| Cat. No. |
Product Name |
CAS No. |
Information |
| H9362 |
Zaloglanstat
|
1513852-12-4 |
Zaloglanstat is a non-opioid, potent, selective and orally bioavailable inhibitor of microsomal prostaglandin E synthase-1 (mPGES-1) currently in development for osteoarthritic pain. |
| H4060 |
Pizuglanstat
|
1244967-98-3 |
Pizuglanstat is a potent, selective prostaglandin D synthase inhibitor with IC50 value of 58nM. |
| H4059 |
PF-9184
|
1221971-47-6 |
PF-9184 is a potent, selective mPGES-1 (microsomal prostaglandin E synthase-1) inhibitor with IC50 of 16.5 nM; shows no effect against COX-1 and COX-2 (>6,500-fold selectivity); inhibits PGE2 synthesis in serum-free cell and human whole blood cultures with IC50 of 0.5-5 uM, while sparing the synthesis of PGF(1alpha)) and PGF(2alpha). |
| H4058 |
mPGES1-IN-17d
|
1469976-70-2 |
mPGES1-IN-17d is a potent, selective mPGES-1 inhibitor with enzyme IC50 of 8 nM, A549 cell IC50 of 16.24 nM, human whole blood IC50 of 249.9 nM; displays excellent in vitro selectivity over mPGES-2, cPGES, COX1/2, other prostanoid synthases, favorable hERG and CEREP panel profile; shows good efficacy in LPS-induced thermal hyperalgesia pain model; demonstrates good oral pharmacokinetic profiles and good CNS B/P ratio in rat and guinea pig. |
| H4057 |
mPGES1-IN-16
|
1915003-93-8 |
mPGES1-IN-16 is a potent and selective mPGES-1 inhibitor with IC50 of 1 nM; displays no activity against a panel of 35 receptors, ion channels, and hERG; shows IC50/IC80 of 6 nM/24 nM for inhibition of PGE2 formation in vitro in LPS-stimulated human whole blood (HWB); orally bioavailable in vivo. |
| H4056 |
MF63
|
892549-43-8 |
MF63 is a potent, selective, and orally active mPGES-1 inhibitor with IC50 of 1.3 nM for human mPGES-1 enzyme, >1000-fold selectivity over other prostanoid synthases; strongly inhibits guinea pig mPGES-1 (IC50= 0.9 nM) but not the mouse or rat enzyme; selectively suppresses the synthesis of PGE(2), but not other prostaglandins inhibitable by NSAIDs, yet retains NSAID-like efficacy at inhibiting LPS-induced pyresis, hyperalgesia, and iodoacetate-induced osteoarthritic pain, relieves pyresis and pain in preclinical models of inflammation. |
| H4055 |
LY3031207
|
1381846-21-4 |
A novel potent (IC50=910 ng/mL), highly selective microsomal prostaglandin E synthase 1 inhibitor (mPGES-1) for treatment of undisclosed indications. |
| H4054 |
hPGDS-IN-1
|
1234708-04-3 |
hPGDS-IN-1 is a potent, selective hPGDS inhibitor with IC50 of 12 nM in FP or EIA assays. |
| H4053 |
HPGDS inhibitor 1
|
1033836-12-2 |
A potent, selective, oral hematopoietic prostaglandin D synthase (HPGDS) inhibitor with enzyme IC50 of 0.6 nM; does not inhibit human L-PGDS, mPGES, COX-1, COX-2, or 5 LOX (IC50>10 uM); reduces the antigen-induced response in vivo. |
| H4052 |
Crisdesalazine
|
927685-43-6 |
Crisdesalazine (AAD-2004, AAD2004) is a derivative of aspirin that inhibits microsomal PGE(2) synthase-1 (mPGES-1) activity in response to both LPS-treated BV2 cell with IC50 of 230 nM and recombinant human mPGES-1 protein with IC50 of 249 nM in vitro; blocked free radical production, PGE(2) formation, and microglial activation in the spinal cords in superoxide dismutase 1(G93A) transgenic mouse model of ALS, reduced autophagosome formation, axonopathy, and motor neuron degeneration, improving motor function and increasing life span, which is superior to riluzole or ibuprofen. |
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