CAY10415

Modify Date: 2024-01-02 19:51:51

CAY10415 Structure
CAY10415 structure
Common Name CAY10415
CAS Number 146062-49-9 Molecular Weight 370.422
Density 1.3±0.1 g/cm3 Boiling Point 623.8±55.0 °C at 760 mmHg
Molecular Formula C19H18N2O4S Melting Point N/A
MSDS N/A Flash Point 331.1±31.5 °C

 Use of CAY10415


MSDC 0160 act as an insulin sensitizer and a modulator of mitochondrial pyruvate carrier (MPC), a key controller of cellular metabolism that influences mTOR (mammalian target of rapamycin) activation. In Vitro: MSDC-0160 acts as insulin sensitizers without activating PPARγ. MSDC-0160 (10 μM) pretreatment (1 hour) prevents the MPP+ (10 μM)-induced loss of both tyrosine hydroxylase (TH)-immunoreactive differentiated Lund human mesencephalic (LUHMES) cells. MSDC-0160 protects only TH-immunoreactive neurons, which is consistent with the selected concentration of MPP+ primarily being toxic to dopamine neurons. In addition, MSDC-0160 counteracts both MPP+-induced shortening of neurite length and reduces branching in both LUHMES cells. MSDC-0160 (10 or 100 μM) prevents the loss of GFP-fluorescent dopaminergic neurons induced by MPP+ (0.75 mM) in nematodes (P =0.0001), whereas 1 μM MSDC-0160 does not. MSDC-0160 (10 μM) blocks LPS-induced increases in iNOS expression in BV2 cell lysates. MSDC-0160 is mainly to prevent the activation of mTOR produced by the metabolic changes rather than to directly inhibit mTOR kinase activity[1]. PPARγ sparing TZD, MSDC-0160, reduces resistance in the insulin/IGF-1 signaling pathway and restores IGF-1-induced akt phosphorylation. MSDC-0160 (10-20 μM) in conbination with IGF-1 prevents the loss of insulin content and maintains insulin secretion. Treatment of human islets with MSDC-0160 (1-50 μM) activates AMPK and downregulates mTOR. MSDC-0160 (1-50 μM) treatment maintains human β-cell phenotype[2]. The combined treatment with PPARγ ligands (MSDC 0160) and γ-radiation synergistically induces caspase-dependent apoptotic cell death, and PPARγ ligands significantly enhance the γ-radiation-induced DNA damage response in a PPARγ-independent manner[3].In Vivo: MSDC-0160 (30 mg/kg per day, p.o.) can be observed in plasma and brain tissue of the mice, proving MSDC-0160 can effectively enter the brain. MSDC-0160 (30 mg/kg per day, p.o.) treatment 3 days after MPTP injection, improves motor behavior, protects nigrostriatal neurons, and suppresses disease progression in the MPTP mouse model of Parkinson’s disease (PD), improves motor behavior in the open-field and rotarod tests in the En1+/- genetic mouse model of PD, and prevents dopaminergic neurodegeneration in the En1+/- genetic mouse model of PD. MSDC-0160 (30 mg/kg, p.o.) modulates mTOR signaling in C. elegans and the MPTP mouse model of PD. MSDC-0160 down-regulates mTOR signaling and restores autophagy in the En1+/- genetic mouse model of PD[1].

 Names

Name 5-[[4-[2-(5-ethylpyridin-2-yl)-2-oxoethoxy]phenyl]methyl]-1,3-thiazolidine-2,4-dione
Synonym More Synonyms

 CAY10415 Biological Activity

Description MSDC 0160 act as an insulin sensitizer and a modulator of mitochondrial pyruvate carrier (MPC), a key controller of cellular metabolism that influences mTOR (mammalian target of rapamycin) activation. In Vitro: MSDC-0160 acts as insulin sensitizers without activating PPARγ. MSDC-0160 (10 μM) pretreatment (1 hour) prevents the MPP+ (10 μM)-induced loss of both tyrosine hydroxylase (TH)-immunoreactive differentiated Lund human mesencephalic (LUHMES) cells. MSDC-0160 protects only TH-immunoreactive neurons, which is consistent with the selected concentration of MPP+ primarily being toxic to dopamine neurons. In addition, MSDC-0160 counteracts both MPP+-induced shortening of neurite length and reduces branching in both LUHMES cells. MSDC-0160 (10 or 100 μM) prevents the loss of GFP-fluorescent dopaminergic neurons induced by MPP+ (0.75 mM) in nematodes (P =0.0001), whereas 1 μM MSDC-0160 does not. MSDC-0160 (10 μM) blocks LPS-induced increases in iNOS expression in BV2 cell lysates. MSDC-0160 is mainly to prevent the activation of mTOR produced by the metabolic changes rather than to directly inhibit mTOR kinase activity[1]. PPARγ sparing TZD, MSDC-0160, reduces resistance in the insulin/IGF-1 signaling pathway and restores IGF-1-induced akt phosphorylation. MSDC-0160 (10-20 μM) in conbination with IGF-1 prevents the loss of insulin content and maintains insulin secretion. Treatment of human islets with MSDC-0160 (1-50 μM) activates AMPK and downregulates mTOR. MSDC-0160 (1-50 μM) treatment maintains human β-cell phenotype[2]. The combined treatment with PPARγ ligands (MSDC 0160) and γ-radiation synergistically induces caspase-dependent apoptotic cell death, and PPARγ ligands significantly enhance the γ-radiation-induced DNA damage response in a PPARγ-independent manner[3].In Vivo: MSDC-0160 (30 mg/kg per day, p.o.) can be observed in plasma and brain tissue of the mice, proving MSDC-0160 can effectively enter the brain. MSDC-0160 (30 mg/kg per day, p.o.) treatment 3 days after MPTP injection, improves motor behavior, protects nigrostriatal neurons, and suppresses disease progression in the MPTP mouse model of Parkinson’s disease (PD), improves motor behavior in the open-field and rotarod tests in the En1+/- genetic mouse model of PD, and prevents dopaminergic neurodegeneration in the En1+/- genetic mouse model of PD. MSDC-0160 (30 mg/kg, p.o.) modulates mTOR signaling in C. elegans and the MPTP mouse model of PD. MSDC-0160 down-regulates mTOR signaling and restores autophagy in the En1+/- genetic mouse model of PD[1].
Related Catalog
References

[1]. Rohatgi N, et al. Novel insulin sensitizer modulates nutrient sensing pathways and maintains β-cell phenotype in human islets. PLoS One. 2013 May 1;8(5):e62012.

[2]. Ghosh A, et al. Mitochondrial pyruvate carrier regulates autophagy, inflammation, and neurodegeneration inexperimental models of Parkinson's disease. Sci Transl Med. 2016 Dec 7;8(368):368ra174.

 Chemical & Physical Properties

Density 1.3±0.1 g/cm3
Boiling Point 623.8±55.0 °C at 760 mmHg
Molecular Formula C19H18N2O4S
Molecular Weight 370.422
Flash Point 331.1±31.5 °C
Exact Mass 370.098724
PSA 114.15000
LogP 2.84
Vapour Pressure 0.0±1.8 mmHg at 25°C
Index of Refraction 1.619
Storage condition -20℃

 Synonyms

Mitoglitazone
5-{4-[2-(5-Ethyl-2-pyridinyl)-2-oxoethoxy]benzyl}-1,3-thiazolidine-2,4-dione
MSDC-0160
2,4-THIAZOLIDINEDIONE,5-[[4-[2-(5-ETHYL-2-PYRIDINYL)-2-OXOETHOXY]PHENYL]METHYL]
2,4-Thiazolidinedione, 5-[[4-[2-(5-ethyl-2-pyridinyl)-2-oxoethoxy]phenyl]methyl]-
5-{4-[2-(5-ethylpyridin-2-yl)-2-oxoethoxy]benzyl}-1,3-thiazolidine-2,4-dione
CAY10415
MSDC 0160
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