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Omzotirome (TRC-150094) 1092551-88-6

Omzotirome (TRC-150094) 1092551-88-6

CAS No.: 1092551-88-6

Omzotirome (TRC150094) is a functional analog of iodothyronine that may be utilized in the research/study of hyperlipide
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This product is for research use only, not for human use. We do not sell to patients.

Omzotirome (TRC150094) is a functional analog of iodothyronine that may be utilized in the research/study of hyperlipidemia (WO2008149379).

Physicochemical Properties


Molecular Formula C19H24N2O3
Molecular Weight 328.41
Exact Mass 328.179
CAS # 1092551-88-6
PubChem CID 25125529
Appearance White to off-white solid powder
LogP 3.068
Hydrogen Bond Donor Count 2
Hydrogen Bond Acceptor Count 4
Rotatable Bond Count 5
Heavy Atom Count 24
Complexity 458
Defined Atom Stereocenter Count 0
SMILES

CC1=CC(=C2CCCC2=C1O)CC3=C(C)N(CCC(=O)O)N=C3C

InChi Key OFUOCIUIWKDKPA-UHFFFAOYSA-N
InChi Code

InChI=1S/C19H24N2O3/c1-11-9-14(15-5-4-6-16(15)19(11)24)10-17-12(2)20-21(13(17)3)8-7-18(22)23/h9,24H,4-8,10H2,1-3H3,(H,22,23)
Chemical Name

3-[4-[(7-hydroxy-6-methyl-2,3-dihydro-1H-inden-4-yl)methyl]-3,5-dimethylpyrazol-1-yl]propanoic acid
HS Tariff Code 2934.99.9001
Storage

Powder-20°C 3 years

4°C 2 years

In solvent -80°C 6 months

-20°C 1 month

Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light.
Shipping Condition Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity


ln Vivo Rats on a high-fat diet given omzotirome (0.750 mg/100 g; ip) show markedly reduced visceral adipose tissue compared to those on a high-fat diet. They also show altered metabolism in two major tissues, which are metabolically very active, and increased energy expenditure and body weight (BW) gain that are comparable to standard chow-fed rats[1]. In rats fed a high-fat diet (HFD), omzotirome, a functional analog of iodothyronines, decreases obesity by boosting energy expenditure and fatty acid oxidation[1].
Animal Protocol Animal/Disease Models: Male Wistar rats (8 weeks)[1]
Doses: 0.750 mg/ 100 g
Route of Administration: Ip
Experimental Results: With high-fat diet rats had Dramatically less visceral adipose tissue (vs. HFD rats) and demonstrated altered metabolism in two major tissues that were very active metabolically and demonstrated increased energy expenditure and body weight (BW) gain comparable to that of standard chow-fed rats.
References

[1]. WO2008149379.

[2]. TRC150094, a novel functional analog of iodothyronines, reduces adiposity by increasing energy expenditure and fatty acid oxidation in rats receiving a high-fat diet. FASEB J. 2010;24(9):3451-3461.

Additional Infomation TRC150094 is under investigation in clinical trial NCT03254446 (Safety and Efficacy Study of TRC150094 to Improve the CV Risk in Subjects With Diabetes, Dyslipidemia and Hypertension).

Solubility Data


Solubility (In Vitro) DMSO: 100 mg/mL (304.50 mM)
Solubility (In Vivo) Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

Injection Formulations
(e.g. IP/IV/IM/SC)
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution 50 μL Tween 80 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO 400 μLPEG300 50 μL Tween 80 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO 100 μLPEG300 200 μL castor oil 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol 100 μL Cremophor 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300:Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH 400 μLPEG300 50 μL Tween 80 450 μL Saline)

Oral Formulations Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).
Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.0450 mL 15.2249 mL 30.4497 mL
5 mM 0.6090 mL 3.0450 mL 6.0899 mL
10 mM 0.3045 mL 1.5225 mL 3.0450 mL
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.