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NSC 90469 (3,5-Diiodo-L-thyronine) is an orally active thyroid hormone derivative. NSC 90469 inhibits JNK phosphorylation and NF-κB acetylation, blocks SIRT1 protein expression, induces elevated PGC-1α levels, and stimulates COX activity. NSC 90469 enhances UCP1-mediated thermogenesis, increases hepatic Dio1 activity, inhibits TSH levels and hypothalamic-pituitary-thyroid axis function, enhances lipid metabolism, and regulates energy metabolism via the mitochondrial pathway. NSC 90469 prevents blood glucose reduction, reduces urinary albumin excretion, inhibits renal matrix expansion, decreases TGF-β1 expression, and reduces renal fibronectin and type Ⅳ collagen deposition. NSC 90469 also increases energy expenditure and prevents diet-induced overweight. NSC 90469 can be used in studies related to diabetic nephropathy, hypothyroidism, non-alcoholic fatty liver disease, and diet-induced obesity.
For research use only. We do not sell to patients.
NSC 90469 (3,5-Diiodo-L-thyronine) is an orally active thyroid hormone derivative. NSC 90469 inhibits JNK phosphorylation and NF-κB acetylation, blocks SIRT1 protein expression, induces elevated PGC-1α levels, and stimulates COX activity. NSC 90469 enhances UCP1-mediated thermogenesis, increases hepatic Dio1 activity, inhibits TSH levels and hypothalamic-pituitary-thyroid axis function, enhances lipid metabolism, and regulates energy metabolism via the mitochondrial pathway. NSC 90469 prevents blood glucose reduction, reduces urinary albumin excretion, inhibits renal matrix expansion, decreases TGF-β1 expression, and reduces renal fibronectin and type Ⅳ collagen deposition. NSC 90469 also increases energy expenditure and prevents diet-induced overweight. NSC 90469 can be used in studies related to diabetic nephropathy, hypothyroidism, non-alcoholic fatty liver disease, and diet-induced obesity[1][2][3][4][5].
NSC 90469 (T2) (100 μM; 1-24 h) attenuates high glucose-induced profibrotic changes, restores the expression and activity of SIRT1, and inhibits the acetylation of NF-κB and phosphorylation of JNK in rat glomerular mesangial cells[1]. NSC 90469 (10-12-10-6 M; 30 min) dose-dependently stimulates cytochrome oxidase activity in brown adipose tissue homogenates from hypothyroid rats, with a half-maximal effective concentration of 10-11 M and a maximal activating concentration of 10-8 M[2]. NSC 90469 (0.1 nM-10000 nM; 24 h) exhibits differential thyroid-mimetic activity in GH3 cells, stimulates GH mRNA expression, and downregulates TRβ2 mRNA expression[3]. NSC 90469 (10-5 M) reduces lipid overload in primary rat hepatocytes exposed to Oleic acid (HY-N1446)/Palmitic acid (HY-N0830) by recruiting adipose triglyceride lipase (ATGL), stimulating mitochondrial function, and regulating the expression of lipid-related proteins[4]. NSC 90469 (10-7-10-5 M; 24 h) reduces lipid accumulation and stimulates mitochondrial uncoupling in FAO rat hepatocellular carcinoma cells exposed to Oleic acid (HY-N1446)/Palmitic acid (HY-N0830) via a non-receptor-mediated mechanism[4]. NSC 90469 inhibits lipid synthesis in HepG2 cells by activating multiple kinase pathways to block the proteolytic cleavage of SREBP-1[4]. NSC 90469 rapidly modulates intracellular Ca2+ and NO levels in pituitary GH3 cells, and activates the mitochondrial Na+/Ca2+ exchanger through the interaction between the plasma membrane and mitochondria[4]. NSC 90469 (0.3 nM; 5 min) stimulates mitochondrial respiration in isolated liver and muscle of goldfish Carassius auratus[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
NSC 90469 Related Antibodies
In Vivo
NSC 90469 (0.25 mg/kg, i.p., once daily for 12 weeks) ameliorates streptozotocin (HY-13753)-induced diabetic nephropathy in male Sprague-Dawley rats, reduces blood glucose to 6.3 mM, decreases the urinary albumin/creatinine ratio to 68.4 μg/mg, and restores the activity and expression of renal SIRT1[1]. NSC 90469 (3,5-diiodo-L-thyronine) (250 μg/kg, i.p.; once daily for 1 week) increases resting energy expenditure by 13% in hypothyroid Wistar rats. It activates brown adipose tissue thermogenesis by enhancing mitochondrial function, sympathetic innervation and angiogenesis, while promoting the multilocular brown adipocyte phenotype, without affecting serum T3/T4 levels[2]. NSC 90469 (100 µg/kg, i.p.; single administration) enhances cold tolerance, increases energy expenditure, and prolongs survival time in hypothyroid rats exposed to low-temperature environments[4]. NSC 90469 (250 µg/kg; daily administration; for 4 consecutive weeks) prevents high-fat diet (HFD)-induced obesity, hepatic lipid accumulation, hyperlipidemia and insulin resistance in rats without inducing thyrotoxicosis[4]. NSC 90469 (1.25 mg/100 g body weight; p.o.; daily) reduces total cholesterol and low-density lipoprotein (LDL) cholesterol by 70% in Western diet-fed Ldlr knockout mice[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reduced kidney weight/body weight ratio to 6.1 mg/g, compared to 13.6 mg/g in untreated diabetic rats. Lowered blood glucose to 6.3 mM/L, compared to 22.1 mM/L in untreated diabetic rats. Decreased 24-hour total urine protein to 13.5 mg, compared to 52.7 mg in untreated diabetic rats. Reduced urine albumin to 20.7 μg/dL, compared to 29.7 μg/dL in untreated diabetic rats. Lowered urine albumin/creatinine ratio to 68.4 μg/mg, compared to 108.3 μg/mg in untreated diabetic rats. Attenuated glomerulosclerosis index and renal fibrosis percentage, compared to untreated diabetic rats. Increased renal SIRT1 protein expression and activity, compared to untreated diabetic rats. Reduced renal mRNA and protein levels of TGF-β1, fibronectin, and collagen IV, compared to untreated diabetic rats. Suppressed renal acetylated NF-κB and phosphorylated JNK levels, compared to untreated diabetic rats.
Animal Model:
Wistar rats (male, 275-300 g, hypothyroidism induced by 4 weeks of intraperitoneal injection of 1 mg/100 g body weight propylthiouracil plus weekly intraperitoneal injection of 6 mg/100 g body weight iopanoic acid)[2]
Dosage:
250 μg/kg
Administration:
i.p.; daily; 1 week; i.p.; single dose 1 hour before euthanasia
Result:
Increased resting energy expenditure by 13% compared to untreated hypothyroid rats. Raised brown adipose tissue contribution to total body weight by 31% compared to untreated hypothyroid rats. Increased multilocular adipocyte percentage to 78% (from 59% in untreated hypothyroid rats). Reduced unilocular adipocyte percentage to 2% (from 10% in untreated hypothyroid rats). Decreased multilocular adipocyte area by 29% compared to untreated hypothyroid rats. Decreased lipid droplet diameter by 38% compared to untreated hypothyroid rats. Increased sympathetic innervation (TH immunoreactive fibers per adipocyte) by 140% compared to untreated hypothyroid rats. Increased vascularization (BS-1 positive capillaries per adipocyte) by 43% compared to untreated hypothyroid rats. Increased mitochondrial content by 35% compared to untreated hypothyroid rats. Increased cytochrome oxidase (COX) activity by 65% compared to untreated hypothyroid rats, restoring it to euthyroid levels. Restored citrate synthase activity and VDAC1 content to euthyroid levels from untreated hypothyroid rat reductions. Increased α-glycerophosphate-energized mitochondrial respiration by 70% in whole brown adipose tissue homogenates compared to untreated hypothyroid rats. Increased basal respiration by 30% in isolated mitochondria compared to untreated hypothyroid rats. Increased arachidonic acid-induced respiration (at 180 μM) by 62% compared to baseline in treated rats, a greater response than the 31% increase in untreated hypothyroid rats. Increased UCP1 protein levels compared to untreated hypothyroid rats. Induced a transient increase in nuclear PGC-1α levels with a single injection 1 hour before euthanasia. Increased mitochondrial PGC-1α levels to euthyroid levels with 1 week of daily administration. Did not affect serum T3/T4 levels, which remained significantly lower than euthyroid levels.
Prevented body weight gain, liver adiposity, hyperlipidemia, and insulin resistance. Detected no signs of thyrotoxicosis (tachycardia, cardiac hyperplasia, decreased thyroid stimulating hormone levels).
Reduced circulating total and LDL cholesterol by 70% compared to controls. Reduced liver apoB levels and circulating apoB48 and apoB100 levels. Reduced plasma T4 levels and caused signs of thyrotoxicosis.
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture and light
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvent & Solubility
In Vitro:
DMSO : 25 mg/mL (47.61 mM; ultrasonic and adjust pH to 2 with 1 M HCL; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Ethanol : 22.22 mg/mL (42.32 mM; ultrasonic and adjust pH to 2 with 1M HCl)
Preparing Stock Solutions
ConcentrationSolventMass
1 mg
5 mg
10 mg
1 mM
1.9045 mL
9.5224 mL
19.0447 mL
5 mM
0.3809 mL
1.9045 mL
3.8089 mL
10 mM
0.1904 mL
0.9522 mL
1.9045 mL
View the Complete Stock Solution Preparation Table
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day. The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.76 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3
Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.76 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (25.0 mg/mL) to 900 μLCorn oil, and mix evenly.
Protocol 4
Add each solvent one by one: 10% EtOH 40% PEG300 5% Tween-80 45% Saline
This protocol yields a clear solution of ≥ 2.22 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (22.2 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 5
Add each solvent one by one: 10% EtOH 90% (20% SBE-β-CD in Saline)
This protocol yields a clear solution of ≥ 2.22 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (22.2 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage
mg/kg
Animal weight (per animal)
g
Dosing volume (per animal)
μL
Number of animals
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO+
%
+
%
Tween-80
+
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO,
. All of co-solvents are available by MedChemExpress (MCE).
, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration:
mg/mL
Method for preparing stock solution:
mg
drug dissolved in
μL
DMSO (Stock solution concentration: mg/mL).
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take
μL DMSO stock solution, add
μL .
μL , mix evenly, next add
μL Tween 80, mix evenly, then add
μL Saline.
Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.
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