313516-66-4 Usage
Description
T0070907 is a cell-permeable chloro-nitro-benzamido compound that acts as a potent, specific, irreversible, and high-affinity antagonist of peroxisome proliferator-activated receptor gamma (PPARγ) with a Ki of 1 nM. It is a promising pharmaceutical candidate with antimicrotubule, antitumor, and radiosensitizing properties. T0070907 decreases tubulin protein levels, leading to cell cycle arrest, apoptosis, and reduced metastasis of colorectal carcinoma cells. It is used as a therapeutic target in breast cancer and stimulates proteasome-dependent degradation of tubulin. T0070907 covalently binds to Cys313 of PPARγ, inducing conformational changes that block the recruitment of transcriptional cofactors to the PPARγ/RXR heterodimer.
Uses
Used in Pharmaceutical Industry:
T0070907 is used as an antagonist for peroxisome proliferator-activated receptor gamma (PPARγ) for its high-affinity binding inhibition of rosiglitazone, a reference thiazolidinedione (TZD). It is employed in the development of drugs targeting PPARγ-related diseases.
Used in Cancer Research:
T0070907 is used as a therapeutic target in breast cancer due to its ability to stimulate proteasome-dependent degradation of tubulin, leading to cell cycle arrest, apoptosis, and reduced metastasis of cancer cells.
Used in Inflammation and Immunology Research:
T0070907 has been used to reduce PPARγ expression in lipopolysaccharide (LPS)-induced leukemia RAW264.7 cell line, helping researchers evaluate the involvement of compounds like wogonin in alleviating ethanol-induced inflammation.
Used in Drug Delivery Systems:
T0070907 can be incorporated into drug delivery systems to improve its bioavailability and therapeutic outcomes in various applications, including cancer treatment and inflammation management.
Chemical Properties:
T0070907 is an off-white solid, which is important for its formulation and stability in pharmaceutical applications.
Biological Activity
Potent and selective PPAR γ antagonist (IC 50 = 1 nM). Displays > 800-fold selectivity for PPAR γ over PPAR α and PPAR δ . In vitro, blocks transcriptional activity of PPAR γ and inhibits rosiglitazone-induced adipogenesis.
Biochem/physiol Actions
T0070907 is very similar in structure and activity to the PPAR-γ antagonist GW9662. T0070907 is more potent and has higher selectivity for PPAR-γ over all other subtypes (about 800-fold) whereas GW9662 has been reported to have some PPAR-α agonist activity.
references
[1] lee g, elwood f, mcnally j, weiszmann j, lindstrom m, amaral k, nakamura m, miao s, cao p, learned rm, chen jl, li y. t0070907, a selective ligand for peroxisome proliferator-activated receptor gamma, functions as an antagonist of biochemical and cellular activities. j biol chem. 2002 may 31;277(22):19649-57.
Check Digit Verification of cas no
The CAS Registry Mumber 313516-66-4 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 3,1,3,5,1 and 6 respectively; the second part has 2 digits, 6 and 6 respectively.
Calculate Digit Verification of CAS Registry Number 313516-66:
(8*3)+(7*1)+(6*3)+(5*5)+(4*1)+(3*6)+(2*6)+(1*6)=114
114 % 10 = 4
So 313516-66-4 is a valid CAS Registry Number.
InChI:InChI=1/C12H8ClN3O3/c13-11-2-1-9(16(18)19)7-10(11)12(17)15-8-3-5-14-6-4-8/h1-7H,(H,14,15,17)
313516-66-4Relevant articles and documents
MOLECULES HAVING PESTICIDAL UTILITY, AND INTERMEDIATES, COMPOSITIONS, AND PROCESSES, RELATED THERETO
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Page/Page column 160, (2016/10/31)
This disclosure relates to the field of moiecuies having pesticida i utility against pests in Phyla Arthropoda, Moliusca, and hJematoda, processes to produce such moiecuies, intermediates used In such processes, pesticidai compositions containing such molecules, and processes of using such pesticidai compositions against such pests. These pesticidai compositions may be used, for example, as acaricldes, insecticides, miticides, moilusclcides, and nematicides. This document discloses moiecuies having the following formula ("Formula One").
