Carboxyamidotriazole

Carboxyamidotriazole is an orally bioavailable, non-selective calcium channel blocker. It blocks L- and T-type calcium channels in GH3 rat pituitary cancer cells (IC50s = 0.5 and 1.5 µg/ml, respectively). It also inhibits calcium influx stimulated by the acetylcholine receptor agonist carbachol (carbamoylcholine, Cay-14486) and the calcium ionophore A23187 (Cay-11016, Cay-22030) in CHO cells expressing human recombinant muscarinic M5 receptors (IC50s = 935 and 359 nM, respectively). Carboxyamidotriazole inhibits the growth of T. gondii in non-cancerous human fibroblasts and HeLa human cervical cancer cells (IC50 = 0.06 µg/ml for both). It inhibits the growth of FaDu and EVSCC17M human squamous cell carcinoma cells (IC50s = 13 and 15 µM, respectively) and of human umbilical vein endothelial cells (HUVECs, IC50 = 1 µM) in vitro. Carboxyamidotriazole (20 µM) also inhibits angiogenesis in a chicken chorioallantoic membrane assay in vivo.Formal Name: 5-amino-1-[[3,5-dichloro-4-(4-chlorobenzoyl)phenyl]methyl]-1H-1,2,3-triazole-4-carboxamide. CAS Number: 99519-84-3. Synonyms: CAI, L-651,582, NSC 609974. Molecular Formula: C17H12Cl3N5O2. Formula Weight: 424.7. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: slightly soluble, Methanol: slightly, heated. SMILES: ClC1=CC=C(C(C2=C(Cl)C=C(CN3N=NC(C(N)=O)=C3N)C=C2Cl)=O)C=C1. InChi Code: 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). InChi Key: WNRZHQBJSXRYJK-UHFFFAOYSA-N.