PZ0196
Tenidap
≥97% (HPLC)
别名:
(3Z)-5-Chloro-2,3-dihydro-3-(hydroxy-2-thienylmethylene)-2-oxo-1H-indole-1-carboxamide, CP 66248
产品名称
Tenidap, ≥97% (HPLC)
form
powder
SMILES string
[s]1c(ccc1)C(=O)c2c3c([n](c2O)C(=O)N)ccc(c3)Cl
InChI
1S/C14H9ClN2O3S/c15-7-3-4-9-8(6-7)11(13(19)17(9)14(16)20)12(18)10-2-1-5-21-10/h1-6,19H,(H2,16,20)
InChI key
IZSFDUMVCVVWKW-UHFFFAOYSA-N
assay
≥97% (HPLC)
color
faintly yellow to dark yellow
solubility
DMSO: 1 mg/mL, clear (warmed)
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
Tenidap is an anti-inflammatory and anti-rheumatic with a variety of activities. Tenidap preferentially inhibits COX-1 with an IC50 value of 30 nM, and also has some lesser inhibitory activity towards COX-2 and 5-lipoxygenase (IC50 values are 1.2 and > 30 μM for COX-2 and 5-lipoxygenase respectively). Tenidap is also a cytokine modulator, an opener of inward rectifying hKIR2.3 channels (EC50 = 402 nM) and has been shown to modulate cytoplasmic pH and inhibit anion transport in vitro.
Tenidap is an anti-inflammatory, anti-rheumatic and cytokine modulator.
signalword
Warning
hcodes
Hazard Classifications
Acute Tox. 4 Oral
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
X Ayral et al.
Osteoarthritis and cartilage, 11(3), 198-207 (2003-03-08)
To test the hypothesis that tenidap has a structure-modifying effect in human knee osteoarthritis. multicenter, prospective, randomized, double blind, 1 year duration. primary painful knee osteoarthritis (ACR criteria) of the medial tibiofemoral compartment, medial joint space width > or =2mm
Tenidap.
R Madhok
Lancet (London, England), 346(8973), 481-485 (1995-08-19)
Hiroko Matsumoto et al.
The Journal of pharmacology and experimental therapeutics, 300(2), 668-672 (2002-01-24)
The effect of tenidap [(+/-)-5-chloro-2,3-dihydro-3-(hydroxy-2-thienylmethylene)-2-oxo-1H-indole-1-carboxamide], a new anti-inflammatory agent, was investigated on DNA synthesis by means of [(3)H]thymidine incorporation, collagen synthesis by means of [(3)H]proline incorporation, cell proliferation, and intracellular pH in nicardipine-reactive human gingival fibroblasts. Tenidap significantly inhibited [(3)H]thymidine
P Lavigne et al.
Osteoarthritis and cartilage, 10(11), 898-904 (2002-11-19)
Introduction and goal Proinflammatory cytokines and prostaglandin E(2) (PGE(2)) play an important role in the pathophysiology of osteolysis and implant loosening. The aim of this study was to evaluate the role of pharmacological agents in the inhibition of Interleukin-1 (IL-1)
Samuel Parry et al.
The Journal of general virology, 87(Pt 8), 2269-2278 (2006-07-19)
The human placenta is relatively resistant to Human immunodeficiency virus 1 (HIV-1), but obstetric complications associated with inflammatory processes, including chorioamnionitis and spontaneous preterm delivery, are associated with increased rates of vertical transmission. It was hypothesized that the pro-inflammatory mediator
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