| Size | Price | Stock | Qty |
|---|---|---|---|
| 10g |
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| Other Sizes |
| ln Vitro |
Axitinib (HY-10065), Lonidamine (HY-B0486), and Pazopanib (HY-10208) are examples of indazole-based agents that have been used in cancer research and show promise as useful building blocks for the creation of new anticancer drugs. In addition, indazole compounds themselves may have anticancer properties[1]. Because indazoles inhibit kinase and monoamine oxidase (MAO) enzymes such as leucinerich repeat kinase enzyme 2 (LRRK2) and glycogen synthase kinase 3 (GSK3), they have demonstrated strong effects against neurological disorders[2]. Several natural and synthetic indazole derivatives, including as SCH772984 (HY-50846), Zanubrutinib (HY-101474A), Nigellicine, Nigellamine, and Nigellidine, have demonstrated notable efficacy in treating a range of gastrointestinal disorders[4].
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| References |
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| Additional Infomation |
1H-indazole is an indazole compound and is a tautomer of 2H-indazole. Indazole is a class of heterocyclic aromatic organic compounds formed by the fusion of a benzene ring and a pyrazole ring. Indazole is a heterocyclic compound with a bicyclic structure, which is formed by the fusion of a pyrazole ring and a benzene ring. It exists in two tautomers: 1H-indazole and 2H-indazole, of which 1H-indazole is more thermodynamically stable. [3] Indazole derivatives are an important class of pharmacologically active substances and are the basic structure of many marketed drugs and compounds under investigation. They have a wide range of biological activities, including cardiovascular activity (antiarrhythmic, antihypertensive), metabolic activity, antibacterial activity, central nervous system activity, anticancer activity and anti-inflammatory activity. [3] This review summarizes the structure and pharmacological functions of a variety of indazole derivatives, which have shown efficacy against cardiovascular diseases under experimental conditions, and emphasizes their potential as cardioprotective agents. [3]
The indazole ring can be functionalized selectively at different positions, and modifications to its planarity, side chains, and chain length can generate a large number of derivatives with different therapeutic properties. [3] Currently, only a few drugs containing the indazole ring are specifically developed for cardiovascular diseases. Promising indazole derivatives discussed in this article include: DY-9760e (a calmodulin antagonist for ischemia/reperfusion injury), YC-1 (for circulatory system diseases), ARRY-797 (a p38α kinase inhibitor for dilated cardiomyopathy), Indazole-Cl (an ERβ agonist for atherosclerosis), and 7-nitroindazole (a neuronal nitric oxide synthase inhibitor). [3] This review also points out that although some studies have shown that indazole derivatives have beneficial effects, more toxicity studies are needed to evaluate the adverse reactions of indazole derivatives in addition to single studies on 7-nitroindazole. [3] |
| Molecular Formula |
C7H6N2
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|---|---|
| Molecular Weight |
118.14
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| Exact Mass |
118.053
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| CAS # |
271-44-3
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| PubChem CID |
9221
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| Appearance |
Light brown to yellow solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
270.0±9.0 °C at 760 mmHg
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| Melting Point |
145-148 °C(lit.)
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| Flash Point |
128.5±11.7 °C
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| Vapour Pressure |
0.0±0.5 mmHg at 25°C
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| Index of Refraction |
1.697
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| LogP |
1.82
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
1
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
9
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| Complexity |
103
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C12=CC=CC=C1NN=C2
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| InChi Key |
BAXOFTOLAUCFNW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C7H6N2/c1-2-4-7-6(3-1)5-8-9-7/h1-5H,(H,8,9)
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| Chemical Name |
1H-indazole
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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: ≥ 100 mg/mL (~846.5 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (42.32 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 (50.0 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: ≥ 5 mg/mL (42.32 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 (50.0 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: ≥ 5 mg/mL (42.32 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 (50.0 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 | 8.4645 mL | 42.3227 mL | 84.6453 mL | |
| 5 mM | 1.6929 mL | 8.4645 mL | 16.9291 mL | |
| 10 mM | 0.8465 mL | 4.2323 mL | 8.4645 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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