ML224 (Synonyms: NCGC00242364; ANTAG3) |
カタログ番号GC12956
One-Click Copy Product Info
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ML224(NCGC00242364; ANTAG3) は選択的 TSHR 逆アゴニストです。 TSH 刺激による cAMP 産生を IC50 = 2.3 μM で阻害します。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1338824-21-7
Sample solution is provided at 25 µL, 10mM.
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ML224(NCGC00242364; ANTAG3) is a selective TSHR inverse agonist; inhibits TSH-stimulated cAMP production with an IC50 = 2.3 μM.IC50 value: 2.3 uM [1]Target: TSHR agonistin vitro: ANTAG3 was selective for TSHR inhibition; half-maximal inhibitory doses were 2.1 μM for TSHR and greater than 30 μM for LH and FSH receptors [2]. in vivo: In mice treated with TRH, ANTAG3 lowered serum free T4 by 44% and lowered mRNAs for sodium-iodide cotransporter and thyroperoxidase by 75% and 83%, respectively. In mice given M22, ANTAG3 lowered serum free T4 by 38% and lowered mRNAs for sodium-iodide cotransporter and thyroperoxidase by 73% and 40%, respectively [2].
References:
[1]. Huang W, et al. Identification of Thyroid Stimulating Hormone Receptor Inverse Agonists. Probe Reports from the NIH Molecular Libraries Program
[2]. Neumann S, et al. A selective TSH receptor antagonist inhibits stimulation of thyroid function in female mice. Endocrinology. 2014 Jan;155(1):310-4.
| Cas No. | 1338824-21-7 | SDF | |
| 同義語 | NCGC00242364; ANTAG3 | ||
| Canonical SMILES | COC(C(COC1=C(C)C=C(NC(C)=O)C=C1C)=C2)=CC=C2C(NC3=C4C=CC=C3)N(C4=O)CC5=CC=CO5 | ||
| Formula | C31H31N3O5 | M.Wt | 525.59 |
| 溶解度 | ≥ 17.05mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9026 mL | 9.5131 mL | 19.0262 mL |
| 5 mM | 380.5 μL | 1.9026 mL | 3.8052 mL |
| 10 mM | 190.3 μL | 951.3 μL | 1.9026 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 13 reference(s) in Google Scholar.)