| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg | |||
| Other Sizes |
| Targets |
The compound targets the c-MPL receptor (also known as the thrombopoietin receptor or TPO receptor). It acts as a c-MPL agonist (CMA) that activates the receptor to promote megakaryocyte differentiation and platelet production. By binding to and activating the TPO receptor, the compound stimulates the signaling pathways that drive the proliferation and maturation of megakaryocytes, leading to increased platelet generation.
|
|---|---|
| ln Vitro |
The proliferation of Ba/F3-HuMpl and UT-7/TPO cells is stimulated by TA-316 (0.01-1000 nM; 4 days), with EC50 values of 0.65 nM and 0.3 nM, respectively [2]. MK lineage markers are upregulated and biased megakaryopoiesis is encouraged by TA-316 (800 nM; 10 days) [2]. VEGFA and FGF2 expression are preferentially enhanced by TA-316 (200 nM; 4 days) [2].
In vitro, TA-316 enhances ex vivo platelet generation from human-induced pluripotent stem (iPS) cells. The compound promotes the differentiation of iPS cells into megakaryocytes and subsequent platelet production. It acts as a potent agonist of the c-MPL/TPO receptor with efficacy comparable to recombinant human thrombopoietin in some respects. Detailed IC₅0 or EC₅0 values are not extensively documented in the available literature. |
| ln Vivo |
In vivo activity data for TA-316 are not extensively documented in the public domain. As a TPO receptor agonist, the compound is expected to stimulate platelet production in vivo, making it useful for treating thrombocytopenia. The compound is primarily used for ex vivo platelet generation from stem cells. Further in vivo studies would be needed to characterize its efficacy in animal models of platelet deficiency.
|
| Enzyme Assay |
The in vitro assay for c-MPL/TPO receptor agonism typically uses cells expressing the TPO receptor (such as Ba/F3 cells or UT-7/TPO cells). Cells are cultured in the presence of varying concentrations of TA-316, and cell proliferation is measured using MTT, CellTiter-Glo, or [3H]-thymidine incorporation. EC₅0 values are calculated from dose-response curves. Receptor activation is confirmed by measuring downstream signaling markers such as STAT3, STAT5, and MAPK phosphorylation by Western blot.
|
| Cell Assay |
Cell viability assay [2]
Cell Types: UT-7/TPO and Ba /F3-HuMpl Cell Tested Concentrations: 0.01-1000 nM Incubation Duration: 4 days Experimental Results: Stimulated UT-7/TPO and Ba/F3-HuMpl cell proliferation. For in vitro cell-based assays, human-induced pluripotent stem (iPS) cells are differentiated toward the megakaryocyte lineage using specific culture conditions and cytokines. TA-316 is added at various concentrations during the differentiation process. Megakaryocyte differentiation is assessed by flow cytometry using megakaryocyte-specific markers (CD41, CD61, CD42b). Platelet generation is quantified by counting CD41+/CD42b+ particles in the culture supernatant. Experiments are typically performed in triplicate. |
| Animal Protocol |
In vivo animal studies for TPO receptor agonists typically involve mouse or rat models of thrombocytopenia (such as chemotherapy-induced or irradiation-induced models). TA-316 is administered orally or intravenously at various doses. Platelet counts are measured in peripheral blood at multiple time points using automated hematology analyzers. Bone marrow analysis may be performed to assess megakaryocyte numbers and morphology. Efficacy is evaluated by the ability to restore platelet counts to normal levels.
|
| ADME/Pharmacokinetics |
Pharmacokinetic properties of TA-316 are not extensively documented. The compound has molecular weight 641.56 and molecular formula C2₈H2₅BrN4O₅S2. The IUPAC name is (E)-5-(2-(1-(5-(4-bromophenyl)-4-hydroxythiophen-3-yl)ethylidene)hydrazine-1-carbonyl)-N-(4-((2-hydroxyethyl)carbamoyl)benzyl)thiophene-2-carboxamide. Purity is typically ≥99%. Further PK parameters would require dedicated studies.
|
| Toxicity/Toxicokinetics |
Toxicological data for TA-316 are not well characterized in the public domain. As a research chemical, standard safety precautions should be observed. The compound is for laboratory use only and not intended for human therapeutic applications. TPO receptor agonists as a class may have potential thrombotic risks. Comprehensive toxicity profiling would be required for therapeutic development.
|
| References | |
| Additional Infomation |
Megakaryocytes/platelets inducing agent (TA-316, CAS# 1429321-13-0) is a chemically synthesized c-MPL agonist used for platelet generation from iPS cells. The compound is also known as TA-316. It is used in research for treating thrombocytopenia and is not approved for clinical use. GMP-grade versions are available for cell therapy applications.
|
| Molecular Formula |
C28H25BRN4O5S2
|
|---|---|
| Molecular Weight |
641.56
|
| Exact Mass |
640.044
|
| CAS # |
1429321-13-0
|
| PubChem CID |
71533707
|
| Appearance |
White to yellow solid powder
|
| Density |
1.54±0.1 g/cm3(Predicted)
|
| LogP |
4.4
|
| Hydrogen Bond Donor Count |
5
|
| Hydrogen Bond Acceptor Count |
8
|
| Rotatable Bond Count |
10
|
| Heavy Atom Count |
40
|
| Complexity |
911
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C/C(=N\NC(=O)C1=CC=C(S1)C(=O)NCC2=CC=C(C=C2)C(=O)NCCO)/C3=CSC(=C3O)C4=CC=C(C=C4)Br
|
| InChi Key |
SOHAFPZIBGBALX-KPGMTVGESA-N
|
| InChi Code |
InChI=1S/C28H25BrN4O5S2/c1-16(21-15-39-25(24(21)35)18-6-8-20(29)9-7-18)32-33-28(38)23-11-10-22(40-23)27(37)31-14-17-2-4-19(5-3-17)26(36)30-12-13-34/h2-11,15,34-35H,12-14H2,1H3,(H,30,36)(H,31,37)(H,33,38)/b32-16+
|
| Chemical Name |
2-N-[(E)-1-[5-(4-bromophenyl)-4-hydroxythiophen-3-yl]ethylideneamino]-5-N-[[4-(2-hydroxyethylcarbamoyl)phenyl]methyl]thiophene-2,5-dicarboxamide
|
| 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 |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~77.94 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
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *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). View More
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)] 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). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.5587 mL | 7.7935 mL | 15.5870 mL | |
| 5 mM | 0.3117 mL | 1.5587 mL | 3.1174 mL | |
| 10 mM | 0.1559 mL | 0.7794 mL | 1.5587 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.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
