| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
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| Targets |
miR-377 and miR-421; TGP-377/421 is a potent dual inhibitor that binds to and inhibits miR-377 and miR-421 at their functional sites. It targets the Dicer processing site of miR-377 with a Kd of 29 μM. By inhibiting these miRNAs, it modulates the expression of their target genes, which are involved in cancer progression and immune regulation.
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| ln Vitro |
In vitro, TGP-377/421 binds to miR-377's Dicer processing site with a Kd of 29 μM. It inhibits the processing of pre-miR-377. It is used in cell-based assays to study the effects of miR-377 and miR-421 inhibition on gene expression and cell function.
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| ln Vivo |
Specific in vivo activity data for TGP-377/421 are not extensively documented. As a miRNA inhibitor, it has potential in cancer research. In vivo studies would be required to evaluate its efficacy and pharmacokinetic properties.
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| Enzyme Assay |
In vitro, the binding affinity of TGP-377/421 to miR-377 is measured using surface plasmon resonance or other biophysical techniques. The inhibition of miRNA processing is assessed by measuring the levels of mature miRNA using qRT-PCR.
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| Cell Assay |
In cell-based assays, cells are treated with TGP-377/421. The compound is typically dissolved in DMSO. The levels of miR-377 and miR-421 are measured by qRT-PCR to confirm inhibition. The effects on target gene expression, cell proliferation, and apoptosis are assessed.
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| Animal Protocol |
In vivo protocols would involve administering TGP-377/421 to tumor-bearing mice. The compound would be given via oral or intraperitoneal routes. Efficacy would be evaluated by measuring tumor growth inhibition and changes in miRNA target gene expression.
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| ADME/Pharmacokinetics |
Dosing and administration routes would need to be established through preclinical studies. TGP-377/421 has a molecular weight of 340.38 and formula C20H16N6. It is soluble in DMSO. Purity: 99%. Storage: Store at -20°C.
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| Toxicity/Toxicokinetics |
Specific toxicity data are not extensively documented. The compound is for research use only. It should be handled with appropriate safety precautions.
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| Additional Infomation |
TGP-377/421 is also known as Targapre-miR-377/421. It is a potent miR-377 and miR-421 inhibitor.
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| Molecular Formula |
C20H16N6
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|---|---|
| Molecular Weight |
340.38
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| Exact Mass |
340.14
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| Elemental Analysis |
C, 70.57; H, 4.74; N, 24.69
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| CAS # |
16752-89-9
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| PubChem CID |
708725
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| Appearance |
Light yellow to brown solid powder
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| LogP |
3
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
26
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| Complexity |
459
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC(=CC(=C1)C2=NC3=C(N2)C=C(C=C3)N)C4=NC5=C(N4)C=C(C=C5)N
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| InChi Key |
AQEJANNNADGRSY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H16N6/c21-13-4-6-15-17(9-13)25-19(23-15)11-2-1-3-12(8-11)20-24-16-7-5-14(22)10-18(16)26-20/h1-10H,21-22H2,(H,23,25)(H,24,26)
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| Chemical Name |
2-[3-(6-amino-1H-benzimidazol-2-yl)phenyl]-3H-benzimidazol-5-amine
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| Synonyms |
TGP-377421; TGP 377421; TGP377421; TGP-377/421; TGP 377/421; TGP377/421; Targapre-miR-377/421; Targapre-miR377/421; Targapre-miR 377/421;
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : ~66.67 mg/mL (~195.87 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.34 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.34 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9379 mL | 14.6895 mL | 29.3789 mL | |
| 5 mM | 0.5876 mL | 2.9379 mL | 5.8758 mL | |
| 10 mM | 0.2938 mL | 1.4689 mL | 2.9379 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.
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