T0070907
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MedKoo CAT#: 406129

CAS#: 313516-66-4

Description: 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

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T0070907
CAS# 313516-66-4

Theoretical Analysis

MedKoo Cat#: 406129
Name: T0070907
CAS#: 313516-66-4
Chemical Formula: C12H8ClN3O3
Exact Mass: 277.02542
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 Quantity
25.0mg USD 90.0 Ready to ship
50.0mg USD 150.0 Ready to ship
100.0mg USD 250.0 Ready to ship
200.0mg USD 450.0 Ready to ship
500.0mg USD 950.0 Ready to ship
1.0g USD 1750.0 Ready to ship
2.0g USD 2850.0 Ready to ship
5.0g USD 4950.0 Ready to ship
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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

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/

Solubility Data

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

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.

Recalculate based on batch purity %
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: 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.
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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1: Zaytseva YY, Wallis NK, Southard RC, Kilgore MW. The PPARgamma antagonist T0070907 suppresses breast cancer cell proliferation and motility via both PPARgamma-dependent and -independent mechanisms. Anticancer Res. 2011 Mar;31(3):813-23. PubMed PMID: 21498701.

2: Harris G, Schaefer KL. The microtubule-targeting agent T0070907 induces proteasomal degradation of tubulin. Biochem Biophys Res Commun. 2009 Oct 16;388(2):345-9. doi: 10.1016/j.bbrc.2009.08.009. Epub 2009 Aug 6. PubMed PMID: 19665001.

3: Collin M, Murch O, Thiemermann C. Peroxisome proliferator-activated receptor-gamma antagonists GW9662 and T0070907 reduce the protective effects of lipopolysaccharide preconditioning against organ failure caused by endotoxemia. Crit Care Med. 2006 Apr;34(4):1131-8. PubMed PMID: 16484917.

4: 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. Epub 2002 Mar 4. PubMed PMID: 11877444.