Details of the Active Pharmaceutical Ingredient (API)

General Information of API (ID: D01001)
Name
Diazoxide
Synonyms    Click to Show/Hide the Synonyms of This API
diazoxide; 364-98-7; Proglycem; Eudemine; Hyperstat; Hypertonalum; Proglicem; Dizoxide; Mutabase; 7-Chloro-3-methyl-2H-1,2,4-benzothiadiazine 1,1-dioxide; Diazossido; Sch 6783; Sch-6783; Diazoxido; Diazoxidum; SRG 95213; SRG-95213; C8H7ClN2O2S; 2H-1,2,4-Benzothiadiazine, 7-chloro-3-methyl-, 1,1-dioxide; UNII-O5CB12L4FN; NSC 76130; NSC-64198; CHEBI:4495; MFCD00078578; 7-chloro-3-methyl-4H-1$l^{6},2,4-benzothiadiazine 1,1-dioxide; O5CB12L4FN; MLS000028459; 7-Cloro-3-metil-2H-1,2,4-benzotiodiazina-1,1-diossido; 364-98-7 (free); Diazossido [Italian]; Diazoxide-d3; NSC64198; NSC76130; NSC-76130; 3-methyl-7-chloro-1,2,4-benzothiadiazine 1,1-dioxide; 7-Chloro-3-methyl-2H-1,2,4-benzothiadiazine1,1-dioxide; Diazossido [DCIT]; NCGC00015380-09; CAS-364-98-7; SMR000058392; 7-Chloro-3-methyl-2H-benzo[e][1,2,4]thiadiazine 1,1-dioxide; DSSTox_CID_2914; Diazoxidum [INN-Latin]; DSSTox_RID_76786; Diazoxido [INN-Spanish]; DSSTox_GSID_22914; 7-chloro-3-methyl-4h-1,2,4-benzothiadiazine 1,1-dioxide; Aroglycem; 7-chloro-3-methyl-4H-benzo[e][1,2,4]thiadiazine 1,1-dioxide; Hyperstat (TN); 1432063-51-8; SR-01000075314; EINECS 206-668-1; NSC 64198; 7-Chloro-3-methyl-2H-1,4-benzothiadiazine 1,1-dioxide; Diazoxide (JAN/USP/INN); Eudimine; 2H-1,4-Benzothiadiazine, 7-chloro-3-methyl-, 1,1-dioxide; 7-chloro-3-methyl-2H-1?^{6},2,4-benzothiadiazine 1,1-dioxide; Eudemine injection; 7-Cloro-3-metil-2H-1,2,4-benzotiodiazina-1,1-diossido [Italian]; Proglycem (TN); Prestwick_163; Diazoxide [USAN:USP:INN:BAN:JAN]; Tocris-0964; Opera_ID_608; Prestwick0_000087; Prestwick1_000087; Prestwick2_000087; Prestwick3_000087; Spectrum3_000735; Spectrum4_001248; Lopac-D-9035; CHEMBL181; D 9035; CBiol_001750; Lopac0_000404; SCHEMBL41254; BSPBio_000014; BSPBio_001307; BSPBio_002290; KBioGR_000027; KBioGR_001776; KBioSS_000027; MLS001076071; MLS001424164; SPECTRUM2300206; SPBio_001953; BPBio1_000016; GTPL2409; CHEMBL1518123; DTXSID7022914; BDBM86248; KBio2_000027; KBio2_002595; KBio2_005163; KBio3_000053; KBio3_000054; KBio3_001510; AOB5782; Bio1_000036; Bio1_000525; Bio1_001014; Bio2_000027; Bio2_000507; HMS1361B09; HMS1568A16; HMS1791B09; HMS1922L22; HMS1989B09; HMS2051P20; HMS2089L04; HMS2093N12; HMS2095A16; HMS2234B23; HMS3261A10; HMS3267I11; HMS3371L13; HMS3393P20; HMS3402B09; HMS3411L18; HMS3675L18; HMS3712A16; HMS3885H12; Pharmakon1600-02300206; 2H-1,2, 4-Benzothiadiazine, 7-chloro-3-methyl-, 1,1-dioxide; 7-Chloro-3-methyl-1lambda~4~,2,4-benzothiadiazin-1-ol 1-oxide; 7-chloro-3-methyl-4H-1lambda6,2,4-benzothiadiazine 1,1-dioxide; BCP26107; HY-B1140; NSC_3019; ZINC3872277; Tox21_110132; Tox21_500404; BDBM50237612; KC-115; NSC759574; s4630; AKOS015896340; AKOS024458715; Tox21_110132_1; ACN-054388; CCG-101062; CCG-204497; CS-4745; DB01119; KS-1444; LP00404; MCULE-5031397425; NC00312; NSC-759574; SDCCGSBI-0050390.P002; IDI1_033777; Diazoxide 100 microg/mL in Acetonitrile; NCGC00015380-01; NCGC00015380-02; NCGC00015380-03; NCGC00015380-04; NCGC00015380-05; NCGC00015380-06; NCGC00015380-07; NCGC00015380-08; NCGC00015380-10; NCGC00015380-11; NCGC00015380-12; NCGC00015380-13; NCGC00015380-20; NCGC00022882-03; NCGC00024907-01; NCGC00024907-02; NCGC00024907-03; NCGC00024907-04; NCGC00024907-05; NCGC00024907-06; NCGC00024907-07; NCGC00024907-08; NCGC00261089-01; CAS_364-98-7; SY066792; DB-048966; B6526; D5402; EU-0100404; FT-0603087; Z3125; VU0239714-6; 2270-EP2281815A1; 2270-EP2295550A2; 2270-EP2301933A1; 2270-EP2308838A1; 2270-EP2311827A1; C06949; D00294; 32273-EP2281815A1; 32273-EP2298415A1; 32273-EP2301933A1; 32273-EP2305640A2; 32273-EP2311827A1; 364D987; A823275; Q420009; SR-01000075314-1; SR-01000075314-3; SR-01000075314-4; SR-01000075314-6; BRD-K73109821-001-05-2; BRD-K73109821-001-10-2; 7-chloro-3-methyl-1,2,4-benzothiadiazine,1,1-dioxide; Diazoxide, European Pharmacopoeia (EP) Reference Standard; 4H-1,2,4-Benzothiadiazine, 7-chloro-3-methyl-, 1,1-dioxide; 7-chloro-3-methyl-4H-1; E?,2,4-benzothiadiazine-1,1-dione; 7-chloro-3-methyl-4h-1; E6,2,4-benzothiadiazine 1,1-dioxide; Diazoxide, United States Pharmacopeia (USP) Reference Standard; 7-chloranyl-3-methyl-4H-1$l^{6},2,4-benzothiadiazine 1,1-dioxide; 7-chloro-3-methyl-2H-1$l^{6},2,4-benzothiadiazine 1,1-dioxide; 7-chloro-3-methyl-4H-1$l^{6},2,4-benzothiadiazine-1,1-dione
Clinical Status
Approved
PubChem CID
3019
Formula
C8H7ClN2O2S
Canonical SMILES
CC1=NS(=O)(=O)C2=C(N1)C=CC(=C2)Cl
InChI
1S/C8H7ClN2O2S/c1-5-10-7-3-2-6(9)4-8(7)14(12,13)11-5/h2-4H,1H3,(H,10,11)
InChIKey
GDLBFKVLRPITMI-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=3019"></iframe>
3D MOL 2D MOL
Physicochemical Properties Molecular Weight 230.67 Topological Polar Surface Area 66.9
XlogP 1.2 Complexity 360
Heavy Atom Count 14 Rotatable Bond Count 0
Hydrogen Bond Donor Count 1 Hydrogen Bond Acceptor Count 3
Full List of Drug Formulations (DFMs) Containing This API
          Diazoxide 1.5g/30ml suspension Click to Show/Hide the Full List of Formulation(s):          2 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
Sorbitol; Propylene Glycol; Carboxymethylcellulose Sodium; Sodium Benzoate; Methylparaben; Poloxamer 188; Propylparaben; Fd&C Red No. 40; Fd&C Yellow No. 6; Water; Alcohol; Hydrochloric Acid; Magnesium Aluminum Silicate
                   Dosage Form Suspension
                   Company Par Pharmaceutical
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Allura red AC dye DIG Info Solute carrier SLCO2B1 (Ki = 4.7 uM) [1]
methylparaben DIG Info Carbonic anhydrase VII (Ki = 780 nM) [2]
Sunset yellow FCF DIG Info Solute carrier SLCO2B1 (Ki = 68.4 uM) [3]
Sodium benzoate DIG Info Carbonic anhydrase II (Ki = 30000 nM) [4]
Allura red AC dye DIG Info Solute carrier SLCO2B1 (Ki = 2.59 uM) [3]
Propylparaben sodium DIG Info Estrogen receptor alpha (EC50 = 38200 nM) [5]
Hydrochloric acid DIG Info Carbonic anhydrase V (Ki = 156 nM) [6]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [7]
Carboxymethylcellulose sodium DIG Info Albendazole monooxygenase (EC50 = 12.6 uM) [8]
Poloxamer 188 DIG Info Albendazole monooxygenase (IC50 = 60 uM) [8]
             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
Sorbitol; Propylene Glycol; Magnesium Aluminum Silicate; Carboxymethylcellulose Sodium; Sodium Benzoate; Methylparaben; Poloxamer 188; Propylparaben; Alcohol; Hydrochloric Acid; Sodium Hydroxide
                   Dosage Form Suspension
                   Company Teva Pharmaceuticals Usa
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
methylparaben DIG Info Carbonic anhydrase VII (Ki = 780 nM) [2]
Sodium benzoate DIG Info Carbonic anhydrase II (Ki = 30000 nM) [4]
Propylparaben sodium DIG Info Estrogen receptor alpha (EC50 = 38200 nM) [5]
Hydrochloric acid DIG Info Carbonic anhydrase V (Ki = 156 nM) [6]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [7]
Carboxymethylcellulose sodium DIG Info Albendazole monooxygenase (EC50 = 12.6 uM) [8]
Poloxamer 188 DIG Info Albendazole monooxygenase (IC50 = 60 uM) [8]
References
1 The activities of drug inactive ingredients on biological targets. Science. 2020 Jul 24;369(6502):403-413.
2 Mono-/dihydroxybenzoic acid esters and phenol pyridinium derivatives as inhibitors of the mammalian carbonic anhydrase isoforms I, II, VII, IX, XII and XIV. Bioorg Med Chem. 2013 Mar 15; 21(6):1564-9.
3 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.
4 Carbonic anhydrase inhibitors. Interaction of isozymes I, II, IV, V, and IX with carboxylates. Bioorg Med Chem Lett. 2005 Feb 1; 15(3):573-8.
5 Discovery of natural estrogen receptor modulators with structure-based virtual screening. Bioorg Med Chem Lett. 2013 Jun 1; 23(11):3329-33.
6 Carbonic anhydrase inhibitors. Inhibition of the newly isolated murine isozyme XIII with anions. Bioorg Med Chem Lett. 2004 Nov 1; 14(21):5435-9.
7 Pharmaceutical excipients inhibit cytochrome P450 activity in cell free systems and after systemic administration. Eur J Pharm Biopharm. 2008 Sep;70(1):279-88.
8 Mediation of in vitro cytochrome p450 activity by common pharmaceutical excipients. Mol Pharm. 2013 Jul 1;10(7):2739-48.

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