Description
C 87 is a novel small-molecule TNFα inhibitor; potently inhibits TNFα-induced cytotoxicity with an IC50 of 8.73 μM.
Product information
CAS Number: 332420-90-3
Molecular Weight: 502.93
Formula: C24H15ClN6O3S
Chemical Name: (4E)-4-[2-(4-chloro-3-nitrophenyl)hydrazin-1-ylidene]-3-phenyl-1-(4-phenyl-1,3-thiazol-2-yl)-4,5-dihydro-1H-pyrazol-5-one
Smiles: [O-][N+](=O)C1=CC(=CC=C1Cl)N/N=C1\C(=NN(C2=NC(=CS2)C2C=CC=CC=2)C\1=O)C1C=CC=CC=1
InChiKey: VELQTEBILFDDQX-XAYXJRQQSA-N
InChi: InChI=1S/C24H15ClN6O3S/c25-18-12-11-17(13-20(18)31(33)34)27-28-22-21(16-9-5-2-6-10-16)29-30(23(22)32)24-26-19(14-35-24)15-7-3-1-4-8-15/h1-14,27H/b28-22+
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 9.33 mg/mL (18.55 mM; Need ultrasonic and warming).
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
How to use
In Vitro:
C 87 (C87) directly binds to TNFα, potently inhibits TNFα-induced cytotoxicity (IC50=8.73 μM) and effectively blocks TNFα-triggered signaling activities. C 87 exhibits good solubility and consistent dose-dependent functions in vitro. C 87 completely blocks TNFα-induced activation of caspase-3 and caspase-8. The activity of c-Jun N-terminal kinase (JNK) is significantly reduced by C 87 in L929 cells. C 87 also prevents the degradation of IκBα in cells treated with TNFα. C 87 potently blocks multiple signaling transduction pathways and downstream target gene activation triggered by TNFα.
In Vivo:
C 87 (C87) attenuates TNFα-induced inflammation, thereby markedly reducing injuries to the liver and improving animal survival. C 87 injection delays the incidence of death and increases the survival rate by two folds compared with the vehicle control. The level of alanine transaminase and aspartate transaminase is consistently reduced in mice with C 87 treatment.
Products are for research use only. Not for human use.
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