Sobetirome is a member of a class of compounds known as selective thyromimetics.
Sobetirome 细胞实验
Cell Line
Concentration
Treated Time
Description
References
A549 and MLE12 cell lines
10-20 nM
36 hours
To assess the effect of TRβ activation on AT1 cell marker expression, GC-1 significantly increased PDPN and HOPX expression at 10-20 nM
Nat Commun. 2024 Oct 7;15(1):8672.
Oligodendrocyte precursor cells (OPCs)
10 μM
7 days
Sobetirome treatment significantly reduced the number of oligodendrocyte precursor cells (PDGFRα+/OLIG2+) and increased the number of oligodendrocytes (MBP+/OLIG2+), similar to Tcf4+/+ controls.
Brain. 2023 Aug 1;146(8):3331-3346.
Human primary microglia
1 μM
24 h
upregulate TREM2 in human primary microglia
Cell Chem Biol. 2022 Feb 17;29(2):239-248.e4.
Mouse primary microglia cells
1 μM
24 h
upregulate Trem2 in mouse primary microglia, and alter the transcript levels of TREM2 pathway-connected genes by upregulating Cd68 and downregulating Il1b
Cell Chem Biol. 2022 Feb 17;29(2):239-248.e4.
Rat oligodendrocyte progenitor cells
50 nM
24 hours
upregulated genes involved in myelination (Mbp, Klf9, and Hr)
JCI Insight. 2019 Apr 18;4(8):e126329.
Rat oligodendrocyte progenitor cells
50 nM
96 hours
promoted differentiation of OPCs into mature oligodendrocytes
JCI Insight. 2019 Apr 18;4(8):e126329.
Sobetirome 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
Bleomycin-induced pulmonary fibrosis model
Oral
5 mg/kg
Administered at days 10, 12, 14, 16 and 18 following bleomycin administration and mice were sacrificed on day 21
To evaluate the therapeutic effect of Sobetirome on pulmonary fibrosis, results showed Sobetirome significantly reduced the degree of pulmonary fibrosis.
Nat Med. 2018 Jan;24(1):39-49.
Mice
Met-β-catenin HCC model
Oral
5 mg/kg
Daily for 5 weeks
To evaluate the therapeutic effect of mTORC1 inhibition on β-catenin-mutated HCC. Results showed that Rapamycin alone or in combination with GC1 significantly reduced tumor burden, with the combination therapy showing more profound effects.
Cell Metab. 2019 May 7;29(5):1135-1150.e6.
Mice
Bleomycin-induced pulmonary fibrosis model
Intraperitoneal injection
30 μg/kg
Daily from day 11 to day 20
To evaluate the anti-fibrotic effects of GC-1, GC-1 significantly reduced fibrosis markers and improved lung function
Nat Commun. 2024 Oct 7;15(1):8672.
Mice
ApoE-deficient mouse model
Intraperitoneal injection
1 mg/kg
21 consecutive days
To evaluate the safety and efficacy of GC-1 as a hepatic mitogen, results showed GC-1 significantly promoted hepatocyte proliferation and reduced serum cholesterol levels
J Hepatol. 2019 Jun;70(6):1170-1179
Mice
Hypothyroid mouse model
Intraperitoneal injection
3.6, 7.2, 14.4 ng/g/day
Daily for 10 days
To evaluate the effect of GC-1 on the thermogenic response of brown adipose tissue (BAT) in hypothyroid mice. Results showed that GC-1 treatment failed to restore the thermogenic response of BAT to norepinephrine (NE).
J Clin Invest. 2001 Jul;108(1):97-105
Mice
Normal mice and hypercholesterolemic mice model
Intraperitoneal injection
5.4, 24, 48, and 97 nmol/kg/day
Once daily for 8 days
To investigate the effects of GC-1 on cholesterol and triglyceride metabolism. GC-1 reduced serum cholesterol and triglyceride levels, increased hepatic HDL receptor SR-BI expression, and stimulated bile acid synthesis and excretion.
Proc Natl Acad Sci U S A. 2005 Jul 19;102(29):10297-302
Male mice
C57BL/6J
Subcutaneous injection
0.1 μg/g
Twice daily for 3.5 days
To evaluate the effect of Sobetirome on exploratory behavior in male mice. Results showed that Sobetirome did not significantly alter the duration mice spent in the light-exposed area in the light-dark preference assay.
Cell. 2024 Oct 3;187(20):5679-5697.e23
Mice
Pitt–Hopkins syndrome mouse model
Intraperitoneal injection
1.0 mg/kg/day
Once daily for 14 days
Sob-AM2 treatment significantly increased the number of oligodendrocytes (CC1+/OLIG2+) and decreased the number of oligodendrocyte precursor cells (PDGFRα+/OLIG2+), similar to Tcf4+/+ controls. Additionally, Sob-AM2 treatment significantly improved hyperlocomotion and anxiety behaviors in the mice.
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