TD-198946 |
| Catalog No.GC14213 |
티에노인다졸 유도체인 TD-198946은 강력한 연골 형성제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 364762-86-7
Sample solution is provided at 25 µL, 10mM.
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TD-198946, a thienoindazole derivative, is a potent chondrogenic agent.
TD-198946 is a potent chondrogenic agent. TD-198946 strongly induces chondrogenic differentiation without promoting hypertrophy in cell and metatarsal organ cultures. TD-198946 induces stronger Col2a1 promoter activity than insulin in ATDC5 cells. In C3H10T1/2 cells, ATDC5 cells and primary mouse chondrocytes, TD-198946 dose-dependently stimulates endogenous expression of the chondrocyte markers Col2a1 and Acan, with maximum effects around 1-10 μM[1].
When administered directly into the joint space, TD-198946 successfully prevents and repaires degeneration of the articular cartilage. TD-198946 exerts its effect through the regulation of Runx1 expression, which is downregulated in both mouse and human OA cartilage compared with normal tissue[1]. TD-198946 has disease-modifying effects on progressed osteoarthritis. TD-198946 may prevent the progression of osteoarthritis by acting on the remaining chondrocytes rather than repairing damaged cartilage, it may be most effective as a therapeutic during the early or middle stages of osteoarthritis, before the articular cartilage is fully eroded[2]. Cartilaginous cell-sheets are generated by culturing mouse and canine costal chondrocytes and human mesenchymal stem cells with TD-198946 on temperature-responsive dishes. The transplanted cell-sheets are then successfully used to promote the reconstruction of permanent cartilage, with no evidence of chondrocyte hypertrophy in the knee articular cartilage defects created in mice and canines[3].
References:
[1]. Yano F, et al. A novel disease-modifying osteoarthritis drug candidate targeting Runx1. Ann Rheum Dis. 2013 May;72(5):748-53.
[2]. Yano F, et al. Disease-modifying effects of TD-198946 on progressed osteoarthritis in a mouse model. Ann Rheum Dis. 2014 Nov;73(11):2062-4.
[3]. Yano F, et al. Cell-sheet technology combined with a thienoindazole derivative small compound TD-198946 for cartilage regeneration. Biomaterials. 2013 Jul;34(22):5581-7.
Animal experiment: | Mice: Each of the prevention and repair models had two groups: (1) TD-198946-treated animals and (2) saline-treated animals. In all the mice tested the left knee joints underwent the operation and the right knee joints are sham-operated. Mice are re-anaesthetised and given a 10 µL intra-articular injection of TD-198946 or saline immediately after surgery (prevention model) or 4 weeks following surgery (repair model) every 5 days for 8 or 4 weeks, respectively[1]. |
References: [1]. Yano F, et al. A novel disease-modifying osteoarthritis drug candidate targeting Runx1. Ann Rheum Dis. 2013 May;72(5):748-53. | |
| Cas No. | 364762-86-7 | SDF | |
| Chemical Name | 1-methyl-8-(4-(quinolin-2-ylmethoxy)phenoxy)-4,5-dihydro-1H-thieno[3,4-g]indazole-6-carboxamide | ||
| Canonical SMILES | CN1C2=C(C=N1)CCC(C2=C3OC4=CC=C(OCC5=NC6=CC=CC=C6C=C5)C=C4)=C(S3)C(N)=O | ||
| Formula | C27H22N4O3S | M.Wt | 482.55 |
| Solubility | DMSO : ≥ 28 mg/mL (58.03 mM) | 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 | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.0723 mL | 10.3616 mL | 20.7232 mL |
| 5 mM | 0.4145 mL | 2.0723 mL | 4.1446 mL |
| 10 mM | 0.2072 mL | 1.0362 mL | 2.0723 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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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 ddH2O, 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
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 5 reference(s) in Google Scholar.)
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