| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
Indazole-Cl targets the estrogen receptor beta (ERβ). It is a selective ERβ agonist with >100-fold selectivity for ERβ over ERα. By activating ERβ, it modulates estrogen receptor signaling. It also has inflammatory effects and inhibits COX-2 expression reduction induced by hypoxia. It prevents hypoxia-induced VSMC migration and invasion.
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|---|---|
| ln Vitro |
Vascular smooth muscle cells (VSMC) with hypoxia-induced intracellular ROS levels are lessened by indazole-Cl (0.1 μM; 6 hours) [1]. Induction of oxidative synthase in VSMCs by hypoxia is inhibited by indazole-Cl (10 μM; 24 hours). VSMCs' internalization and hypoxia-induced cell migration are inhibited by indazole-Cl (1 μM; 24-72 hours) [1].
Indazole-Cl is a selective ERβ agonist and a selective estrogen receptor modifier (SERM). It has inflammatory effects. It inhibits the hypoxia-induced decrease in COX-2 expression and inhibits ROS production. It prevents hypoxia-induced VSMC migration and invasion. Its activity has been confirmed in various in vitro and in vivo studies. |
| ln Vivo |
Indazole-Cl prevents hypoxia-induced VSMC migration and invasion. It inhibits the hypoxia-induced decrease in COX-2 expression and inhibits ROS production. Its effects on estrogen receptor signaling and inflammation make it a valuable research tool for studying the role of ERβ in various physiological and pathological processes.
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| Enzyme Assay |
The primary in vitro assays for Indazole-Cl include radioligand binding assays to measure its affinity for ERβ and ERα. The compound's ability to displace labeled estradiol from ERβ and ERα is measured to determine its selectivity. Functional assays measure its ability to activate ERβ-mediated transcription in reporter gene assays. Its effects on COX-2 expression and ROS production are assessed in cell-based assays.
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| Cell Assay |
In vitro cellular experiments for Indazole-Cl involve treating cells, such as vascular smooth muscle cells, with the compound and measuring its effects on ERβ activation, COX-2 expression, ROS production, and cell migration. The activation of ERβ is assessed by measuring the expression of ERβ target genes. COX-2 expression is measured by Western blot or qPCR. ROS production is measured using fluorescent probes. Cell migration is assessed using wound healing or transwell migration assays.
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| Animal Protocol |
In vivo animal experiments for Indazole-Cl are not extensively detailed in the available literature. As an ERβ agonist, it could be evaluated in animal models of cardiovascular disease, inflammation, or cancer where ERβ plays a role. Its effects on disease progression and inflammatory markers would be assessed.
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| ADME/Pharmacokinetics |
Indazole-Cl has a molecular weight of 260.68 and a molecular formula of C13H9ClN2O2. It is a selective ERβ agonist with >100-fold selectivity for ERβ over ERα. The compound has a CAS number of 848142-62-1. It is a selective estrogen receptor modifier (SERM). It is typically used as a research reagent.
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| Toxicity/Toxicokinetics |
Indazole-Cl is a research compound that is not intended for human use. Its toxicological profile is not extensively characterized in the available literature. As with all research chemicals, standard safety precautions should be followed when handling. Its safety would need to be established for therapeutic applications.
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| References | |
| Additional Infomation |
Indazole-Cl (Ind-Cl) is a selective estrogen receptor modifier (SERM) and a selective ERβ agonist with >100-fold selectivity for ERβ over ERα. It has inflammatory effects and inhibits the hypoxia-induced decrease in COX-2 expression and ROS production. It prevents hypoxia-induced VSMC migration and invasion.
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| Molecular Formula |
C13H9CLN2O2
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|---|---|
| Molecular Weight |
260.67
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| Exact Mass |
260.035
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| CAS # |
848142-62-1
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| PubChem CID |
11368987
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| Appearance |
Off-white to light brown solid powder
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| LogP |
3.09
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
18
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| Complexity |
297
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| Defined Atom Stereocenter Count |
0
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| SMILES |
OC1=CC=C(N2N=C3C=CC(=CC3=C2Cl)O)C=C1
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| InChi Key |
ZNHQDSBJVFFIAK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H9ClN2O2/c14-13-11-7-10(18)5-6-12(11)15-16(13)8-1-3-9(17)4-2-8/h1-7,17-18H
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| Chemical Name |
3-chloro-2-(4-hydroxyphenyl)indazol-5-ol
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| Synonyms |
Indazole Cl; Indazole-Cl
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| 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: ~100 mg/mL (~383.6 mM; with ultrasonication)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.59 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 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 DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and 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 (9.59 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 DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. 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. Solubility in Formulation 3: 2.5 mg/mL (9.59 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Suspended solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.8363 mL | 19.1813 mL | 38.3627 mL | |
| 5 mM | 0.7673 mL | 3.8363 mL | 7.6725 mL | |
| 10 mM | 0.3836 mL | 1.9181 mL | 3.8363 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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