T0070907 | CAS#313516-66-4 | PRAR Inhibitor

MedKoo Cat#: 406129 | Name: T0070907

Description:

WARNING: This product is for research use only, not for human or veterinary use.

T0070907 was identified as a potent and selective PPARgamma antagonist. With an apparent binding affinity (concentration at 50% inhibition of [(3)H]rosiglitazone binding or IC(50)) of 1 nm, T0070907 covalently modifies PPARgamma on cysteine 313 in helix 3 of human PPARgamma2. T0070907 blocked PPARgamma function in both cell-based reporter gene and adipocyte differentiation assays. T0070907 is a novel tool for the study of PPARgamma/RXRalpha heterodimer function.

Chemical Structure

T0070907

CAS#313516-66-4

Theoretical Analysis

MedKoo Cat#: 406129

Name: T0070907

CAS#: 313516-66-4

Chemical Formula: C12H8ClN3O3

Exact Mass: 277.0254

Molecular Weight: 277.66

Elemental Analysis: C, 51.91; H, 2.90; Cl, 12.77; N, 15.13; O, 17.29

Price and Availability

Size	Price	Availability
10mg	USD 90.00	Ready to ship
25mg	USD 150.00	Ready to ship
50mg	USD 250.00	Ready to ship
100mg	USD 450.00	Ready to ship
200mg	USD 750.00	Ready to ship
500mg	USD 1,650.00	Ready to ship
1g	USD 2,950.00	Ready to ship
2g	USD 5,250.00	Ready to ship

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Related CAS #

No Data

Synonym

T0070907, T-0070907, T 0070907

IUPAC/Chemical Name

2-chloro-5-nitro-N-(pyridin-4-yl)benzamide

InChi Key

FRPJSHKMZHWJBE-UHFFFAOYSA-N

InChi Code

InChI=1S/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)

SMILES Code

O=C(NC1=CC=NC=C1)C2=CC([N+]([O-])=O)=CC=C2Cl

Appearance

White to off-white solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO, not in water

Shelf Life

>5 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Certificate of Analysis

View CoA: current batch, Lot# A9T03K27

View CoA: current batch, Lot#B7B11C01

QC Data

View QC data: current batch, Lot#B7B11C01

View QC data: current batch, Lot# A9T03K27

Safety Data Sheet (SDS)

View Safety Data Sheet (SDS)

Instruction

View handling instruction

Biological target:

T0070907 is a potent PPARγ antagonist with a Ki of 1 nM.

In vitro activity:

Hence, the impact of radiation on the induction of apoptosis was evaluated in ME180 (Figure 5A and B) and HeLa cells (Figure 5C and D) treated with or without T0070907. Radiation failed to significantly increase the apoptosis in both cell lines tested; however, T0070907 promoted apoptosis in ME180 cells and the apoptosis was maximum in both HeLa and ME180 cells treated with T0070907 and radiation. T0070907 has promoted the induction of protein levels of p53 by radiation suggesting the radiosensitizing effect of T0070907 in ME180 cervical cancer cells is p53 dependent (Figure 5E). Reference: Reprod Sci. 2014 Nov; 21(11): 1352–1361. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4212328/

In vivo activity:

The treatment of mice with T007 (T0070907) decreased the levels of these osteoclastogenesis genes in a dose-dependent fashion compared to the osteoporosis animals administered with the vehicle (Fig. 10c). Moreover, T007 treatment significantly increased the mRNA and protein expression levels of OPG in OVX-induced bone loss models, while inhibiting RANKL expression and the ratio of RANKL/OPG (Fig. 10d-f). This implied that T007 prevents from OVX-induced bone loss. Reference: Cell Commun Signal. 2019; 17: 136. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6815399/

	Solvent	mg/mL	mM
Solubility
	DMSO	25.7	92.56
	DMF	10.0	36.02
	DMF:PBS (pH 7.2) (1:4)	0.2	0.72

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 277.66 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. An Z, Muthusami S, Yu JR, Park WY. T0070907, a PPAR γ inhibitor, induced G2/M arrest enhances the effect of radiation in human cervical cancer cells through mitotic catastrophe. Reprod Sci. 2014 Nov;21(11):1352-61. doi: 10.1177/1933719114525265. Epub 2014 Mar 18. PMID: 24642720; PMCID: PMC4212328. 2. Kawahara A, Haraguchi N, Tsuchiya H, Ikeda Y, Hama S, Kogure K. Peroxisome proliferator-activated receptor γ (PPARγ)-independent specific cytotoxicity against immature adipocytes induced by PPARγ antagonist T0070907. Biol Pharm Bull. 2013;36(9):1428-34. doi: 10.1248/bpb.b13-00024. PMID: 23995653. 3. Li X, Ning L, Ma J, Xie Z, Zhao X, Wang G, Wan X, Qiu P, Yao T, Wang H, Fan S, Wan S. The PPAR-γ antagonist T007 inhibits RANKL-induced osteoclastogenesis and counteracts OVX-induced bone loss in mice. Cell Commun Signal. 2019 Oct 26;17(1):136. doi: 10.1186/s12964-019-0442-3. PMID: 31655621; PMCID: PMC6815399. 4. Chen T, Zhang Y, Liu Y, Zhu D, Yu J, Li G, Sun Z, Wang W, Jiang H, Hong Z. MiR-27a promotes insulin resistance and mediates glucose metabolism by targeting PPAR-γ-mediated PI3K/AKT signaling. Aging (Albany NY). 2019 Sep 28;11(18):7510-7524. doi: 10.18632/aging.102263. Epub 2019 Sep 28. PMID: 31562809; PMCID: PMC6781997.

In vitro protocol:

In vivo protocol:

1. Li X, Ning L, Ma J, Xie Z, Zhao X, Wang G, Wan X, Qiu P, Yao T, Wang H, Fan S, Wan S. The PPAR-γ antagonist T007 inhibits RANKL-induced osteoclastogenesis and counteracts OVX-induced bone loss in mice. Cell Commun Signal. 2019 Oct 26;17(1):136. doi: 10.1186/s12964-019-0442-3. PMID: 31655621; PMCID: PMC6815399.

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PMID: 38942291. 7: Shi L, Li LJ, Sun XY, Chen YY, Luo D, He LP, Ji HJ, Gao WP, Shen HX. Er-Dong- Xiao-Ke decoction regulates lipid metabolism via PPARG-mediated UCP2/AMPK signaling to alleviate diabetic meibomian gland dysfunction. J Ethnopharmacol. 2024 Oct 28;333:118484. doi: 10.1016/j.jep.2024.118484. Epub 2024 Jun 24. PMID: 38925318. 8: van den Boom R, Vergauwen L, Knapen D. Effects of Metabolic Disruption on Lipid Metabolism and Yolk Retention in Zebrafish Embryos. Environ Toxicol Chem. 2024 Aug;43(8):1880-1893. doi: 10.1002/etc.5930. Epub 2024 Jun 11. PMID: 38860666. 9: Zhao Y, Zhao X, Feng X. Alpha-lipoic acid upregulates the PPARγ/NRF2/GPX4 signal pathway to inhibit ferroptosis in the pathogenesis of unexplained recurrent pregnancy loss. Open Med (Wars). 2024 Jun 5;19(1):20240963. doi: 10.1515/med-2024-0963. PMID: 38859880; PMCID: PMC11163161. 10: Shang J, Kojetin DJ. 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