agonist activity at rat S1P1 receptor expressed in CHO-K1 cells assessed as induction of GTPgammaS binding Agonist activity at rat S1P1 receptor expressed in CHO-K1 cells assessed as induction of GTPgammaS binding	[PMID: 22405291]
CHO-K1	EC₅₀	200 nM Compound: 4, CS-0777-P	Agonist activity at rat S1P3R expressed in CHO-K1 cells by [35S]GTPgammaS binding assay Agonist activity at rat S1P3R expressed in CHO-K1 cells by [35S]GTPgammaS binding assay	[PMID: 24900318]
CHO-K1	EC₅₀	200 nM Compound: 4, CS-0777-P	Agonist activity at rat S1P3 receptor expressed in CHO-K1 cells assessed as induction of GTPgammaS binding Agonist activity at rat S1P3 receptor expressed in CHO-K1 cells assessed as induction of GTPgammaS binding	[PMID: 22405291]
CHO-K1	EC₅₀	350 nM Compound: 4, CS-0777-P	Agonist activity at human S1P3R expressed in CHO-K1 cells by [35S]GTPgammaS binding assay Agonist activity at human S1P3R expressed in CHO-K1 cells by [35S]GTPgammaS binding assay	[PMID: 24900318]
CHO-K1	EC₅₀	350 nM Compound: 4, CS-0777-P	Agonist activity at human S1P3 receptor expressed in CHO-K1 cells assessed as induction of GTPgammaS binding Agonist activity at human S1P3 receptor expressed in CHO-K1 cells assessed as induction of GTPgammaS binding	[PMID: 22405291]

Chemical Information

CAS No. 840523-39-9
Molecular Weight 422.46
Formula C₂₁H₃₁N₂O₅P
SMILES

O=P(O)(O)OC[C@](C)(N)CCC1=CC=C(C(CCCC2=CC=C(C=C2)C)=O)N1C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Protocols

All Animals and Diseases

How to Select the Route of Administration for Mammals
Route-of-administration selection in mammals is a pharmacokinetic, pharmacodynamic, formulation, animal-welfare, and translational decision, not a default technical choice. The selected route should match the study goal: intravenous dosing is most useful when complete systemic exposure and rapid onset are required, oral dosing is most translational for orally intended medicines but is affected by absorption and first-pass metabolism, subcutaneous or intramuscular dosing can provide slower systemic exposure, and intraperitoneal dosing can be useful in rodent proof-of-concept studies but may have limited clinical translation. Published route-comparison studies show that the same compound can produce different exposure, onset, bioavailability, tissue distribution, and tolerability depending on route; therefore, route choice should be supported by pilot pharmacokinetic or pharmacodynamic evidence when the literature is insufficient. Unresolved questions include how to standardize route sel

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (266 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[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

Calculators

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Dilution Calculator

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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