Details of the Active Pharmaceutical Ingredient (API)

General Information of API (ID: D00029)
Name
Amiloride
Synonyms    Click to Show/Hide the Synonyms of This API
AMILORIDE; Amipramidin; 2609-46-3; Midamor; Guanamprazine; Amipramizid; Amipramizide; Guanamprazin; Amilorida; Amiloridum; Amyloride; Amiloridum [INN-Latin]; Amilorida [INN-Spanish]; 3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-carboxamide; N-Amidino-3,5-diamino-6-chloropyrazinecarboxamide; N-Amidino-3,5-diamino-6-chlorpyrazincarboxamid; UNII-7DZO8EB0Z3; 3,5-Diamino-N-(aminoiminomethyl)-6-chloropyrazinecarboxamide; MK-870; Amiloride hydrochloride hydrate; CHEMBL945; Pyrazinecarboxamide, 3,5-diamino-N-(aminoiminomethyl)-6-chloro-; 3,5-diamino-6-chloro-N-(diaminomethylidene)pyrazine-2-carboxamide; 7DZO8EB0Z3; CHEBI:2639; N-amidino-3,5-diamino-6-chloro-2-pyrazinecarboxamide; NCGC00015089-08; Amiloride [INN:BAN]; AMIPRAMIDINE; DSSTox_CID_23853; DSSTox_RID_80077; Amiloride Hydrocholride; DSSTox_GSID_43853; C6H8ClN7O; Amiclaran (TN); Amiloride (INN); 137053-86-2; CAS-2609-46-3; CCRIS 6545; EINECS 220-024-7; (3,5-diamino-6-chloropyrazin-2-yl)-N-(???methyl)carboxamide; AmilorideHCl; Amikal (Hydrochloride dihydrate); Midamor (Hydrochloride dihydrate); MK-870 (Hydrochloride dihydrate); Spectrum_000034; Tocris-0890; Prestwick0_000007; Prestwick1_000007; Prestwick2_000007; Prestwick3_000007; Spectrum2_000118; Spectrum3_000293; Spectrum4_000132; Spectrum5_000776; Lopac-A-7410; Lopac0_000111; SCHEMBL27562; BSPBio_000013; BSPBio_001572; BSPBio_001826; KBioGR_000292; KBioGR_000544; KBioSS_000292; KBioSS_000394; MLS001060798; BIDD:GT0466; DivK1c_000182; SPBio_000136; SPBio_001934; BPBio1_000015; GTPL2421; DTXSID9043853; BCBcMAP01_000101; BDBM16173; KBio1_000182; KBio2_000292; KBio2_000394; KBio2_002860; KBio2_002962; KBio2_005428; KBio2_005530; KBio3_000583; KBio3_000584; KBio3_001326; NINDS_000182; Bio1_000359; Bio1_000848; Bio1_001337; Bio2_000292; Bio2_000772; HMS1791O14; HMS1989O14; HMS2089H05; HMS2213E05; HMS3355K04; ACT05635; ACT05652; BCP16815; HY-B0285; ZINC4340269; Tox21_110080; 3,5-diamino-N-[amino(imino)methyl]-6-chloropyrazine-2-carboxamide; BBL028157; SBB037856; STL373007; AKOS015961348; Tox21_110080_1; CCG-204206; DB00594; MCULE-5948863568; SDCCGSBI-0050099.P005; IDI1_000182; IDI1_034042; NCGC00015089-01; NCGC00015089-02; NCGC00015089-03; NCGC00015089-04; NCGC00015089-05; NCGC00015089-06; NCGC00015089-07; NCGC00015089-09; NCGC00015089-11; NCGC00015089-12; NCGC00015089-13; NCGC00015089-14; NCGC00015089-15; NCGC00015089-16; NCGC00015089-17; NCGC00015089-24; NCGC00024443-02; NCGC00024443-05; NCGC00024443-06; NCGC00024443-07; NCGC00024443-09; AC-13631; SMR000486264; ST079279; (3,5-Diamino-6-chloropyrazinoyl)guanidine; SBI-0050099.P004; N-amidino-3,5-diamino-6-chloropyrazinamide; AB00053415; FT-0703177; C06821; D07447; AB00053415-24; AB00053415-25; AB00053415_26; AB00053415_27; AB00053415_28; 117188-EP2277879A1; 117188-EP2298776A1; 609A463; Q419995; J-016249; BRD-K97181089-003-02-3; BRD-K97181089-310-03-0; N-amidino 3,5-diamino-6-chloro-2-pyrazinecarboxamide; F2173-0531; N-(3,5-Diamino-6-chloro-pyrazine-2-carbonyl)-guanidine; 3,5-diamino-N-carbamimidoyl-6-chloro-pyrazine-2-carboxamide; 3,5-diamino-6-chloro-N-(diaminomethylene)pyrazinamide;hydrochloride
Clinical Status
Approved
Disease Indication Essential hypertension ICD-11: BA00 [1]
PubChem CID
16231
Formula
C6H8ClN7O
Canonical SMILES
C1(=C(N=C(C(=N1)Cl)N)N)C(=O)N=C(N)N
InChI
1S/C6H8ClN7O/c7-2-4(9)13-3(8)1(12-2)5(15)14-6(10)11/h(H4,8,9,13)(H4,10,11,14,15)
InChIKey
XSDQTOBWRPYKKA-UHFFFAOYSA-N
   Click to Show/Hide the Molecular Data (Structure/Property) of This API
Structure
<iframe style="width: 300px; height: 300px;" frameborder="0" src="https://embed.molview.org/v1/?mode=balls&cid=16231"></iframe>
3D MOL 2D MOL
Physicochemical Properties Molecular Weight 229.63 Topological Polar Surface Area 159
XlogP -0.7 Complexity 279
Heavy Atom Count 15 Rotatable Bond Count 1
Hydrogen Bond Donor Count 4 Hydrogen Bond Acceptor Count 5
Full List of Drug Formulations (DFMs) Containing This API
          Amiloride 5 mg tablet Click to Show/Hide the Full List of Formulation(s):          7 Formulation(s)
             Drug Formulation 1 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
D&c yellow no. 10; Fd&c yellow no. 6; Magnesium stearate; Dibasic calcium phosphate dihydrate; Croscarmellose sodium; Cellulose, microcrystalline; Colloidal silicon dioxide; Povidone k29/32
                   Dosage Form Oral Tablet
                   Company Cadila Healthcare; Zydus Pharmaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Sunset yellow FCF DIG Info Solute carrier SLCO2B1 (Ki = 68.4 uM) [2]
Quinoline yellow WS DIG Info Estrogen receptor alpha (IC50 = 18 uM) [3]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [4]
             Drug Formulation 2 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
D&c yellow no. 10; Fd&c yellow no. 6; Magnesium stearate; Calcium phosphate, dibasic, dihydrate; Silicon dioxide; Cellulose, microcrystalline
                   Dosage Form Oral Tablet
                   Company Golden State Medical Supply
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Sunset yellow FCF DIG Info Solute carrier SLCO2B1 (Ki = 68.4 uM) [2]
Quinoline yellow WS DIG Info Estrogen receptor alpha (IC50 = 18 uM) [3]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
             Drug Formulation 3 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
D&c yellow no. 10; Fd&c yellow no. 6; Magnesium stearate; Dibasic calcium phosphate dihydrate; Silicon dioxide; Cellulose, microcrystalline
                   Dosage Form Oral Tablet
                   Company Par Pharmaceutical
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Sunset yellow FCF DIG Info Solute carrier SLCO2B1 (Ki = 68.4 uM) [2]
Quinoline yellow WS DIG Info Estrogen receptor alpha (IC50 = 18 uM) [3]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
             Drug Formulation 4 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
D&c yellow no. 10; Fd&c yellow no. 6; Magnesium stearate; Dibasic calcium phosphate dihydrate; Silicon dioxide; Microcrystalline cellulose
                   Dosage Form Oral Tablet
                   Company Carilion Materials Management
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Sunset yellow FCF DIG Info Solute carrier SLCO2B1 (Ki = 68.4 uM) [2]
Quinoline yellow WS DIG Info Estrogen receptor alpha (IC50 = 18 uM) [3]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
             Drug Formulation 5 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Lactose; Magnesium stearate; Crospovidone; Povidone; Cellulose, microcrystalline; Starch, corn
                   Dosage Form Oral Tablet
                   Company AvKARE; AvPAK; Rising Pharmaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [5]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Crospovidone DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
             Drug Formulation 6 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Lactose monohydrate; Magnesium stearate; Calcium phosphate, dibasic, anhydrous; Starch, corn
                   Dosage Form Oral Tablet
                   Company Kaiser Foundation Hospitals; Paddock Laboratories,
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
             Drug Formulation 7 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Lactose; Magnesium stearate
                   Dosage Form Oral Tablet
                   Company Physicians Total Care
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
          Amiloride Hydrochloride 5mg tablet Click to Show/Hide the Full List of Formulation(s):          1 Formulation(s)
             Drug Formulation 1 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Colloidal Silicon Dioxide; Croscarmellose Sodium; D&C Yellow 10 Lake; Dibasic Calcium Phosphate Dihydrate; Fd&C Yellow 6 Lake; Magnesium Stearate; Microcrystalline Cellulose; Silicon Dioxide
                   Dosage Form Tablet
                   Company Bryant Ranch Prepack
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Sunset yellow FCF DIG Info Solute carrier SLCO2B1 (Ki = 68.4 uM) [2]
Quinoline yellow WS DIG Info Estrogen receptor alpha (IC50 = 18 uM) [3]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [4]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
References
1 FDA label for approved amiloride from the official website of the U.S. Food and Drug Administration.
2 Bacterial metabolism rescues the inhibition of intestinal drug absorption by food and drug additives. Proc Natl Acad Sci U S A. 2020 Jul 7;117(27):16009-16018.
3 The activities of drug inactive ingredients on biological targets. Science. 2020 Jul 24;369(6502):403-413.
4 Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.
5 Mediation of in vitro cytochrome p450 activity by common pharmaceutical excipients. Mol Pharm. 2013 Jul 1;10(7):2739-48.

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