Product Name :
YS-121
Description:
YS-121 is a dual inhibitor of Microsomal prostaglandin E2 synthase-1 (mPGES-1) . Cyclooxygenases (COX-1 and COX-2) have been involved in catalyzing the formation of prostaglandins and related eicosanoids and play an essential role in the pathogenesis of breast cancer. Actions of COX-2 are mediated by prostaglandin E2 (PGE2). Microsomal PGES-1 (mPGES-1), the inducible form of PGES, has a marked affinity for coupling with COX-2. Expression of mPGES-1 has been observed in inflammatory conditions and cancers of the stomach, colon, lung, endometrium, and skin . YS-121 inhibited the activity of mPGES-1 with an IC50 of 3.9 μM . YS-121 also inhibited the activity of 5-LO with the IC50 of 4.1 μM . YS-121 effectively inhibited PGE2 and LT synthesis in both cell free and intact cell assays. Intraperitoneal administration of YS-121 (1.5 mg/kg) reduced pleural levels of PGE2 and LTB4 while blocking exudate formation and leukocyte infiltration in carrageenan-induced rat pleurisy . YS-121 (10 μM) showed minor effects on COX-1 and COX-2, inhibiting these enzymes 24.8% and 38%, respectively .
CAS:
916482-17-2
Molecular Weight:
407.96
Formula:
C20H26ClN3O2S
Chemical Name:
2-({4-chloro-6-[(2,3-dimethylphenyl)amino]pyrimidin-2-yl}sulfanyl)octanoic acid
Smiles :
CCCCCCC(SC1N=C(Cl)C=C(NC2C=CC=C(C)C=2C)N=1)C(O)=O
InChiKey:
HVJBWTVMRIOTEL-UHFFFAOYSA-N
InChi :
InChI=1S/C20H26ClN3O2S/c1-4-5-6-7-11-16(19(25)26)27-20-23-17(21)12-18(24-20)22-15-10-8-9-13(2)14(15)3/h8-10,12,16H,4-7,11H2,1-3H3,(H,25,26)(H,22,23,24)
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
YS-121 is a dual inhibitor of Microsomal prostaglandin E2 synthase-1 (mPGES-1) .{{Rilpivirine} medchemexpress|{Rilpivirine} Anti-infection|{Rilpivirine} Technical Information|{Rilpivirine} Description|{Rilpivirine} custom synthesis|{Rilpivirine} Epigenetics} Cyclooxygenases (COX-1 and COX-2) have been involved in catalyzing the formation of prostaglandins and related eicosanoids and play an essential role in the pathogenesis of breast cancer.{{M-CSF Protein, Mouse} MedChemExpress|{M-CSF Protein, Mouse} Purity & Documentation|{M-CSF Protein, Mouse} Formula|{M-CSF Protein, Mouse} supplier|{M-CSF Protein, Mouse} Epigenetic Reader Domain} Actions of COX-2 are mediated by prostaglandin E2 (PGE2). Microsomal PGES-1 (mPGES-1), the inducible form of PGES, has a marked affinity for coupling with COX-2. Expression of mPGES-1 has been observed in inflammatory conditions and cancers of the stomach, colon, lung, endometrium, and skin . YS-121 inhibited the activity of mPGES-1 with an IC50 of 3.9 μM . YS-121 also inhibited the activity of 5-LO with the IC50 of 4.1 μM . YS-121 effectively inhibited PGE2 and LT synthesis in both cell free and intact cell assays. Intraperitoneal administration of YS-121 (1.5 mg/kg) reduced pleural levels of PGE2 and LTB4 while blocking exudate formation and leukocyte infiltration in carrageenan-induced rat pleurisy .PMID:24257686 YS-121 (10 μM) showed minor effects on COX-1 and COX-2, inhibiting these enzymes 24.8% and 38%, respectively .|Product information|CAS Number: 916482-17-2|Molecular Weight: 407.96|Formula: C20H26ClN3O2S|Chemical Name: 2-({4-chloro-6-[(2,3-dimethylphenyl)amino]pyrimidin-2-yl}sulfanyl)octanoic acid|Smiles: CCCCCCC(SC1N=C(Cl)C=C(NC2C=CC=C(C)C=2C)N=1)C(O)=O|InChiKey: HVJBWTVMRIOTEL-UHFFFAOYSA-N|InChi: InChI=1S/C20H26ClN3O2S/c1-4-5-6-7-11-16(19(25)26)27-20-23-17(21)12-18(24-20)22-15-10-8-9-13(2)14(15)3/h8-10,12,16H,4-7,11H2,1-3H3,(H,25,26)(H,22,23,24)|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|Products are for research use only. Not for human use.|