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| | 5-Amino-1-(3,5-dichloro-4-(4-chlorobenzoyl)benzyl)-1H-1,2,3-triazole-4-carboxamide Basic information |
| Product Name: | 5-Amino-1-(3,5-dichloro-4-(4-chlorobenzoyl)benzyl)-1H-1,2,3-triazole-4-carboxamide | | Synonyms: | 5-Amino-1-[3,5-dichloro-4-(4-chlorobenzoyl)benzyl]-1H-[1,2,3]triazole-4-carboxylic acid amide;1H-1,2,3-TRIAZOLE-4-CARBOXAMIDE-5-AMINO-1-[[3,5-DICHLORO-4-(4-CHLOROBENZOYL)PHENYL]METHYL];5-Amino-1-(3,5-dichloro-4-(4-chlorobenzoyl)benzyl)-1H-1,2,3-triazole-4-carboxamide;1-[3,5-Dichloro-4-(4-chlorobenzoyl)benzyl]-5-amino-1H-1,2,3-triazole-4-carboxamide;5-Amino-1-[4-(4-chlorobenzoyl)-3,5-dichlorobenzyl]-1H-1,2,3-triazole-4-carboxamide;L-651582;carboxyaMido-triazole(5-AMino-1-(3,5-dichloro-4-(4-chlorobenzoyl)benzyl)-1H-1,2,3-triazole-4-carboxaMide);Merck L651582 5-aMino-1-[3,5-dichloro-4-(4-chloro-benzoyl)-benzyl]-1H-[1,2,3]triazole-4-carboxylic acid aMide | | CAS: | 99519-84-3 | | MF: | C17H12Cl3N5O2 | | MW: | 424.67 | | EINECS: | | | Product Categories: | | | Mol File: | 99519-84-3.mol |  |
| | 5-Amino-1-(3,5-dichloro-4-(4-chlorobenzoyl)benzyl)-1H-1,2,3-triazole-4-carboxamide Chemical Properties |
| Melting point | 200-202 °C | | Boiling point | 685.5±65.0 °C(Predicted) | | density | 1.65±0.1 g/cm3(Predicted) | | storage temp. | Store at +4°C | | solubility | DMSO: soluble10mg/mL (clear solution) | | form | powder | | pka | 14.16±0.50(Predicted) | | color | white to beige | | InChI | 1S/C17H12Cl3N5O2/c18-10-3-1-9(2-4-10)15(26)13-11(19)5-8(6-12(13)20)7-25-16(21)14(17(22)27)23-24-25/h1-6H,7,21H2,(H2,22,27) | | InChIKey | WNRZHQBJSXRYJK-UHFFFAOYSA-N | | SMILES | NC(=O)c1nnn(Cc2cc(Cl)c(c(Cl)c2)C(=O)c3ccc(Cl)cc3)c1N |
| Hazard Codes | T | | Risk Statements | 25 | | Safety Statements | 45 | | RIDADR | UN 2811 6.1 / PGIII | | WGK Germany | 3 | | Storage Class | 6.1C - Combustible acute toxic Cat.3
toxic compounds or compounds which causing chronic effects | | Hazard Classifications | Acute Tox. 3 Oral |
| | 5-Amino-1-(3,5-dichloro-4-(4-chlorobenzoyl)benzyl)-1H-1,2,3-triazole-4-carboxamide Usage And Synthesis |
| Uses | Carboxyamidotriazole is an orally active calcium channel blocker. Carboxyamidotriazole also exhibits inhibition of pro-inflammatory cytokines in tumor associated macrophages as potential anti-cancer m
echanism. | | Biological Activity | Orally active Ca 2+ channel blocker; inhibits K + - and carbachol-stimulated Ca 2+ influx (IC 50 values are 500 and 935 nM respectively). Exhibits antiproliferative, antiangiogenic and antimetastatic activity in vivo and displays selectivity towards numerous mismatch repair-deficient tumor cell lines in vitro . | | in vivo | Carboxyamidotriazole (30 mg/kg; i.g.; daily; 19 days) combined with 2-deoxyglucose retards the growth of LLC tumors in C57BL/6 mice[4].
Carboxyamidotriazole (10-40 mg/kg; i.g.; once daily; from day 12 to day 26 after arthritis induction) reduces the severity of arthritis, inhibits hind paw swelling, decreases the infiltration of joint pathological inflammatory cells in the adjuvant arthritis model of Lewis rats induced by complete Freund's adjuvant[9].
Carboxyamidotriazole (30 mg/kg; i.g.; once daily; from day 7 to day 29 after inoculation of tumor cells) inhibits tumor growth, enhances the weights of gastrocnemius muscle and epididymal adipose tissue in the C57BL/6J mouse model inoculated with Lewis lung carcinoma cells[10].
Carboxyamidotriazole (30 mg/kg; i.g.; once daily; for 29 days) combined with low-dose Sorafenib (HY-10201) synergistically inhibits tumor growth in the C57BL/6J mouse model inoculated with Lewis lung carcinoma cells[11].
Carboxyamidotriazole (20 mg/kg; i.g.; once daily) combined with 1-MT or DMF, increases the number of CD8+ T cells in tumor-infiltrating lymphocytes (TILs), enhances the anti-tumor immune response of T cells, inhibits tumor growth, and prolongs the survival in the C57BL/6, BALB/c or RAG1 KO mouse models inoculated with B16, C26, 4T1 or B16-OVA tumor cells[12].
Carboxyamidotriazole (40 mg/kg, p.o., once daily, 14 days) reduces Bleomycin (HY-108345)-induced lung injury in mice[13].
| Animal Model: | C57BL/6 mice (weight: 18-22 g) + LLC xenograft model[4] | | Dosage: | Carboxyamidotriazole (30 mg/kg, dissolved in PEG 400), 2-DG (450 mg/kg) | | Administration: | Carboxyamidotriazole was administered intragastrically daily, and 2-DG was administered intraperitoneally daily for 19 days | | Result: | Caused no obvious changes in the animal body weight and behaviors.
Resulted in slower tumor growth than in the groups treated with Carboxyamidotriazole or 2-DG alone.
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| Animal Model: | C57BL/6J male mice (weight: 18-22 g, 6-8 weeks old) inoculated with Lewis lung carcinoma cells[11] | | Dosage: | 30 mg/kg | | Administration: | Intragastric administration, once daily, 29 days | | Result: | Synergistically inhibited tumor growth in combination with low-dose Sorafenib.
Showed comparable efficacy to high-dose Sorafenib monotherapy.
Alleviated weight loss during cancer progression and inhibited NANOG expression in tumor tissues.
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| | storage | Store at +4°C |
| | 5-Amino-1-(3,5-dichloro-4-(4-chlorobenzoyl)benzyl)-1H-1,2,3-triazole-4-carboxamide Preparation Products And Raw materials |
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